Ahmed Kamal

Summary

Affiliation: Indian Institute of Chemical Technology
Country: India

Publications

  1. Mullagiri K, Nayak V, Sunkari S, Mani G, Guggilapu S, Nagaraju B, et al. New (3-(1H-benzo[d]imidazol-2-yl))/(3-(3H-imidazo[4,5-b]pyridin-2-yl))-(1H-indol-5-yl)(3,4,5-trimethoxyphenyl)methanone conjugates as tubulin polymerization inhibitors. Medchemcomm. 2018;9:275-281 pubmed publisher
    ..Further, the apoptosis-inducing ability of these derivatives (5g and 6f) was confirmed by Hoechst staining, measurement of mitochondrial membrane potential and ROS generation and annexin V-FITC assays. ..
  2. Sankara Rao N, Nagesh N, Lakshma Nayak V, Sunkari S, Tokala R, Kiranmai G, et al. Design and synthesis of DNA-intercalative naphthalimide-benzothiazole/cinnamide derivatives: cytotoxicity evaluation and topoisomerase-IIα inhibition. Medchemcomm. 2019;10:72-79 pubmed publisher
    ..In addition, the most potent derivatives 4a and 4b were also found to inhibit DNA topoisomerase-II. ..
  3. Kamal A, Shaik T, Malik M. Embracing synthetic lethality of novel anticancer therapies. Expert Opin Drug Discov. 2015;10:1119-32 pubmed publisher
    ..Research on PARP inhibitors is progressing at a good pace but there are still some significant challenges that must be addressed. ..
  4. Krishna N, Saraswati A, Sathish M, Shankaraiah N, Kamal A. Silver catalyzed domino aza-annulation/Diels-Alder cyclization of 2-ene-yne anilines: a facile one-pot access to carbazole, dihydrocarbazole and tetrahydrocarbazole frameworks. Chem Commun (Camb). 2016;52:4581-4 pubmed publisher
    ..A series of symmetrical, unsymmetrical and base sensitive dienophiles provide the corresponding carbazoles under mild conditions in excellent yields with high regioselectivity. ..
  5. Reddy C, Sathish M, Adhikary S, Nanubolu J, Alarifi A, Maurya R, et al. Phenacyl azides as efficient intermediates: one-pot synthesis of pyrrolidines and imidazoles. Org Biomol Chem. 2017;15:2730-2733 pubmed publisher
  6. Seddigi Z, Malik M, Saraswati A, Ahmed S, Babalghith A, Lamfon H, et al. Recent advances in combretastatin based derivatives and prodrugs as antimitotic agents. Medchemcomm. 2017;8:1592-1603 pubmed publisher
    ..The present review highlights the investigations into the parallel development of both new CA-4 based derivatives and prodrugs in the past few years. ..
  7. Donthiboina K, Anchi P, Sri Ramya P, Karri S, Srinivasulu G, Godugu C, et al. Synthesis of substituted biphenyl methylene indolinones as apoptosis inducers and tubulin polymerization inhibitors. Bioorg Chem. 2019;86:210-223 pubmed publisher
    ..In addition, morphological changes were clearly observed by AO/EB and DAPI staining studies. Moreover, ROS detection using DCFDA, JC-1, and annexin V-FITC assays demonstrated the significant apoptosis induction by 10e. ..
  8. Rahim A, Shaik S, Baig M, Alarifi A, Kamal A. Iodine mediated oxidative cross-coupling of unprotected anilines and heteroarylation of benzothiazoles with 2-methylquinoline. Org Biomol Chem. 2018;16:635-644 pubmed publisher
    ..These transformations do not require any transition metals or peroxides and tolerate various functional groups such as methoxy, hydroxy, bromo, chloro and nitro groups. Moreover, a plausible mechanistic pathway is proposed. ..
  9. request reprint
    Kamal A, Srikanth Y, Ashraf M, Khan M, Shaik T, Kalivendi S, et al. Synthesis and anticancer activities of new Benzothiadiazinyl Hydrazinecarboxamides and Anilino[1,2,4]triazolo[1,5-b][1,2,4]thiadiazine 5,5-diones. Med Chem. 2011;7:165-72 pubmed
    ..Further studies showed that cancer cell growth inhibition by compounds 22 and 23 could be in part due to the inhibition of tubulin polymerization, with the IC50 values of 4.70 and 5.25 µM, respectively. ..

More Information

Publications100

  1. Kumar N, Vanjari Y, Thatikonda S, Pooladanda V, Sharma P, Sridhar B, et al. Synthesis of enamino-2-oxindoles via conjugate addition between α-azido ketones and 3-alkenyl oxindoles: Cytotoxicity evaluation and apoptosis inducing studies. Bioorg Med Chem Lett. 2018;28:3564-3573 pubmed publisher
    ..Extent of apoptosis was also analyzed by Annexin binding and JC-1 staining. Moreover, this method is amenable for the generation of a library of new class of stable bioactive enamino-2-oxindoles. ..
  2. Kamal A, Kumar G, Vishnuvardhan M, Shaik A, Reddy V, Mahesh R, et al. Synthesis of phenstatin/isocombretastatin-chalcone conjugates as potent tubulin polymerization inhibitors and mitochondrial apoptotic inducers. Org Biomol Chem. 2015;13:3963-81 pubmed publisher
    ..Molecular docking studies indicated that compounds like 3e occupy the colchicine binding site of tubulin. ..
  3. Kamal A, Faazil S, Ramaiah M, Ashraf M, Balakrishna M, Pushpavalli S, et al. Synthesis and study of benzothiazole conjugates in the control of cell proliferation by modulating Ras/MEK/ERK-dependent pathway in MCF-7 cells. Bioorg Med Chem Lett. 2013;23:5733-9 pubmed publisher
    ..Hence these small molecules have the potential to control both the cell proliferation as well as the invasion process in the highly malignant breast cancers. ..
  4. Prasad B, Lakshma Nayak V, Srikanth P, Baig M, Subba Reddy N, Babu K, et al. Synthesis and biological evaluation of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides as antimitotic agents. Bioorg Chem. 2018;83:535-548 pubmed publisher
    ..Thus, 7f exhibits anti-proliferative properties by inhibiting the tubulin polymerization through the binding at the colchicine active site and by induction of apoptosis. ..
  5. Bagul C, Rao G, Makani V, Tamboli J, Pal Bhadra M, Kamal A. Synthesis and biological evaluation of chalcone-linked pyrazolo[1,5-a]pyrimidines as potential anticancer agents. Medchemcomm. 2017;8:1810-1816 pubmed publisher
    ..Molecular docking studies described the binding of these hybrids to the ATP binding site of EGFR. ..
  6. Sayeed I, Vishnuvardhan M, Nagarajan A, Kantevari S, Kamal A. Imidazopyridine linked triazoles as tubulin inhibitors, effectively triggering apoptosis in lung cancer cell line. Bioorg Chem. 2018;80:714-720 pubmed publisher
    ..Overall, the current study demonstrates that the synthesis of imidazopyridine linked triazole conjugates as promising anticancer agents causing G2/M arrest and apoptotic-inducing ability. ..
  7. Sathish M, Chetan Dushantrao S, Nekkanti S, Tokala R, Thatikonda S, Tangella Y, et al. Synthesis of DNA interactive C3-trans-cinnamide linked β-carboline conjugates as potential cytotoxic and DNA topoisomerase I inhibitors. Bioorg Med Chem. 2018;26:4916-4929 pubmed publisher
  8. Kamal A, Reddy T, Vishnuvardhan M, Nimbarte V, Subba Rao A, Srinivasulu V, et al. Synthesis of 2-aryl-1,2,4-oxadiazolo-benzimidazoles: Tubulin polymerization inhibitors and apoptosis inducing agents. Bioorg Med Chem. 2015;23:4608-23 pubmed publisher
    ..Molecular docking studies of compounds 5l and 5x into the colchicine-binding site of the tubulin, revealed the possible mode of interaction by these compounds. ..
  9. Kamal A, Sathish M, Srinivasulu V, Chetna J, Chandra Shekar K, Nekkanti S, et al. Asymmetric Michael addition of ketones to nitroolefins: pyrrolidinyl-oxazole-carboxamides as new efficient organocatalysts. Org Biomol Chem. 2014;12:8008-18 pubmed publisher
    ..These results support the preferential formation of syn-products by the approach of trans-β-nitrostyrene through the re-face of anti-enamine. ..
  10. Kamal A, Babu K, Vishnu Vardhan M, Hussaini S, Mahesh R, Shaik S, et al. Sulfamic acid promoted one-pot three-component synthesis and cytotoxic evaluation of spirooxindoles. Bioorg Med Chem Lett. 2015;25:2199-202 pubmed publisher
    ..Some of the compounds like 4o and 4p exhibited remarkable cytotoxicities with IC50 values of 0.35μM and 1.92μM against MDA-MB-231 cell line. ..
  11. Kamal A, Tamboli J, Ramaiah M, Adil S, Pushpavalli S, Ganesh R, et al. Quinazolino linked 4?-amidopodophyllotoxin conjugates regulate angiogenic pathway and control breast cancer cell proliferation. Bioorg Med Chem. 2013;21:6414-26 pubmed publisher
    ..Thus these conjugates have the potential to control breast cancer cell growth by effecting tumor angiogenesis and invasion. ..
  12. Kamal A, Kumar G, Polepalli S, Shaik A, Reddy V, Reddy M, et al. Design and synthesis of aminostilbene-arylpropenones as tubulin polymerization inhibitors. ChemMedChem. 2014;9:2565-79 pubmed publisher
    ..79 μM. Moreover, dot-blot analysis of cyclin B1 demonstrated that some of the congeners strongly induced cyclin B1 protein levels. Molecular docking studies indicated that these compounds occupy the colchicine binding site of tubulin. ..
  13. Kamal A, Shaik B, Nayak V, Nagaraju B, Kapure J, Shaheer Malik M, et al. Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers. Bioorg Med Chem. 2014;22:5155-67 pubmed publisher
    ..Further, mitochondrial membrane potential, ROS generation, caspase-3 activation assay, Hoechst staining and DNA fragmentation analysis revealed that these conjugates induce cell death by apoptosis. ..
  14. Kamal A, Rao A, Nayak V, Reddy N, Swapna K, Ramakrishna G, et al. Synthesis and biological evaluation of imidazo[1,5-a]pyridine-benzimidazole hybrids as inhibitors of both tubulin polymerization and PI3K/Akt pathway. Org Biomol Chem. 2014;12:9864-80 pubmed publisher
    ..The molecular docking simulations predicted the binding interactions of 5d and 5l with colchicine binding site of the tubulin, which is in compliance with the antiproliferative activity data. ..
  15. Kamal A, Ali Hussaini S, Rahim A, Riyaz S. Podophyllotoxin derivatives: a patent review (2012 - 2014). Expert Opin Ther Pat. 2015;25:1025-34 pubmed publisher
    ..However, its low natural abundance is a major problem in carrying out research on PPT skeleton. This issue is expected to be addressed with the development of newer synthetic strategies to access structurally modified PPTs. ..
  16. Kamal A, Shaik A, Polepalli S, Reddy V, Kumar G, Gupta S, et al. Pyrazole-oxadiazole conjugates: synthesis, antiproliferative activity and inhibition of tubulin polymerization. Org Biomol Chem. 2014;12:7993-8007 pubmed publisher
    ..Elucidation of zebrafish embryos revealed that the conjugates cause developmental defects. Molecular docking simulations determined the binding modes of these potent conjugates at the colchicine site of tubulin. ..
  17. request reprint
    Kamal A, Riyaz S, Srivastava A, Rahim A. Tankyrase inhibitors as therapeutic targets for cancer. Curr Top Med Chem. 2014;14:1967-76 pubmed
    ..The current review covers the progress, mechanism and binding modes of recently known Tankyrase inhibitors and discusses the rational approaches that were used to identify the tankyrase inhibitors. ..
  18. Kamal A, Balakrishna M, Nayak V, Shaik T, Faazil S, Nimbarte V. Design and synthesis of imidazo[2,1-b]thiazole-chalcone conjugates: microtubule-destabilizing agents. ChemMedChem. 2014;9:2766-80 pubmed publisher
    ..Moreover, molecular docking studies indicated that this conjugate (11 x) interacts and binds efficiently with the tubulin protein. ..
  19. Kamal A, Rahim A, Riyaz S, Poornachandra Y, Balakrishna M, Kumar C, et al. Regioselective synthesis, antimicrobial evaluation and theoretical studies of 2-styryl quinolines. Org Biomol Chem. 2015;13:1347-57 pubmed publisher
    ..luteus and S. aureus MLS16. Further, theoretical studies such as those on druggable properties and PMI plot have been carried out. ..
  20. Kamal A, Sreekanth K, Kumar P, Shankaraiah N, Balakishan G, Ramaiah M, et al. Synthesis and potential cytotoxic activity of new phenanthrylphenol-pyrrolobenzodiazepines. Eur J Med Chem. 2010;45:2173-81 pubmed publisher
    ..Our findings suggested the phenanthrylphenol-PBD conjugate 4c, which is a cyclin D1 inhibitor could be considered as a promising lead compound against breast cancer for further investigation. ..
  21. Reddy C, Nayak V, Mani G, Kapure J, Adiyala P, Maurya R, et al. Synthesis and biological evaluation of spiro[cyclopropane-1,3'-indolin]-2'-ones as potential anticancer agents. Bioorg Med Chem Lett. 2015;25:4580-6 pubmed publisher
    ..Further, measurement of mitochondrial membrane potential and Annexin V-FITC assay also suggested that 6b and 6u induced cell death by apoptosis. ..
  22. Kamal A, Tekumalla V, Raju P, Naidu V, Diwan P, Sistla R. Pyrrolo[2,1-c][1,4]benzodiazepine-beta-glucuronide prodrugs with a potential for selective therapy of solid tumors by PMT and ADEPT strategies. Bioorg Med Chem Lett. 2008;18:3769-73 pubmed publisher
    ..Enhanced water solubility and improved stability are the other important outcomes upon modifying these molecules as their prodrugs. ..
  23. Kamal A, Reddy V, Shaik A, Kumar G, Vishnuvardhan M, Polepalli S, et al. Synthesis of (Z)-(arylamino)-pyrazolyl/isoxazolyl-2-propenones as tubulin targeting anticancer agents and apoptotic inducers. Org Biomol Chem. 2015;13:3416-31 pubmed publisher
    ..These investigations reveal that such conjugates containing pyrazole with a trimethoxy phenyl ring and indole moieties have potential for the development of newer chemotherapeutic agents. ..
  24. Kamal A, Bharathi E, Reddy J, Ramaiah M, Dastagiri D, Reddy M, et al. Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents. Eur J Med Chem. 2011;46:691-703 pubmed publisher
    ..Further some detailed biological assays relating to the cell cycle aspects and tubulin depolymerization activity have been examined with a view to understand the mechanism of action of this conjugate. ..
  25. request reprint
    Kamal A, Khan M, Reddy K, Ahmed S, Kumar M, Juvekar A, et al. 1,2,4-benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity. Bioorg Med Chem Lett. 2007;17:5345-8 pubmed
    ..Their DNA thermal denaturation studies have been carried out and one of the compounds (4b) elevates the DNA helix melting temperature of the CT-DNA by 6.7 degrees C after incubation for 36 h. ..
  26. Kamal A, Rajender -, Reddy D, Reddy M, Balakishan G, Shaik T, et al. Remarkable enhancement in the DNA-binding ability of C2-fluoro substituted pyrrolo[2,1-c][1,4]benzodiazepines and their anticancer potential. Bioorg Med Chem. 2009;17:1557-72 pubmed publisher
    ..Some representative C2-fluoro substituted dimers (8a and 14a) have also exhibited significant anticancer activity in the 60 cancer cell line assay of the National Cancer Institute (NCI). ..
  27. Kamal A, Tangella Y, Manasa K, Sathish M, Srinivasulu V, Chetna J, et al. PhI(OAc)2-mediated one-pot oxidative decarboxylation and aromatization of tetrahydro-β-carbolines: synthesis of norharmane, harmane, eudistomin U and eudistomin I. Org Biomol Chem. 2015;13:8652-62 pubmed publisher
    ..The utility of this protocol has been demonstrated in the synthesis of β-carboline alkaloids norharmane (2o), harmane (2p), eudistomin U (9) and eudistomin I (12). ..
  28. Shankaraiah N, Kumar N, Amula S, Nekkanti S, Jeengar M, Naidu V, et al. One-pot synthesis of podophyllotoxin-thiourea congeners by employing NH₂SO₃H/NaI: Anticancer activity, DNA topoisomerase-II inhibition, and apoptosis inducing agents. Bioorg Med Chem Lett. 2015;25:4239-44 pubmed publisher
    ..Molecular docking results of the title compounds with topoisomerase-IIα were presented as theoretical support for the experimental data. ..
  29. Kamal A, Shaik A, Rao B, Khan I, Bharath Kumar G, Jain N. Design and synthesis of pyrazole/isoxazole linked arylcinnamides as tubulin polymerization inhibitors and potential antiproliferative agents. Org Biomol Chem. 2015;13:10162-78 pubmed publisher
  30. Kamal A, Srikanth Y, Ramaiah M, Khan M, Kashi Reddy M, Ashraf M, et al. Synthesis, anticancer activity and apoptosis inducing ability of bisindole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates. Bioorg Med Chem Lett. 2012;22:571-8 pubmed publisher
    ..The apoptotic nature of these compounds was further evidenced by increased expression of cleaved-PARP and active caspase-7 in MCF-7 cells. ..
  31. Kamal A, Shaik A, Jain N, Kishor C, Nagabhushana A, Supriya B, et al. Design and synthesis of pyrazole-oxindole conjugates targeting tubulin polymerization as new anticancer agents. Eur J Med Chem. 2015;92:501-13 pubmed publisher
    ..Zebrafish screening revealed that 12b, and 12d caused developmental defects. Docking analysis demonstrated that the congeners occupy the colchicine binding pocket of tubulin. ..
  32. request reprint
    Kamal A, Hussaini S, Malik M. Recent developments towards podophyllotoxin congeners as potential apoptosis inducers. Anticancer Agents Med Chem. 2015;15:565-74 pubmed
    ..Therefore the present review focuses on the studies carried out in the design and synthesis of new podophyllotoxin derivatives and their evaluation as apoptosis inducers. ..
  33. Reddy T, Kulhari H, Reddy V, Bansal V, Kamal A, Shukla R. Design, synthesis and biological evaluation of 1,3-diphenyl-1H-pyrazole derivatives containing benzimidazole skeleton as potential anticancer and apoptosis inducing agents. Eur J Med Chem. 2015;101:790-805 pubmed publisher
    ..The ease of synthesis and the remarkable biological activities make these compounds promising new frameworks for the development of cancer therapeutics. ..
  34. Kamal A, Sathish M, Nayak V, Srinivasulu V, Kavitha B, Tangella Y, et al. Design and synthesis of dithiocarbamate linked β-carboline derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability. Bioorg Med Chem. 2015;23:5511-26 pubmed publisher
    ..Overall, the present study emphasizes the importance of linking a dithiocarbamate moiety to the β-carboline scaffold for exhibiting profound activity. ..
  35. Kumar N, Thatikonda S, Tokala R, Kumari S, Lakshmi U, Godugu C, et al. Sulfamic acid promoted one-pot synthesis of phenanthrene fused-dihydrodibenzo-quinolinones: Anticancer activity, tubulin polymerization inhibition and apoptosis inducing studies. Bioorg Med Chem. 2018;26:1996-2008 pubmed publisher
    ..Analysis of mitochondrial membrane potential through JC-1 staining and annexin V binding assay indicated the extent of apoptosis in A549 cancer cells. ..
  36. Kamal A, Mahesh R, Nayak V, Babu K, Kumar G, Shaik A, et al. Discovery of pyrrolospirooxindole derivatives as novel cyclin dependent kinase 4 (CDK4) inhibitors by catalyst-free, green approach. Eur J Med Chem. 2016;108:476-485 pubmed publisher
    ..Furthermore, it was observed that there is an increase in expression levels of cyclin dependent kinase inhibitors like Cip1/p21 and Kip1/p27. ..
  37. Kamal A, Ashraf M, Basha S, Ali Hussaini S, Singh S, Vishnuvardhan M, et al. Design, synthesis and antiproliferative activity of the new conjugates of E7010 and resveratrol as tubulin polymerization inhibitors. Org Biomol Chem. 2016;14:1382-94 pubmed publisher
    ..Structure based studies, western blotting and immunofluorescence experiments demonstrated that RSV-1 and RSV-11 depolymerize microtubules in the HepG2 cell line, resulting in an accumulation of G2/M cells. ..
  38. request reprint
    Kamal A, Azeeza S, Malik M, Shaik A, Rao M. Efforts towards the development of new antitubercular agents: potential for thiolactomycin based compounds. J Pharm Pharm Sci. 2008;11:56s-80s pubmed
    ..We have also attempted to highlight the efforts that are being made in the development of new molecules based on thiolactomycin as lead compound, including studies from this laboratory. ..
  39. Kamal A, Shaik A, Polepalli S, Kumar G, Reddy V, Mahesh R, et al. Synthesis of arylpyrazole linked benzimidazole conjugates as potential microtubule disruptors. Bioorg Med Chem. 2015;23:1082-95 pubmed publisher
    ..These investigations reveal that such conjugates having pyrazole and benzimidazole moieties have the potential in the development of newer chemotherapeutic agents. ..
  40. Kamal A, Reddy M, Ramaiah M, Rajender -, Reddy J, Srikanth Y, et al. Synthesis and biological evaluation of estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates as potential anticancer agents. Bioorg Med Chem. 2011;19:2565-81 pubmed publisher
    ..Among all these conjugates, one of the compound 5c could be considered as the most effective compound particularly against MCF-7 breast cancer cell line. ..
  41. Kamal A, Reddy B, Sridevi B, Ravikumar A, Venkateswarlu A, Sravanthi G, et al. Synthesis and biological evaluation of phaitanthrin congeners as anti-mycobacterial agents. Bioorg Med Chem Lett. 2015;25:3867-72 pubmed publisher
    ..Phaitanthrin derivatives are prepared by modifying the keto functionality of tryptanthrin. These phaitanthrin congeners are found to display promising anti-tubercular activity. ..
  42. Shankaraiah N, Siraj K, Nekkanti S, Srinivasulu V, Sharma P, Senwar K, et al. DNA-binding affinity and anticancer activity of β-carboline-chalcone conjugates as potential DNA intercalators: Molecular modelling and synthesis. Bioorg Chem. 2015;59:130-9 pubmed publisher
  43. Kamal A, Syed M, Mohammed S. Therapeutic potential of benzothiazoles: a patent review (2010 - 2014). Expert Opin Ther Pat. 2015;25:335-49 pubmed publisher
    ..Its structural simplicity and ease of synthesis provides scope for the development of chemical libraries that could serve in the discovery of new chemical entities progressing towards the market. ..
  44. Kumar N, Sharma P, Reddy T, Shankaraiah N, Bhargava S, Kamal A. Microwave-assisted one-pot synthesis of new phenanthrene fused-tetrahydrodibenzo-acridinones as potential cytotoxic and apoptosis inducing agents. Eur J Med Chem. 2018;151:173-185 pubmed publisher
    ..The increase of caspase-3 activation by 3.7 folds supported the strong apoptosis induction. In addition, an in vitro 3D-spheroid progression assay was performed with 8m that significantly suppressed the tumor cells. ..
  45. Kamal A, Nayak V, Bagul C, Vishnuvardhan M, Mallareddy A. Investigation of the mechanism and apoptotic pathway induced by 4β cinnamido linked podophyllotoxins against human lung cancer cells A549. Apoptosis. 2015;20:1518-29 pubmed publisher
    ..Moreover, these compounds did not significantly inhibit the noncancerous human embryonic kidney cells, HEK-293. ..
  46. Kamal A, Nagaseshadri B, Nayak V, Srinivasulu V, Sathish M, Kapure J, et al. Synthesis and biological evaluation of benzimidazole-oxindole conjugates as microtubule-targeting agents. Bioorg Chem. 2015;63:72-84 pubmed publisher
    ..By and large, the results demonstrated that these benzimidazole-oxindole conjugates possess cytotoxic property by inhibiting the tubulin polymerization. ..
  47. Kamal A, Hussaini S, Sucharitha M, Poornachandra Y, Sultana F, Ganesh Kumar C. Synthesis and antimicrobial potential of nitrofuran-triazole congeners. Org Biomol Chem. 2015;13:9388-97 pubmed publisher
    ..Most of these compounds exhibited ten times lower cytotoxicity toward the normal cells compared to the antimicrobial activity. ..
  48. Kamal A, Bajee S, Lakshma Nayak V, Venkata Subba Rao A, Nagaraju B, Ratna Reddy C, et al. Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents. Bioorg Med Chem Lett. 2016;26:2957-2964 pubmed publisher
    ..Docking studies revealed that these conjugates interact and bind at the colchicine binding site of the tubulin. ..
  49. Srikanth P, Nayak V, Suresh Babu K, Kumar G, Ravikumar A, Kamal A. 2-Anilino-3-Aroylquinolines as Potent Tubulin Polymerization Inhibitors. ChemMedChem. 2016;11:2050-62 pubmed publisher
    ..Molecular docking studies revealed that these compounds bind efficiently to β-tubulin at the colchicine binding site. ..
  50. Ashraf M, Shaik T, Malik M, Syed R, Mallipeddi P, Vardhan M, et al. Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability. Bioorg Med Chem Lett. 2016;26:4527-4535 pubmed publisher
    ..The molecular docking studies suggested that the binding of these mimics at the colchicine site of the tubulin is similar to that of combretastatin A-4. ..
  51. Reddy V, Bonam S, Reddy T, Akunuri R, Naidu V, Nayak V, et al. 4β-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer. Eur J Med Chem. 2018;144:595-611 pubmed publisher
    ..Further apoptotic studies were also performed on these DU-145 cells, which showed that this class of compounds could induce apoptosis effectively. ..
  52. Shankaraiah N, Jadala C, Nekkanti S, Senwar K, Nagesh N, Shrivastava S, et al. Design and synthesis of C3-tethered 1,2,3-triazolo-β-carboline derivatives: Anticancer activity, DNA-binding ability, viscosity and molecular modeling studies. Bioorg Chem. 2016;64:42-50 pubmed publisher
    ..Viscosity measurements and molecular docking studies substantiate that these compounds indeed bind to DNA via the minor groove. ..
  53. Kamal A, Ramakrishna G, Raju P, Viswanath A, Ramaiah M, Balakishan G, et al. Synthesis and anti-cancer activity of chalcone linked imidazolones. Bioorg Med Chem Lett. 2010;20:4865-9 pubmed publisher
    ..Surprisingly, the increased concentration of the same compound to 30 microM caused accumulation of cells in G0/G1 phase of the cell cycle. ..
  54. Kamal A, Dastagiri D, Ramaiah M, Bharathi E, Reddy J, Balakishan G, et al. Synthesis, anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole-pyrrolobenzodiazepine conjugates. Bioorg Med Chem. 2010;18:6666-77 pubmed publisher
    ..Some detailed biological assays relating to the cell cycle aspects associated to Bax and caspases have been examined with a view to understand the mechanism of action of these conjugates. ..
  55. Kamal A, Prabhakar S, Janaki Ramaiah M, Venkat Reddy P, Ratna Reddy C, Mallareddy A, et al. Synthesis and anticancer activity of chalcone-pyrrolobenzodiazepine conjugates linked via 1,2,3-triazole ring side-armed with alkane spacers. Eur J Med Chem. 2011;46:3820-31 pubmed publisher
    ..These findings suggest that one of the compound 4d among this series is most effective and has potential for detailed investigations. ..
  56. Kamal A, Reddy M, Ramaiah M, Srikanth Y, Rajender -, Reddy V, et al. Synthesis of aryl-substituted naphthalene-linked pyrrolobenzodiazepine conjugates as potential anticancer agents with apoptosis-inducing ability. ChemMedChem. 2011;6:1665-79 pubmed publisher
    ..One conjugate in particular is the most promising candidate of the series, with the potential to be selected for further studies, either alone or in combination with existing anticancer therapies. ..
  57. Ganga Reddy V, Srinivasa Reddy T, Lakshma Nayak V, Prasad B, Reddy A, Ravikumar A, et al. Design, synthesis and biological evaluation of N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)-1,3-diphenyl-1H-pyrazole-4-carboxamides as CDK1/Cdc2 inhibitors. Eur J Med Chem. 2016;122:164-177 pubmed publisher
    ..Based on these studies, two compounds 16 and 27 have been identified as promising new molecules that have the potential to be developed as leads. ..
  58. Nayak V, Nagesh N, Ravikumar A, Bagul C, Vishnuvardhan M, Srinivasulu V, et al. 2-aryl benzimidazole conjugate induced apoptosis in human breast cancer MCF-7 cells through caspase independent pathway. Apoptosis. 2017;22:118-134 pubmed publisher
    ..Most importantly, this compound was less toxic towards non-tumorigenic breast epithelial cells, MCF-10A. Furthermore, docking studies also support the potentiality of this molecule to bind to the DNA topoisomerase II. ..
  59. Kamal A, Hussaini S, Faazil S, Poornachandra Y, Narender Reddy G, Kumar C, et al. Anti-tubercular agents. Part 8: synthesis, antibacterial and antitubercular activity of 5-nitrofuran based 1,2,3-triazoles. Bioorg Med Chem Lett. 2013;23:6842-6 pubmed publisher
    ..Compound 8e showed promising antitubercular activity with MIC value of 0.25 ?g/ml. Most of these compounds are less toxic to normal mammalian cells than the widely used antibacterial drug Ciprofloxacin. ..
  60. Kamal A, Balakishan G, Ramakrishna G, Shaik T, Sreekanth K, Balakrishna M, et al. Synthesis and biological evaluation of cinnamido linked pyrrolo[2,1-c][1,4]benzodiazepines as antimitotic agents. Eur J Med Chem. 2010;45:3870-84 pubmed publisher
    ..Interestingly, compounds 5b and 6b have been identified as a new class of inhibitors of tubulin polymerization and their action has been rationalized by the cell cycle arrest in G0 and G2/M phase. ..
  61. Lakshma Nayak V, Nagaseshadri B, Vishnuvardhan M, Kamal A. Investigation of the apoptotic pathway induced by benzimidazole-oxindole conjugates against human breast cancer cells MCF-7. Bioorg Med Chem Lett. 2016;26:3313-3317 pubmed publisher
    ..It was further confirmed by western blot analysis of pro apoptotic protein Bax, anti apoptotic protein Bcl-2, cytochrome c release, caspase-9 activity and cleavage of PARP. ..
  62. Baig M, Nayak V, Budaganaboyina P, Mullagiri K, Sunkari S, Gour J, et al. Synthesis and biological evaluation of imidazo[2,1-b]thiazole-benzimidazole conjugates as microtubule-targeting agents. Bioorg Chem. 2018;77:515-526 pubmed publisher
    ..Further, molecular docking studies revealed that compound 6d occupied the colchicine binding site. ..
  63. Donthiboina K, Namballa H, Shaik S, Nanubolu J, Shankaraiah N, Kamal A. Iodine promoted dual oxidative C(sp3)-H amination of 2-methyl-3-arylquinazolin-4(3H)-ones: a facile route to 1,4-diarylimidazo[1,5-a]quinazolin-5(4H)-ones. Org Biomol Chem. 2018;16:1720-1727 pubmed publisher
    ..This tandem transformation provides an efficient approach to construct various functionalized imidazo[1,5-a]quinazolin-5(4H)-ones in a straightforward manner via a sequential amination-oxidation-annulation-aromatisation. ..
  64. Sri Ramya P, Guntuku L, Angapelly S, Karri S, Digwal C, Babu B, et al. Curcumin inspired 2-chloro/phenoxy quinoline analogues: Synthesis and biological evaluation as potential anticancer agents. Bioorg Med Chem Lett. 2018;28:892-898 pubmed publisher
    ..Additionally, the promising candidate 6c could induce G2/M cell cycle arrest and apoptosis in PC-3 cells, as determined by AO-EB staining, DAPI staining, analysis of ROS levels as well as annexin binding assay. ..
  65. Kumar N, Sharma P, Reddy T, Nekkanti S, Shankaraiah N, Lalita G, et al. Synthesis of 2,3,6,7-tetramethoxyphenanthren-9-amine: An efficient precursor to access new 4-aza-2,3-dihydropyridophenanthrenes as apoptosis inducing agents. Eur J Med Chem. 2017;127:305-317 pubmed publisher
    ..Moreover, its treatment leads to collapse of the mitochondrial membrane potential (D?m). ..
  66. Kamal A, Srikanth P, Vishnuvardhan M, Kumar G, Suresh Babu K, Hussaini S, et al. Combretastatin linked 1,3,4-oxadiazole conjugates as a Potent Tubulin Polymerization inhibitors. Bioorg Chem. 2016;65:126-36 pubmed publisher
    ..Further, DNA fragmentation and Hoecst staining assays confirm that 5m induces apoptosis. Molecular docking studies and competitive binding assay indicated that 5m effectively bind at the colchicine binding site of the tubulin. ..
  67. Kamal A, Faazil S, Hussaini S, Ramaiah M, Balakrishna M, Patel N, et al. Synthesis and mechanistic aspects of 2-anilinonicotinyl-pyrazolo[1,5-a]pyrimidine conjugates that regulate cell proliferation in MCF-7 cells via estrogen signaling. Bioorg Med Chem Lett. 2016;26:2077-83 pubmed publisher
    ..Moreover, ER alpha protein expression was studied to understand regulatory role of these conjugates on estrogen activity in estrogen positive breast cancer cells like MCF-7 and compounds 6a and 6c reduced their activity. ..
  68. Kumar G, Nayak V, Sayeed I, Reddy V, Shaik A, Mahesh R, et al. Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents. Bioorg Med Chem. 2016;24:1729-40 pubmed publisher
    ..23 μM and 1.01 μM, respectively. Molecular docking studies indicated that these compounds (5c and 5d) occupy the colchicine binding site of the tubulin. ..
  69. Saraswati A, Ali Hussaini S, Krishna N, Babu B, Kamal A. Glycogen synthase kinase-3 and its inhibitors: Potential target for various therapeutic conditions. Eur J Med Chem. 2018;144:843-858 pubmed publisher
    ..The present review focuses on the recent developments in the area of GSK-3 inhibitors and also enlightens its therapeutic applicability in various disease conditions. ..
  70. Shaik S, Nayak V, Sultana F, Rao A, Shaik A, Babu K, et al. Design and synthesis of imidazo[2,1-b]thiazole linked triazole conjugates: Microtubule-destabilizing agents. Eur J Med Chem. 2017;126:36-51 pubmed publisher
  71. Sathish M, Kavitha B, Nayak V, Tangella Y, Ajitha A, Nekkanti S, et al. Synthesis of podophyllotoxin linked β-carboline congeners as potential anticancer agents and DNA topoisomerase II inhibitors. Eur J Med Chem. 2018;144:557-571 pubmed publisher
    ..Further, detailed biological studies such as cell cycle analysis, topoisomerase II inhibition, Comet assay, DNA binding studies and docking studies have revealed that these congeners are DNA interacting topoisomerase II inhibitors. ..
  72. Sri Ramya P, Angapelly S, Guntuku L, Singh Digwal C, Nagendra Babu B, Naidu V, et al. Synthesis and biological evaluation of curcumin inspired indole analogues as tubulin polymerization inhibitors. Eur J Med Chem. 2017;127:100-114 pubmed publisher
    ..Additionally, the treatment by these compounds led to the impairment of mitochondrial membrane potential (D?m) in PC-3 cells. ..
  73. Narasimha Rao M, Nagaraju B, Kovvuri J, Polepalli S, Alavala S, Vishnuvardhan M, et al. Synthesis of imidazo-thiadiazole linked indolinone conjugates and evaluated their microtubule network disrupting and apoptosis inducing ability. Bioorg Chem. 2018;76:420-436 pubmed publisher
    ..Docking studies revealed that these compounds (7, 14 and 15) bind with αAsn101, αThr179, αSer178, βCys241, βLys254 and βLys352 in the colchicine-binding site of the tubulin. ..
  74. Khan I, Garikapati K, Shaik A, Makani V, Rahim A, Shareef M, et al. Design, synthesis and biological evaluation of 1, 4-dihydro indeno[1,2-c] pyrazole linked oxindole analogues as potential anticancer agents targeting tubulin and inducing p53 dependent apoptosis. Eur J Med Chem. 2018;144:104-115 pubmed publisher
    ..33 μM showed significant upregulation of tumor suppressor proteins like p53, p21 and pro-apoptotic Bax. The molecular docking analysis demonstrated that these congeners occupy the colchicine binding pocket of the tubulin. ..
  75. Srinivasa Reddy T, Ganga Reddy V, Kulhari H, Shukla R, Kamal A, Bansal V. Synthesis of (Z)-1-(1,3-diphenyl-1H-pyrazol-4-yl)-3-(phenylamino)prop-2-en-1-one derivatives as potential anticancer and apoptosis inducing agents. Eur J Med Chem. 2016;117:157-66 pubmed publisher
  76. Kamal A, Suresh P, Ramaiah M, Mallareddy A, Imthiajali S, Pushpavalli S, et al. Synthesis and biological evaluation of 4?-sulphonamido and 4?-[(4'-sulphonamido)benzamide]podophyllotoxins as DNA topoisomerase-II? and apoptosis inducing agents. Bioorg Med Chem. 2012;20:2054-66 pubmed publisher
    ..Moreover activation of caspase-3, p21, p16, NF-kB and down regulation of Bcl-2 protein suggests that this compound (11e) has apoptotic cell death inducing ability, apart from acting as a topo-II? inhibitor. ..
  77. request reprint
    Kamal A, Shaik A, Kumar C, Mongolla P, Rani P, Krishna K, et al. Metabolic profiling and biological activities of bioactive compounds produced by Pseudomonas sp. strain ICTB-745 isolated from Ladakh, India. J Microbiol Biotechnol. 2012;22:69-79 pubmed
    ..The metabolites from Pseudomonas sp. strain ICTB-745 have interesting potential for use as a biopesticide in pest control programs. ..
  78. Dutta S, Shaik A, Ganesh Kumar C, Kamal A. Statistical optimization of production conditions of ?-glucosidase from Bacillus stratosphericus strain SG9. 3 Biotech. 2017;7:221 pubmed publisher
    ..The bacterial strain was identified by 16S rRNA gene sequence and biochemical characterization. The strain was identified as Bacillus stratosphericus and is a first report of its kind. ..
  79. Kamal A, Lakshma Nayak V, Nagesh N, Vishnuvardhan M, Subba Reddy N. Benzo[b]furan derivatives induces apoptosis by targeting the PI3K/Akt/mTOR signaling pathway in human breast cancer cells. Bioorg Chem. 2016;66:124-31 pubmed publisher
    ..Western blot analysis revealed that these compounds inhibit the PI3K/Akt/mTOR signaling pathway and induced mitochondrial mediated apoptosis in human breast cancer cells (MCF-7). ..
  80. Shaik T, Hussaini S, Nayak V, Sucharitha M, Malik M, Kamal A. Rational design and synthesis of 2-anilinopyridinyl-benzothiazole Schiff bases as antimitotic agents. Bioorg Med Chem Lett. 2017;27:2549-2558 pubmed publisher
    ..Furthermore, 4y induced apoptosis as evidenced by biological studies like mitochondrial membrane potential, caspase-3, and Annexin V-FITC assays. ..
  81. Shaik S, Vishnuvardhan M, Sultana F, Subba Rao A, Bagul C, Bhattacharjee D, et al. Design and synthesis of 1,2,3-triazolo linked benzo[d]imidazo[2,1-b]thiazole conjugates as tubulin polymerization inhibitors. Bioorg Med Chem. 2017;25:3285-3297 pubmed publisher
    ..Molecular docking studies indicated that these conjugates occupy the colchicine binding site of the tubulin protein. ..
  82. Mani G, Shaik S, Tangella Y, Bale S, Godugu C, Kamal A. A facile I2-catalyzed synthesis of imidazo[1,2-a]pyridines via sp3 C-H functionalization of azaarenes and evaluation of anticancer activity. Org Biomol Chem. 2017;15:6780-6791 pubmed publisher
    ..The synthesized compounds were screened for their anti-cancer activity in selected human cancer cell lines. Compounds 4a, 4b, 4c, 4i, 7a, 7b and 7m have significant IC50 values ranging from 4.88 ± 0.28 to 14.55 ± 0.74 ?M. ..
  83. Subba Rao A, Vishnu Vardhan M, Subba Reddy N, Srinivasa Reddy T, Shaik S, Bagul C, et al. Synthesis and biological evaluation of imidazopyridinyl-1,3,4-oxadiazole conjugates as apoptosis inducers and topoisomerase II? inhibitors. Bioorg Chem. 2016;69:7-19 pubmed publisher
    ..Topo II mediated DNA relaxation assay results showed that conjugate 8q could significantly inhibit the activity of topo II. Moreover, molecular docking studies also indicated binding to the topoisomerase enzyme (PDBID 1ZXN). ..
  84. Tangella Y, Manasa K, Laxma Nayak V, Sathish M, Sridhar B, Alarifi A, et al. An efficient one-pot approach for the regio- and diastereoselective synthesis of trans-dihydrofuran derivatives: cytotoxicity and DNA-binding studies. Org Biomol Chem. 2017;15:6837-6853 pubmed publisher
    ..In addition, compounds 1g and 1r showed significant topoisomerase II inhibitory activities. Moreover, an in silico study of these synthesized compounds revealed that they possess drug-like properties. ..
  85. Baig M, Shaik S, Nayak V, Alarifi A, Kamal A. Iodine-catalyzed Csp3-H functionalization of methylhetarenes: One-pot synthesis and cytotoxic evaluation of heteroarenyl-benzimidazoles and benzothiazole. Bioorg Med Chem Lett. 2017;27:4039-4043 pubmed publisher
    ..Among them 3h, 3q and 5b showed significant cytotoxic activities with an IC50 of 1.69, 1.62 and 2.81µM respectively against lung cancer (A549) cell line. ..
  86. Shaik A, Rao G, Kumar G, Patel N, Reddy V, Khan I, et al. Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells. Eur J Med Chem. 2017;139:305-324 pubmed publisher
    ..Our study indicates that pyrazolochalcone conjugates could serve as potential leads in the development of tailored cancer therapeutics. ..
  87. Shaik S, Sultana F, Ravikumar A, Sunkari S, Alarifi A, Kamal A. Regioselective oxidative cross-coupling of benzo[d]imidazo[2,1-b]thiazoles with styrenes: a novel route to C3-dicarbonylation. Org Biomol Chem. 2017;15:7696-7704 pubmed publisher
    ..This method offers the advantages of broad substrate scope, ecofriendly feature and high atom economy apart from higher yields. ..
  88. Kumar N, Sharma P, Kumari S, Brahma U, Nekkanti S, Shankaraiah N, et al. Synthesis of substituted phenanthrene-9-benzimidazole conjugates: Cytotoxicity evaluation and apoptosis inducing studies. Eur J Med Chem. 2017;140:128-140 pubmed publisher
    ..JC-1 staining and annexin binding assays indicated the extent of apoptosis in PC-3 cells. Further, relative viscosity measurements and molecular docking studies indicated that these compounds bind to DNA by intercalation. ..
  89. Kovvuri J, Nagaraju B, Nayak V, Akunuri R, Rao M, Ajitha A, et al. Design, synthesis and biological evaluation of new ?-carboline-bisindole compounds as DNA binding, photocleavage agents and topoisomerase I inhibitors. Eur J Med Chem. 2018;143:1563-1577 pubmed publisher
  90. Ramya P, Guntuku L, Angapelly S, Digwal C, Lakshmi U, Sigalapalli D, et al. Synthesis and biological evaluation of curcumin inspired imidazo[1,2-a]pyridine analogues as tubulin polymerization inhibitors. Eur J Med Chem. 2018;143:216-231 pubmed publisher
  91. Adiyala P, Tekumalla V, Sayeed I, Nayak V, Nagarajan A, Shareef M, et al. Development of pyrrolo[2,1-c][1,4]benzodiazepine β-glucoside prodrugs for selective therapy of cancer. Bioorg Chem. 2018;76:288-293 pubmed publisher
    ..Another important property of these molecules is their enhanced water solubility and stability, which are essential for a molecule to be an effective drug. ..