Om Silakari

Summary

Publications

  1. Singh P, Choudhary S, Kashyap A, Verma H, Kapil S, Kumar M, et al. An exhaustive compilation on chemistry of triazolopyrimidine: A journey through decades. Bioorg Chem. 2019;88:102919 pubmed publisher
  2. Kumar Singh P, Kashyap A, Silakari O. Exploration of the therapeutic aspects of Lck: A kinase target in inflammatory mediated pathological conditions. Biomed Pharmacother. 2018;108:1565-1571 pubmed publisher
    ..This article provides evidence and information establishing Lck as one of the therapeutic targets in various inflammation mediated pathophysiological conditions. ..
  3. Kashyap A, Singh P, Silakari O. In silico designing of domain B selective gyrase inhibitors for effective treatment of resistant tuberculosis. Tuberculosis (Edinb). 2018;112:83-88 pubmed publisher
    ..tuberculosis H37Rv strain. Two compounds exhibited significant anti-TB activity, whereas other three compounds were found to be outliers of the in silico study. ..
  4. Kapil S, Singh P, Silakari O. An update on small molecule strategies targeting leishmaniasis. Eur J Med Chem. 2018;157:339-367 pubmed publisher
    ..This review provides an overview of leishmaniasis along with the main emphasis on novel heterocycles reported for their anti-leishmanial activity in recent years. ..
  5. Singh P, Silakari O. Molecular dynamics guided development of indole based dual inhibitors of EGFR (T790M) and c-MET. Bioorg Chem. 2018;79:163-170 pubmed publisher
    ..101 µM. Overall, this work is one of the earliest report of compounds having significant dual inhibitory potential against secondary acquired EGFR and cMET, with IC50 values in nanomolar range. ..
  6. Chadha N, Bahia M, Kaur M, Silakari O. Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions. Bioorg Med Chem. 2015;23:2953-74 pubmed publisher
    ..The structure based SAR of TZD derivatives for various protein targets would serve as a benchmark for the alteration of existing ligands to design new ones with better binding interactions. ..
  7. Kaur G, Silakari O. Benzimidazole scaffold based hybrid molecules for various inflammatory targets: Synthesis and evaluation. Bioorg Chem. 2018;80:24-35 pubmed publisher
    ..Additionally, compound 3j showed gastrointestinal safety with reduced lipid peroxidation. Docking results of compound 3j with COX-2 and 5-LOX were also consistent with the in vivo anti-inflammatory results. ..
  8. Choudhary S, Singh P, Verma H, Singh H, Silakari O. Success stories of natural product-based hybrid molecules for multi-factorial diseases. Eur J Med Chem. 2018;151:62-97 pubmed publisher
    ..This review strives to encompass all natural product-derived hybrid molecules which act as multi-targeting agents striking various targets involved in different pathways of complex diseased conditions reported in literature. ..
  9. Chadha N, Silakari O. Active site fingerprinting and pharmacophore screening strategies for the identification of dual inhibitors of protein kinase C (ΡΚCβ) and poly (ADP-ribose) polymerase-1 (PARP-1). Mol Divers. 2016;20:747-61 pubmed publisher
    ..Thus, novel hits have been predicted to have good binding affinities for [Formula: see text] and PARP-1 proteins, which could be further investigated for in vitro/in vivo activity. ..

More Information

Publications21

  1. Kaur M, Singh M, Chadha N, Silakari O. Oxindole: A chemical prism carrying plethora of therapeutic benefits. Eur J Med Chem. 2016;123:858-894 pubmed publisher
    ..Thus, this review will provide insights for the synthetic as well as medicinal chemist for the designing and synthesis of novel oxindole derivatives with novel improved range of pharmacological implications. ..
  2. Singh P, Singh H, Silakari O. Kinases inhibitors in lung cancer: From benchside to bedside. Biochim Biophys Acta. 2016;1866:128-40 pubmed publisher
    ..It also explains the rationale of designing these along with possible interactions with their targets, biological data and possible problems associated with these inhibitors. ..
  3. Singh D, Silakari O. Facile alkylation of 4-nitrobenzotriazole and its platelet aggregation inhibitory activity. Bioorg Med Chem. 2017;25:5260-5267 pubmed publisher
    ..82±0.19mM] are also found to be highly active. Furthermore, all compounds possess P2Y12 binding affinity as confirmed by VASP/P2Y12 phosphorylation assay. ..
  4. Chadha N, Silakari O. Pharmacophore based design of some multi-targeted compounds targeted against pathways of diabetic complications. J Mol Graph Model. 2017;76:412-418 pubmed publisher
    ..These positive results support the progress of a low cost multi-targeted agent with putative roles in diabetic complications. ..
  5. Nalini -, Chadha N, Bahia M, Kaur M, Bahadur R, Silakari O. Computational design of new protein kinase D 1 (PKD1) inhibitors: homology-based active site prediction, energy-optimized pharmacophore, docking and database screening. Mol Divers. 2018;22:47-56 pubmed publisher
    ..These newly retrieved hits were docked against our PKD1 protein model, and those displaying essential interactions are reported herein as new hits, which could serve as new leads for cancer research, especially pancreatic cancer. ..
  6. Singh M, Kaur M, Singh N, Silakari O. Exploration of multi-target potential of chromen-4-one based compounds in Alzheimer's disease: Design, synthesis and biological evaluations. Bioorg Med Chem. 2017;25:6273-6285 pubmed publisher
    ..12?nM). It (7m) also ameliorated scopolamine induced memory deficit in mice employing Morris water maze test. Thus, flavonoids might be the promising lead compounds as potential polyfunctional anti-Alzheimer's agents. ..
  7. Kaur M, Singh P, Singh M, Bahadur R, Silakari O. Molecular dynamics and integrated pharmacophore-based identification of dual [Formula: see text] inhibitors. Mol Divers. 2018;22:95-112 pubmed publisher
    ..The top two hit compounds with novel scaffolds 2-oxo-1,2-dihydroquinoline and benzo[d]oxazole showed inhibitory activity for JAK3 and [Formula: see text]. ..
  8. Singh P, Silakari O. Chemotherapeutics-resistance "arms" race: An update on mechanisms involved in resistance limiting EGFR inhibitors in lung cancer. Life Sci. 2017;186:25-32 pubmed publisher
    ..Current approaches focussing on development of third generation inhibitors, dual inhibitors or inhibitors of HSP90 have shown significant activity but do not answer the long term question of resistance. ..
  9. Chadha N, Jaggi A, Silakari O. Structure-based design of new poly (ADP-ribose) polymerase (PARP-1) inhibitors. Mol Divers. 2017;21:655-660 pubmed publisher
    ..Thus, a structure-based design approach utilized in the present study helped to identify thiazolidine-2,4-dione as a novel scaffold against PARP-1 for potential development of potent anticancer therapeutics. ..
  10. Chadha N, Silakari O. Identification of low micromolar dual inhibitors for aldose reductase (ALR2) and poly (ADP-ribose) polymerase (PARP-1) using structure based design approach. Bioorg Med Chem Lett. 2017;27:2324-2330 pubmed publisher
    ..The positive results of the biochemical assay suggest that these compounds may be further optimized and utilized for the treatment of diabetic retinopathy. ..
  11. Chadha N, Silakari O. Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view. Eur J Med Chem. 2017;134:159-184 pubmed publisher
    ..This compiled information may serve as a benchmark for the alteration of existing ligands to design novel potent molecules with lesser side effects. ..
  12. Pathak D, Chadha N, Silakari O. Identification of non-resistant ROS-1 inhibitors using structure based pharmacophore analysis. J Mol Graph Model. 2016;70:85-93 pubmed publisher
    ..Thus, these identified hits show good binding affinities with WT and mutant ROS-1 proteins that may be further evaluated for their in-vitro/in-vivo activity. ..