Summary: Chemicals with two conjoined aromatic rings incorporating two nitrogen atoms and one of the carbons oxidized with a keto oxygen.

Top Publications

  1. Zhang X, Waibel M, Hasserodt J. An autoimmolative spacer allows first-time incorporation of a unique solid-state fluorophore into a detection probe for acyl hydrolases. Chemistry. 2010;16:792-5 pubmed publisher
  2. Sociali G, Magnone M, Ravera S, Damonte P, Vigliarolo T, Von Holtey M, et al. Pharmacological Sirt6 inhibition improves glucose tolerance in a type 2 diabetes mouse model. FASEB J. 2017;31:3138-3149 pubmed publisher
    ..G., Millo, E., Caffa, I., Cea, M., Parenti, M. D., Del Rio, A., Murone, M., Mostoslavsky, R., Grozio, A., Nencioni, A., Bruzzone S. Pharmacological Sirt6 inhibition improves glucose tolerance in a type 2 diabetes mouse model. ..
  3. El Sayed S, Metwally K, El Shanawani A, Abdel Aziz L, El Rashedy A, Soliman M, et al. Quinazolinone-based rhodanine-3-acetic acids as potent aldose reductase inhibitors: Synthesis, functional evaluation and molecular modeling study. Bioorg Med Chem Lett. 2017;27:4760-4764 pubmed publisher
    ..Docking and molecular dynamic simulations of the most active rhodanine-3-acetic acid derivatives were also carried out, to provide the basis for further structure-guided design of novel inhibitors. ..
  4. Fruman D, Cantley L. Idelalisib--a PI3K? inhibitor for B-cell cancers. N Engl J Med. 2014;370:1061-2 pubmed publisher
  5. Fan Y, Li W, Liu D, Bai M, Song H, Xu Y, et al. Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1,2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3K? inhibitors. Eur J Med Chem. 2017;139:95-106 pubmed publisher
    ..All these results suggested that 1i is a potent PI3K? inhibitor and could be considered as a potential candidate for the development of anticancer agents. ..
  6. Pham T, Walden M, Butler C, Díaz González R, Pérez Moreno G, Ceballos Pérez G, et al. Novel 1,2-dihydroquinazolin-2-ones: Design, synthesis, and biological evaluation against Trypanosoma brucei. Bioorg Med Chem Lett. 2017;27:3629-3635 pubmed publisher
    ..The SAR developed on 24 provides new directions for further optimization of this novel scaffold for anti-trypanosomal drug discovery. ..
  7. Park G, Chung Y, Jeong J, Kim D. A p110?-specific inhibitor combined with bortezomib blocks drug resistance properties of EBV-related B cell origin cancer cells via regulation of NF-?B. Int J Oncol. 2017;50:1711-1720 pubmed publisher
    ..Our results provide supportive evidence for the clinical application of CAL-101 and bortezomib to treat EBV-infected hematologic cancer. ..
  8. Prins R, Burke R, Tyner J, Druker B, Loriaux M, Spurgeon S. CX-4945, a selective inhibitor of casein kinase-2 (CK2), exhibits anti-tumor activity in hematologic malignancies including enhanced activity in chronic lymphocytic leukemia when combined with fludarabine and inhibitors of the B-cell receptor pathway. Leukemia. 2013;27:2094-6 pubmed publisher
  9. Bernlochner I, Sibbing D. Thienopyridines and other ADP-receptor antagonists. Handb Exp Pharmacol. 2012;:165-98 pubmed publisher
    ..Whether individualized antiplatelet treatment incorporating different P2Y12 receptor inhibitors improves patients' clinical outcomes warrants further investigation. ..

More Information


  1. Cao Y, Yang G, Hunter Z, Liu X, Xu L, Chen J, et al. The BCL2 antagonist ABT-199 triggers apoptosis, and augments ibrutinib and idelalisib mediated cytotoxicity in CXCR4 Wild-type and CXCR4 WHIM mutated Waldenstrom macroglobulinaemia cells. Br J Haematol. 2015;170:134-8 pubmed publisher
  2. El Azab A, Abdel Aziz A, Ghabbour H, Al Gendy M. Synthesis, in vitro antitumour activity, and molecular docking study of novel 2-substituted mercapto-3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinone analogues. J Enzyme Inhib Med Chem. 2017;32:1229-1239 pubmed publisher
    A novel series of 2-substituted mercapto-3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinones 1-20 was synthesised and evaluated for in vitro antitumour activity...
  3. Becerra A, Quintero C, Morales V, Valderrama M, Aguirre A, Faúndez M, et al. Synthesis of 4(3H)quinazolinimines with selective cytotoxic effect on human acute promyelocytic leukemia cells. Bioorg Med Chem. 2017;25:2681-2688 pubmed publisher
    ..The mechanism associated to cytotoxic effect was mainly apoptosis, which not was decreased by antioxidant addition, thereby suggesting that the compounds exert apoptotic death through a mechanism unrelated with oxidative stress. ..
  4. Haghighijoo Z, Firuzi O, Hemmateenejad B, Emami S, Edraki N, Miri R. Synthesis and biological evaluation of quinazolinone-based hydrazones with potential use in Alzheimer's disease. Bioorg Chem. 2017;74:126-133 pubmed publisher
    ..These results demonstrate that quinazolinone-hydrazone derivatives represent a valuable scaffold for the discovery of novel non-peptidic BACE1 inhibitors. ..
  5. Zhang G, Yuan J, Qian G, Gu C, Wei K, Mo D, et al. Phthalazino[1,2-b]quinazolinones as p53 Activators: Cell Cycle Arrest, Apoptotic Response and Bak-Bcl-xl Complex Reorganization in Bladder Cancer Cells. J Med Chem. 2017;60:6853-6866 pubmed publisher
    ..1 Herein the synthesized phthalazino[1,2-b]quinazolinones were discovered as p53 activators in bladder cancer cells...
  6. Rogers S, Hii H, Huang J, Ancliffe M, Gottardo N, Dallas P, et al. A novel technique of serial biopsy in mouse brain tumour models. PLoS ONE. 2017;12:e0175169 pubmed publisher
    ..This approach represents a significant advance in murine brain surgery that may be applicable to other brain tumour models. Importantly, the methodology has the potential to accelerate the preclinical in vivo drug screening process. ..
  7. Bordt E, Clerc P, Roelofs B, Saladino A, Tretter L, Adam Vizi V, et al. The Putative Drp1 Inhibitor mdivi-1 Is a Reversible Mitochondrial Complex I Inhibitor that Modulates Reactive Oxygen Species. Dev Cell. 2017;40:583-594.e6 pubmed publisher
    ..2 mM). Overall, these results suggest that mdivi-1 is not a specific Drp1 inhibitor. The ability of mdivi-1 to reversibly inhibit complex I and modify mitochondrial ROS production may contribute to effects observed in disease models. ..
  8. Ward A, Dong L, Harris J, Khanna K, Al Ejeh F, Fairlie D, et al. Quinazolinone derivatives as inhibitors of homologous recombinase RAD51. Bioorg Med Chem Lett. 2017;27:3096-3100 pubmed publisher
    ..Additionally, compound 17 significantly inhibits TNBC cell sensitivity to DNA damage, implying a potentially targeted therapy for cancer treatment. ..
  9. Tang Z, Cao W, Guo X, Dai X, Lu J, Chen X, et al. Identification of a novel autophagic inhibitor cepharanthine to enhance the anti-cancer property of dacomitinib in non-small cell lung cancer. Cancer Lett. 2018;412:1-9 pubmed publisher
    ..Collectively, CEP might be further developed as an autophagic inhibitor, and combined treatment of CEP and DAC could offer an effective strategy for NSCLC treatment. ..
  10. Sultana N, Sarfraz M, Tanoli S, Akram M, Sadiq A, Rashid U, et al. Synthesis, crystal structure determination, biological screening and docking studies of N1-substituted derivatives of 2,3-dihydroquinazolin-4(1H)-one as inhibitors of cholinesterases. Bioorg Chem. 2017;72:256-267 pubmed publisher
    ..Overall, the synthesized compounds have established a structural foundation for the design of new inhibitors of cholinesterase. ..
  11. Elger C, Hong S, Brandt C, Mancione L, Han J, Strohmaier C. BGG492 as an adjunctive treatment in patients with partial-onset seizures: A 12-week, randomized, double-blind, placebo-controlled, phase II dose-titration study with an open-label extension. Epilepsia. 2017;58:1217-1226 pubmed publisher
    ..Safety and tolerability data were consistent with the known safety profile for BGG492, and no new safety risks were identified. ..
  12. Zhou K, Shi L, Wang Z, Zhou J, Manaenko A, Reis C, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017;295:116-124 pubmed publisher
    ..The activation of the NLRP3 inflammasome in EBI after SAH was mediated by RIP1-RIP3-DRP1 pathway. Nec-1 and Mdivi-1 can inhibit inflammation and improve neurological function after SAH. ..
  13. Finkelstein D, Billings J, Adlard P, Ayton S, Sedjahtera A, Masters C, et al. The novel compound PBT434 prevents iron mediated neurodegeneration and alpha-synuclein toxicity in multiple models of Parkinson's disease. Acta Neuropathol Commun. 2017;5:53 pubmed publisher
    ..We conclude that compounds designed to target a pool of pathological iron that is not held in high-affinity complexes in the tissue can maintain the survival of SNpc neurons and could be disease-modifying in PD. ..
  14. Brown C, Kong T, McNulty J, D Aiuto L, Williamson K, McClain L, et al. Discovery of potent antiviral (HSV-1) quinazolinones and initial structure-activity relationship studies. Bioorg Med Chem Lett. 2017;27:4601-4605 pubmed publisher
    The discovery of antiviral activity of 2,3-disubstituted quinazolinones, prepared by a one-pot, three-component condensation of isatoic anhydride with amines and aldehydes, against Herpes Simplex Virus (HSV)-1 is reported...
  15. Kim J, Park S, Kim B, Choe Y, Lee D. Insulin-stimulated lipid accumulation is inhibited by ROS-scavenging chemicals, but not by the Drp1 inhibitor Mdivi-1. PLoS ONE. 2017;12:e0185764 pubmed publisher
    ..Therefore, our results indicated that ROS are an essential regulator of adipocyte differentiation in 3T3-L1 cells...
  16. Masson G, Maslen S, Williams R. Analysis of phosphoinositide 3-kinase inhibitors by bottom-up electron-transfer dissociation hydrogen/deuterium exchange mass spectrometry. Biochem J. 2017;474:1867-1877 pubmed publisher
    ..Owing to the relatively minor amounts of protein required, this technique may be utilised in pharmaceutical development for screening potential therapeutics. ..
  17. Pepper C, Buggins A, Jones C, Walsby E, Forconi F, Pratt G, et al. Phenotypic heterogeneity in IGHV-mutated CLL patients has prognostic impact and identifies a subset with increased sensitivity to BTK and PI3K? inhibition. Leukemia. 2015;29:744-7 pubmed publisher
  18. Bétrian S, Ysebaert L, Heider K, Delord J, Fournie J, Quillet Mary A. Idelalisib improves CD37 antibody BI 836826 cytotoxicity against chemo-resistant /relapse-initiating CLL cells: a rationale for combination treatment. Blood Cancer J. 2016;6:e496 pubmed publisher
  19. Morelli M, Calvo E, Ordoñez E, Wick M, Viqueira B, López Casas P, et al. Prioritizing phase I treatment options through preclinical testing on personalized tumorgraft. J Clin Oncol. 2012;30:e45-8 pubmed publisher
  20. Shustik C, Bence Bruckler I, Delage R, Owen C, Toze C, Coutre S. Advances in the treatment of relapsed/refractory chronic lymphocytic leukemia. Ann Hematol. 2017;96:1185-1196 pubmed publisher
    ..Allogeneic hematopoietic stem cell transplantation (HSCT) remains a potentially curative option for younger patients with a suitable donor. ..
  21. Burger J, Okkenhaug K. Haematological cancer: idelalisib-targeting PI3K? in patients with B-cell malignancies. Nat Rev Clin Oncol. 2014;11:184-6 pubmed publisher
  22. Lampson B, Brown J. PI3K?-selective and PI3K?/?-combinatorial inhibitors in clinical development for B-cell non-Hodgkin lymphoma. Expert Opin Investig Drugs. 2017;26:1267-1279 pubmed publisher
    ..Whether newer PI3K inhibitors will demonstrate differentiated toxicity profiles in comparable patient populations while retaining efficacy remains to be seen. ..
  23. Byrd J, Jones J, Woyach J, Johnson A, Flynn J. Entering the era of targeted therapy for chronic lymphocytic leukemia: impact on the practicing clinician. J Clin Oncol. 2014;32:3039-47 pubmed
    ..Therapy for CLL has evolved significantly over the past decade with introduction of targeted therapy for CLL. This has the potential to completely transform how CLL is treated in the future. ..
  24. Haustraete E, Obert J, Diab S, Abbes S, Zini J, Valade S, et al. Idelalisib-related pneumonitis. Eur Respir J. 2016;47:1280-3 pubmed publisher
  25. Wollenberg R, Saei W, Westphal K, Klitgaard C, Nielsen K, Lysøe E, et al. Chrysogine Biosynthesis Is Mediated by a Two-Module Nonribosomal Peptide Synthetase. J Nat Prod. 2017;80:2131-2135 pubmed publisher
    ..Overexpression of NRPS14 enhanced chrysogine production, suggesting that the NRPS is the bottleneck in the biosynthetic pathway. ..
  26. Compagno M, Wang Q, Pighi C, Cheong T, Meng F, Poggio T, et al. Phosphatidylinositol 3-kinase δ blockade increases genomic instability in B cells. Nature. 2017;542:489-493 pubmed publisher
    ..This effect should be carefully considered, as such inhibitors can be administered to patients for years. ..
  27. Jones J, Robak T, Brown J, Awan F, Badoux X, Coutre S, et al. Efficacy and safety of idelalisib in combination with ofatumumab for previously treated chronic lymphocytic leukaemia: an open-label, randomised phase 3 trial. Lancet Haematol. 2017;4:e114-e126 pubmed publisher
    ..Gilead Sciences, Inc. ..
  28. Molica S. Targeted therapy in the treatment of chronic lymphocytic leukemia: facts, shortcomings and hopes for the future. Expert Rev Hematol. 2017;10:425-432 pubmed publisher
    ..Given the increasing number of patients who have access to treatment with small-KI molecules, generally administered over an extended duration, more sustainable pricing for such therapies is needed. ..
  29. He D, Wang M, Zhao S, Shu Y, Zeng H, Xiao C, et al. Pharmaceutical prospects of naturally occurring quinazolinone and its derivatives. Fitoterapia. 2017;119:136-149 pubmed publisher
    b>Quinazolinones belong to a family of heterocyclic nitrogen compounds that have attracted increasing interest because of their broad spectrum of biological functions...
  30. Ding M, Dong Q, Liu Z, Liu Z, Qu Y, Li X, et al. Inhibition of dynamin-related protein 1 protects against myocardial ischemia-reperfusion injury in diabetic mice. Cardiovasc Diabetol. 2017;16:19 pubmed publisher
    ..Pharmacological inhibition of Drp1 prevents mitochondrial fission and reduces MI/R injury in diabetic mice. The findings suggest Drp1 may be a potential novel therapeutic target for diabetic cardiac complications. ..
  31. Wang Y, Huang Z, Chen S, Wang C, Shan C, Yin Q, et al. Design, Synthesis, and Evaluation of New Selective NM23-H2 Binders as c-MYC Transcription Inhibitors via Disruption of the NM23-H2/G-Quadruplex Interaction. J Med Chem. 2017;60:6924-6941 pubmed publisher
    ..This work provides a new strategy to modulate c-MYC transcription for the development of selective anticancer drugs. ..
  32. Eyre T, Fox C, Shankara P, Went R, Schuh A. Idelalisib-Rituximab induces clinical remissions in patients with TP53 disrupted B cell prolymphocytic leukaemia. Br J Haematol. 2017;177:486-491 pubmed publisher
  33. Hrast M, Rozman K, Jukic M, Patin D, Gobec S, Sova M. Synthesis and structure-activity relationship study of novel quinazolinone-based inhibitors of MurA. Bioorg Med Chem Lett. 2017;27:3529-3533 pubmed publisher
    ..Furthermore, furan-substituted quinazolinones (38, 46) showed promising antibacterial activities, with MICs from 1µg/mL to 8µg/mL, concomitant with their ..
  34. Peón A, Robles A, Blanco B, Convertino M, Thompson P, Hawkins A, et al. Reducing the Flexibility of Type?II Dehydroquinase for Inhibition: A Fragment-Based Approach and Molecular Dynamics Study. ChemMedChem. 2017;12:1512-1524 pubmed publisher
  35. Shiver M, Mahmoud F, Gao L. Response to Idelalisib in a Patient with Stage IV Merkel-Cell Carcinoma. N Engl J Med. 2015;373:1580-2 pubmed publisher
  36. Fazio P, Schain M, Mrzljak L, Amini N, Nag S, Al Tawil N, et al. Patterns of age related changes for phosphodiesterase type-10A in comparison with dopamine D2/3 receptors and sub-cortical volumes in the human basal ganglia: A PET study with 18F-MNI-659 and 11C-raclopride with correction for partial volume effect. Neuroimage. 2017;152:330-339 pubmed publisher
    ..Moreover as result of the analysis, in the striatum for both the molecular targets, we observed a gender effect with higher BPND the female group. ..
  37. Garber K. Kinase inhibitors overachieve in CLL. Nat Rev Drug Discov. 2014;13:162-4 pubmed publisher
  38. Pan S, Sharma P, Shah S, Deshpande D. Bitter taste receptor agonists alter mitochondrial function and induce autophagy in airway smooth muscle cells. Am J Physiol Lung Cell Mol Physiol. 2017;313:L154-L165 pubmed publisher