Benzotriazole Substituted 2-Phenylquinazolines as Anticancer Agents: Synthesis, Screening, Antiproliferative and Tubulin Polymerization Inhibition Activity

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dc.contributor.authorDwivedi, Ashish Ranjan
dc.contributor.authorRawat, Suraj Singh
dc.contributor.authorKumar, Vijay
dc.contributor.authorKumar, Naveen
dc.contributor.authorKumar, Vinay
dc.contributor.authorYadav, Ravi Prakash
dc.contributor.authorBaranwal, Somesh
dc.contributor.authorPrasad, Amit
dc.contributor.authorKumar, Vinod
dc.date.accessioned2024-01-21T10:37:04Z
dc.date.accessioned2024-08-13T11:19:28Z
dc.date.available2024-01-21T10:37:04Z
dc.date.available2024-08-13T11:19:28Z
dc.date.issued2022-10-28T00:00:00
dc.description.abstractAims: Development of anticancer agents targeting tubulin protein. Background: Tubulin protein is being explored as an important target for anticancer drug development. Ligands binding to the colchicine binding site of the tubulin protein act as tubulin polymerization inhibitors and arrest the cell cycle in the G2/M phase. Objective: Synthesis and screening of benzotriazole-substituted 2-phenyl quinazolines as potential anticancer agents. Methods: A series of benzotriazole-substituted quinazoline derivatives have been synthesized and evaluated against human MCF-7 (breast), HeLa (cervical) and HT-29 (colon) cancer cell lines using standard MTT assays. Results: ARV-2 with IC50 values of 3.16 �M, 5.31 �M, 10.6 �M against MCF-7, HELA and HT29 cell lines, respectively displayed the most potent antiproliferative activities in the series while all the compounds were found non-toxic against HEK293 (normal cells). In the mechanistic studies involving cell cycle analysis, apoptosis assay and JC-1 studies, ARV-2 and ARV-3 were found to induce mitochondria-mediated apoptosis. Conclusion: The benzotriazole-substituted 2-phenyl quinazolines have the potential to be developed as potent anticancer agents. � 2023 Bentham Science Publishers.en_US
dc.identifier.doi10.2174/1568009623666221028121906
dc.identifier.issn15680096
dc.identifier.urihttp://10.2.3.109/handle/32116/3476
dc.identifier.urlhttps://www.eurekaselect.com/210444/article
dc.language.isoen_USen_US
dc.publisherBentham Science Publishersen_US
dc.subject2-Phenylquinazolinesen_US
dc.subjectanticanceren_US
dc.subjectantiproliferativeen_US
dc.subjectcell cycleen_US
dc.subjectHeLa cellsen_US
dc.subjecttubulin polymerization inhibitorsen_US
dc.titleBenzotriazole Substituted 2-Phenylquinazolines as Anticancer Agents: Synthesis, Screening, Antiproliferative and Tubulin Polymerization Inhibition Activityen_US
dc.title.journalCurrent Cancer Drug Targetsen_US
dc.typeArticleen_US
dc.type.accesstypeClosed Accessen_US

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