European Journal of Medicinal Chemistry p. 164 - 177 (2016)
Update date:2022-08-11
Topics:
Ganga Reddy
Srinivasa Reddy
Lakshma Nayak
Prasad, Budaganaboyina
Reddy, Adiyala Praveen
Ravikumar
Taj, Shaik
Kamal, Ahmed
A series of new (N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives (8–35) were designed, synthesized and evaluated as CDK1/Cdc2 inhibitors. Biological evaluation assays indicated that compounds 16 and 27 showed the most potent growth inhibitory activity against human cancer cell lines (MIAPaCa-2, MCF-7 and HeLa) with GI50values ranging from 0.13 to 0.7?μM, compared with the positive control nocodazole (0.81–0.95?μM). Flow cytometric analysis revealed that these compounds induce cell cycle arrest in the G2/M phase and Western blot analysis suggested that compound treatment resulted in reduction of CDK1 expression levels in MCF-7?cell line. Moreover, the apoptosis inducing effect of the compounds was studied using Hoechst staining, Rhodamine 123 staining (MMP), carboxy-DCFDA staining (ROS), Annexin V-FITC assay. 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.
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