Oxindole-benzothiazole hybrids as CDK2 inhibitors and anticancer agents: design, synthesis and biological evaluation.

ABSTRACT: In the current study, molecular hybridization between the oxindole core and benzothiazole system through an acetohydrazide moiety was accomplished for the design of a new series of oxindole-benzothiazole hybrids 9a-r targeting CDK2 for cancer therapy. The afforded hybrids displayed promising growth inhibitory activity on NCI cancer cell lines at 10 µM. Compound 9o displayed mean GI% = 55.91%. Based on the potent activity of 9o, it was further assessed for its cytotoxic activity at five dose level and it demonstrated GI₅₀ reaching 2.02 µM. Analysis of the cell cycle of the prostate cancer cell line DU145 after treatment with 9o confirmed its ability to arrest its cell cycle at the G1 phase. Moreover, 9o proved its ability to potentiate the apoptosis and necrosis of the same cell

SUBMITTER: Abdel-Mohsen HT 

PROVIDER: S-EPMC11396129 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature