A Series of Isatin-Hydrazones with Cytotoxic Activity and CDK2 Kinase Inhibitory Activity: A Potential Type II ATP Competitive Inhibitor.

ABSTRACT: Isatin derivatives potentially act on various biological targets. In this article, a series of novel isatin-hydrazones were synthesized in excellent yields. Their cytotoxicity was tested against human breast adenocarcinoma (MCF7) and human ovary adenocarcinoma (A2780) cell lines using MTT assay. Compounds 4j (IC₅₀ = 1.51 ± 0.09 µM) and 4k (IC₅₀ = 3.56 ± 0.31) showed excellent activity against MCF7, whereas compound 4e showed considerable cytotoxicity against both tested cell lines, MCF7 (IC₅₀ = 5.46 ± 0.71 µM) and A2780 (IC₅₀ = 18.96± 2.52 µM), respectively. Structure-activity relationships (SARs) revealed that, halogen substituents at 2,6-position of the C-ring of isatin-hydrazones are the most potent derivatives. In-silico

SUBMITTER: Al-Salem HS 

PROVIDER: S-EPMC7582667 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature