Structure-Activity Relationship Studies of Chalcones and Diarylpentanoids with Antitumor Activity: Potency and Selectivity Optimization.

ABSTRACT: We previously reported that chalcone CM-M345 (1) and diarylpentanoid BP-C4 (2) induced p53-dependent growth inhibitory activity in human cancer cells. Herein, CM-M345 (1) and BP-C4 (2) analogues were designed and synthesized in order to obtain more potent and selective compounds. Compounds 16, 17, 19, 20, and 22-24 caused pronounced in vitro growth inhibitory activity in HCT116 cells (0.09 < GI₅₀ < 3.10 μM). Chemical optimization of CM-M345 (1) led to the identification of compound 36 with increased selectivity for HCT116 cells expressing wild-type p53 compared to its p53-null isogenic derivative and low toxicity to non-tumor HFF-1 cells. The molecular modificat

SUBMITTER: Moreira J 

PROVIDER: S-EPMC10610188 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature