Synthesis, QSAR Study and Antitumor Activity of Desmosdumotin-C Analogues
- Author:
Zhuo XIANG
1
Author Information
- Publication Type:Journal Article
- Keywords: Antitumor apoptosis; CoMFA study; Des-C derivatives; Structure-activity relationship; Synthesis
- From: Chinese Pharmaceutical Journal 2017;52(16):1387-1392
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To further design and synthesize Desmosdumotin-C(Des-C) derivatives and investigate their antitumor activities. METHODS: QSAR study using the CoMFA method was performed on a set of reported Des-C derivatives to facilitate the elucidation of their SAR and discovery of new potent Des-C derivatives. Flow cytometry was used to investigate antitumor activity. RESULTS: The established model showed good predictive ability and aid in the design of potent Des-C derivatives. An efficient three-step synthetic strategy toward Des-C derivatives was developed and applied to synthesize 10 new derivatives which showed superior antitumor activities against A549 and HL60 cells in vitro. CONCLUSION: The structural modification of Des-C would significantly increase the antitumor activity. It is preliminarily confirmed that the derivatives are potent antitumor agents with apoptosis-inducing ability, which provides the basis for the further study.
