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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Formamide Derivatives of Resveratrol: Synthesis, Characterization and Cytotoxicity

Author(s): Hai-Jun Ni, Hui-Jie Cheng, Wei-Wei Ge, Meng-Xue Lin, Qing-Shan Li and Ban-Feng Ruan

Volume 13, Issue 6, 2016

Page: [495 - 504] Pages: 10

DOI: 10.2174/157018081306160618153304

Price: $65

Abstract

Resveratrol (3,4,5'-trihydroxy-trans-stilibene) is a famous natural product which exhibits potential antitumor activity both in vitro and in vivo. In this article, A series of formamide derivatives of resveratrol (C1-27) were synthesized and their cytotoxic activities were evaluated, with results indicating that most of the compounds exhibited antitumor activity against both Smmc7721 and SGC7901 cancer cell lines. Among them, compound C21 displayed the most potent antitumor activities, with IC50 values of 7.68 and 6.16 M against Smmc7721 and SGC7901 cancer cell lines respectively. All compounds reported herein were characterized by 1H NMR, 13C NMR, MS and IR spectrum. Additionally, the structure of compound C10 was confirmed by X-ray crystallographic analysis.

Keywords: Resveratrol, formamide derivatives, synthesis, characterization, single-crystal x-ray diffraction, antitumor activity.

Graphical Abstract


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