Synthesis and Cytotoxic Evaluation of Alkoxylated Chalcones

Molecules

Xiao-Guang Bai¹  Chang-Liang Xu¹  Shuang-Shuang Zhao²  Hong-Wei He²  Yu-Cheng Wang²  Ju-Xian Wang¹ 

[1]Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China

关键词: alkoxylated chalcones;    synthesis;    cytotoxicity;   

DOI  :  10.3390/molecules191117256

来源: mdpi

【 摘 要 】

A series of chalcones a1–20 bearing a 4-OMe groups on the A-ring were initially synthesized and their anticancer activities towards HepG2 cells evaluated. Subsequently, a series of chalcones b1–42 bearing methoxy groups at the 2' and 6'-positions of the B-ring were synthesized and their anticancer activities towards five human cancer cell lines (HepG2, HeLa, MCF-7, A549 and SW1990) and two non-tumoral human cell lines evaluated. The results showed that six compounds (b6, b8, b11, b16, b18, b22, b23 and b29) displayed promising activities, with compounds b22 and b29 in particular showing higher levels of activity than etoposide against all five cancer cell lines. Compound b29 showed a promising SI value compared with both HMLE and L02 (2.1–6.5 fold in HMLE and > 33 > 103.1 fold in L02, respectively).

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.