Synthesis and Biological Evaluation of 4-Aroyl-6,7,8-Trimethoxyquinolines as a Novel Class of Anticancer Agents

Molecules

Cheng-Chih Hsieh¹  Hsueh-Yun Lee¹  Chih-Ying Nien¹  Ching-Chuan Kuo¹  Chi-Yen Chang¹  Jang-Yang Chang¹ 

[1] ¹Graduate Institute of Medical Sciences, National Defense Medical Center, No.161, Sec.6. Min-Chuan E. Road, Taipei 114, Taiwan

关键词: combretastatin analogs;    multidrug-resistant;    trimethoxyquinolines;    antiproliferative activity;   

DOI  :  10.3390/molecules16032274

来源: mdpi

【 摘 要 】

A series of 2-aroyl and 2-aryl-5,6,7-trimethoxyquinoline and 4-aroyl-6,7,8-trimethoxyquinoline combretastatin analogs were synthesized and evaluated for their potential anticancer activity. The 4-aroylquinoline 11 inhibited the growth of the human cancer cells lines KB, HT-29, and MKN45, as well as the three human resistant cancer cell lines KB-vin10, KB-S15, and KB-7D, with IC₅₀ values of 217, 327, 239, 246, 213, and 252 nM, respectively.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.