Synthesis and biological evaluation of 4-aroyl-6,7,8-trimethoxyquinolines as a novel class of anticancer agents

Cheng-Chih Hsieh; Hsueh-Yun Lee; Chih-Ying Nien; Ching-Chuan Kuo; Chi-Yen Chang; Jang-Yang Chang; Jing-Ping Liou

doi:10.3390/molecules16032274

Synthesis and biological evaluation of 4-aroyl-6,7,8-trimethoxyquinolines as a novel class of anticancer agents

Molecules. 2011 Mar 7;16(3):2274-84. doi: 10.3390/molecules16032274.

Authors

Cheng-Chih Hsieh¹, Hsueh-Yun Lee, Chih-Ying Nien, Ching-Chuan Kuo, Chi-Yen Chang, Jang-Yang Chang, Jing-Ping Liou

Affiliation

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

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Humans
Quinolines / chemical synthesis*
Quinolines / pharmacology*

Substances

Antineoplastic Agents
Quinolines