Molecules 2011, 16(3), 2274-2284; doi:10.3390/molecules16032274
Article

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

Cheng-Chih Hsieh 1,2 , Hsueh-Yun Lee 3 , Chih-Ying Nien 3 , Ching-Chuan Kuo 4 email, Chi-Yen Chang 4 email, Jang-Yang Chang 4,* email and Jing-Ping Liou 3,* email
1 Graduate Institute of Medical Sciences, National Defense Medical Center, No.161, Sec.6. Min-Chuan E. Road, Taipei 114, Taiwan 2 Department of Pharmacy Practice, Tri-Service General Hospital, No.325, Sec.2. Cheng-Kung Road, Taipei 114, Taiwan 3 School of Pharmacy, College of Pharmacy, Taipei Medical University, No. 250 Wuxing Street, Taipei 11031, Taiwan 4 National Institute of Cancer Research, National Health Research Institutes. 2 F, No.367, Sheng Li Road, Tainan 704, Taiwan
* Authors to whom correspondence should be addressed.
Received: 28 January 2011; in revised form: 2 March 2011 / Accepted: 4 March 2011 / Published: 7 March 2011
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: combretastatin analogs; multidrug-resistant; trimethoxyquinolines; antiproliferative activity

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Cite This Article

MDPI and ACS Style

Hsieh, C.-C.; Lee, H.-Y.; Nien, C.-Y.; Kuo, C.-C.; Chang, C.-Y.; Chang, J.-Y.; Liou, J.-P. Synthesis and Biological Evaluation of 4-Aroyl-6,7,8-Trimethoxyquinolines as a Novel Class of Anticancer Agents. Molecules 2011, 16, 2274-2284.

AMA Style

Hsieh C-C, Lee H-Y, Nien C-Y, Kuo C-C, Chang C-Y, Chang J-Y, Liou J-P. Synthesis and Biological Evaluation of 4-Aroyl-6,7,8-Trimethoxyquinolines as a Novel Class of Anticancer Agents. Molecules. 2011; 16(3):2274-2284.

Chicago/Turabian Style

Hsieh, Cheng-Chih; Lee, Hsueh-Yun; Nien, Chih-Ying; Kuo, Ching-Chuan; Chang, Chi-Yen; Chang, Jang-Yang; Liou, Jing-Ping. 2011. "Synthesis and Biological Evaluation of 4-Aroyl-6,7,8-Trimethoxyquinolines as a Novel Class of Anticancer Agents." Molecules 16, no. 3: 2274-2284.

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