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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

1,2, 3, 3, 4
,
4
,
4,*  and 3,*
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 / Revised: 2 March 2011 / Accepted: 4 March 2011 / Published: 7 March 2011
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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 combretastatin analogs; multidrug-resistant; trimethoxyquinolines; antiproliferative activity
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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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.

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