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Molecules 2012, 17(5), 5870-5881; doi:10.3390/molecules17055870

Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines

, , , , ,  and *
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, China
* Author to whom correspondence should be addressed.
Received: 28 April 2012 / Revised: 10 May 2012 / Accepted: 11 May 2012 / Published: 16 May 2012
(This article belongs to the Section Medicinal Chemistry)
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Two series of novel 2-substituted-4-amino-6-halogenquinolines 8al and 13ah were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents exhibited good to excellent antiproliferative activity. Among them, compound 8e was a considered promising lead for further structural modifications with IC50 values of 0.03 μM, 0.55 μM, 0.33 μM and 1.24 μM, which was 2.5- to 186-fold more active than gefitinib and compound 1.
Keywords: 2-substituted-4-amino-6-halogenquinolines; design; synthesis; antiproliferative activity 2-substituted-4-amino-6-halogenquinolines; design; synthesis; antiproliferative activity
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.

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Jiang, N.; Zhai, X.; Li, T.; Liu, D.; Zhang, T.; Wang, B.; Gong, P. Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines. Molecules 2012, 17, 5870-5881.

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