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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 3.0).

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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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