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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

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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MDPI and ACS Style

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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