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

Molecules

Nan Jiang¹  Xin Zhai¹  Ting Li¹  Difa Liu¹  Tingting Zhang¹  Bin Wang¹ 

[1]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

关键词: 2-substituted-4-amino-6-halogenquinolines;    design;    synthesis;    antiproliferative activity;   

DOI  :  10.3390/molecules17055870

来源: mdpi

【 摘 要 】

Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a–l and 13a–h 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.

【 授权许可】

CC BY   
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.