Synthesis of novel analogs of 2-pyrazoline obtained from [(7-chloroquinolin-4-yl)amino]chalcones and hydrazine as potential antitumor and antimalarial agents

被引：117

作者：

Insuasty, Braulio ^{[1
]}

Montoya, Alba ^{[1
]}

Becerra, Diana ^{[1
]}

Quiroga, Jairo ^{[1
]}

Abonia, Rodrigo ^{[1
]}

Robledo, Sara ^{[2
]}

Velez, Ivan Dario ^{[2
]}

Upegui, Yulieth ^{[2
]}

Nogueras, Manuel ^{[3
]}

Cobo, Justo ^{[3
]}

机构：

[1] Univ Valle, Dept Chem, Heterocycl Cpds Res Grp, Cali 25360, Colombia

[2] Univ Antioquia, PECET SIU, Medellin, Colombia

[3] Univ Jaen, Dept Inorgan & Organ Chem, Jaen 23071, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 67卷

关键词：

Pyrazolines; Chalcones; Cyclocondensation reaction; Antitumor and antimalarial activities; IN-VITRO; CHALCONE DERIVATIVES; ANTIMICROBIAL ACTIVITY; INHIBITORY PROPERTIES; CELL-LINES; ANTIBACTERIAL; ANTICANCER; DESIGN; CANCER; PYRAZOLINES;

D O I：

10.1016/j.ejmech.2013.06.049

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of N-acetyl and N-formyl-pyrazoline derivatives 6 and 7-8 were synthesized by cyclocondensation reaction of [(7-chloroquinolin-4-yl)amino]chalcones with hydrazine hydrate in acetic acid and hydrazine hydrate in formic acid respectively. These compounds were evaluated in vitro as antitumor and as antimalarial agents. Compounds 7b and 8b-e showed remarkable antitumor activity against cancer cell lines, with the most important GI(50) values ranging from 0.13 to 0.99 mu M. The best antimalarial response was observed for compound 7a with an inhibition percentage of 50.8% for Plasmodium falciparum, a hemolytic capacity of 3.2% and an IC50 of 14.1 mu g/mL. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：252 / 262

页数：11

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