Synthesis and Cytotoxic Evaluation of 3-(4-Fluorophenyl)-4,5-dihydro-5-(3,4,5-trimethoxy/4-nitrophenyl)-N-(substituted-phenyl)pyrazole-1-carboxamide Analogues

被引：2

作者：

Ahsan, Mohamed J. ^{[1
]}

Kumawat, Bhawani S. ^{[1
]}

Kumawat, Sonu ^{[1
]}

Sharma, Piush ^{[1
]}

Bakht, Mohammad A. ^{[2
]}

Hassan, Mohd Z. ^{[3
]}

Hussain, Afzal ^{[4
]}

Saraswat, Pankaj ^{[5
]}

Khalilullah, Habibullah ^{[6
]}

机构：

[1] Maharishi Arvind Coll Pharm, Dept Pharmaceut Chem, Jaipur 302039, Rajasthan, India

[2] Prince Sattam Bin Abdulaziz Univ, Coll Sci & Humanities, Dept Chem, POB 11323, Al Kharj, Saudi Arabia

[3] King Khalid Univ, Coll Pharm, Dept Pharmaceut Chem, Abha 62529, Saudi Arabia

[4] Birla Inst Sci & Technol, Dept Pharmaceut Sci & Technol, Ranchi 835215, Jharkhand, India

[5] Alwar Pharm Coll, Dept Pharmaceut Chem, Alwar 301030, Rajasthan, India

[6] Qassim Univ, Unaizah Coll Pharm, Dept Pharmaceut Chem, Al Qassim 51911, Saudi Arabia

来源：

SYNOPEN | 2018年 / 2卷 / 02期

关键词：

anticancer agents; breast cancer cell lines; MCF-7; MDA-MB-231; SRB assay; pyrazolines;

D O I：

10.1055/s-0036-1591980

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A novel series of 3-(4-fluorophenyl)-4,5-dihydro-5-(3,4,5-trimethoxy/4-nitro phenyl)-N-(substituted-phenyl)pyrazole-1-carboxamide analogues 4a-n was synthesized in two steps from 4-fluoroace-tophenone. The pyrazoline analogues were evaluated for cytotoxicity against two breast cancer cell lines (MCF-7 and MBA-MD-231) by the sulforhodamine B (SRB) assay. N-(4-Chlorophenyl)-3-(4-fluorophenyl)5-(4-nitrophenyl)-4,5-dihydro-1H-pyrazole-1-carboxamide (4b) showed the most promising cytotoxicity among the series, with GI(50) <0.1 and 45.8 mu M against the cancer cell lines, MCF-7 and MDA-MB-231, respectively. The anticancer activity of 4b was found to be comparable to that of the standard drug adriamycin (GI(50) < 0.1) against the MCF-7 cancer cell line. Structure activity relationships (SAR) are also considered.

引用

页码：114 / 121

页数：8

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