1H-1,2,3-Triazole Tethered Nitroimidazole-Isatin Conjugates: Synthesis, Docking, and Anti-Proliferative Evaluation against Breast Cancer

被引：49

作者：

Kumar, Sumit ^{[1
]}

Saha, Sourav Taru ^{[2
]}

Gu, Liang ^{[2
]}

Palma, Gabriella ^{[2
]}

Perumal, Shanen ^{[2
]}

Singh-Pillay, Ashona ^{[3
]}

Singh, Parvesh ^{[3
]}

Anand, Amit ^{[4
]}

Kaur, Mandeep ^{[2
]}

Kumar, Vipan ^{[1
]}

机构：

[1] Guru Nanak Dev Univ, Dept Chem, Amritsar 143005, Punjab, India

[2] Univ Witwatersrand, Sch Mol & Cell Biol, Private Bag 3, ZA-2050 Johannesburg, South Africa

[3] Univ KwaZulu Natal, Sch Chem & Phys, P Bag X54001, ZA-4000 Durban, South Africa

[4] Khalsa Coll, Dept Chem, Amritsar 143005, Punjab, India

来源：

ACS OMEGA | 2018年 / 3卷 / 09期

基金：

新加坡国家研究基金会;

关键词：

ESTROGEN-RECEPTOR MODULATORS; IN-VITRO; IMIDAZOLE DERIVATIVES; DESIGN; AGENTS; INHIBITORS; HYBRIDS; STATISTICS; ANTICANCER; FERROCENE;

D O I：

10.1021/acsomega.8b01513

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

1H-1,2,3-Triazole tethered imidazole-isatin and imidazole-isatin-thiosemicarbazone conjugates were synthesized and evaluated against MCF-7 and MDA-MB-231 cell lines. Antiproliferative activities of the synthesized conjugates revealed an optimum combination of longer alkyl chain length as spacer and a halogen-substituent on the isatin ring as a prerequisite for good activity. The compound 6g with an optimum combination of chloro-substituent at C-5 position of isatin ring and a butyl chain length proved to be most active and noncytotoxic with IC50s of 54.25 and 26.12 mu M against MCF-7 and MDA-MB-231 cell lines, respectively.

引用

页码：12106 / 12113

页数：8

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