2,6-Disubstituted imidazo[2,1-b][1,3,4]thiadiazoles: Search for anticancer agents

被引：57

作者：

Noolvi, Malleshappa N. ^{[1
]}

Patel, Harun M. ^{[2
]}

Kamboj, Santa ^{[3
]}

Kaur, Amandeep ^{[3
]}

Mann, Vikas ^{[3
]}

机构：

[1] Shree Dhanvantary Pharm Coll, Dept Pharmaceut Chem, Kim Surat 3941110, Gujarat, India

[2] RC Patel Inst Pharmaceut Educ & Res, Dept Pharmaceut Chem, Shirpur Dhule 425405, Maharashtra, India

[3] ASBASJSM Coll Pharm, Dept Pharmaceut Chem, Bela Ropar 140111, Punjab, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 56卷

关键词：

Synthesis imidazo[2,1-b][1,3,4]thiadiazole; Anticancer agents; NCI; POTENTIAL ANTITUMOR AGENTS; QUINAZOLINE; DERIVATIVES; SERIES;

D O I：

10.1016/j.ejmech.2012.08.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this study, some novel 2,6-disubstituted imidazo[2,1-b][1,3,4]thiadiazoles 4 (a-i), 7 (a-p) and 11 (a-i) were synthesized from 5-substituted-1,3,4-thiadiazol-2-amine. The newly synthesized compounds 4a, 4b, 4c, 4e, 4g, 7j, 7l, 11b and 11c were evaluated in the National Cancer Institute for single dose in vitro primary cytotoxicity assay. Among the tested nine compounds, compound 4b (107166/760239) and 4c (107168/760240) were passed the criteria for activity in this assay and scheduled automatically for evaluation against the full panel of 60 human tumor cell lines at a minimum of five concentrations at 10-fold dilutions. 3-(2-(4-methoxyphenyl)imidazo[2,1-b][1,3,4]thiadiazol-6-yl)aniline (4c) exhibited significant in vitro anticancer activity against Non Small Cell Lung Cancer HOP-92 cell line (GI(50): 0.114 mu M) and Renal Cancer CAKI-1 cell line (GI(50): 0.743 mu M). (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：56 / 69

页数：14

共 22 条

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