Synthesis, Anti-Inflammatory, and Anticancer Activity Evaluation of Some Heterocyclic Amidine and Bis-Amidine Derivatives

被引：13

作者：

Sondhi, Sham M. ^{[1
]}

Rani, Reshma ^{[1
]}

Roy, Partha ^{[2
]}

Agrawal, S. K. ^{[3
]}

Saxena, A. K. ^{[3
]}

机构：

[1] Indian Inst Technol Roorkee, Dept Chem, Roorkee 247667, Uttarakhand, India

[2] Indian Inst Technol Roorkee, Dept Biotechnol, Roorkee 247667, Uttarakhand, India

[3] Indian Inst Integrat Med, Div Pharmacol, Jammu 180001, India

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2011年 / 48卷 / 04期

关键词：

EFFICIENT SYNTHESIS; ANTITUMOR; BENZIMIDAZOLE; AGENTS; DIAMIDINES; INHIBITORS; ASSAY;

D O I：

10.1002/jhet.658

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Heterocyclic amidine derivatives of benzothiazole (6a-c), benzimidazole (6d-f), benzoxazole (6g-i), and bis-amidine derivatives of pyrimidine, (7a, 7b) & triazole (7c-e) ring system have been synthesized by nucleophilic addition reaction. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50 mg/kg p.o., compounds 6c (39%), 6e (39%), and 6f (39%) exhibited anti-inflammatory activity comparable to standard drug ibuprofen, which showed 39% activity and compounds 6b, 6e, 7a, and 7c exhibited moderate anticancer activity against cervix (HELA); neuroblastoma (IMR-32); breast (MCF-7), leukemia (THP-1); and cervix (HELA) human cancer cell lines, respectively.

引用

页码：921 / 926

页数：6

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