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

被引：10
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
收藏
页码：921 / 926
页数：6
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