Synthesis, anticancer, and anti-inflammatory activity evaluation of methanesulfonamide and amidine derivatives of 3,4-diaryl-2-imino-4-thiazolines

被引：31

作者：

Sondhi, Sham M. ^{[1
]}

Rani, Reshma ^{[1
]}

Gupta, P. P. ^{[2
]}

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

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

机构：

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

[2] BRD Med Coll, Dept Pharmacol, Gorakhpur 273013, UP, India

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

来源：

MOLECULAR DIVERSITY | 2009年 / 13卷 / 03期

关键词：

Amidine; Sulfonamide; Heterocyclic; Anti-inflammatory; Anticancer; Thiazolines; ANALGESIC ACTIVITY EVALUATION; SULFONAMIDE; ANTITUMOR; THIAZOLE; POTENT; ANTIBACTERIAL; INHIBITORS; AGENTS; ASSAY; ACID;

D O I：

10.1007/s11030-009-9125-0

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Condensation of 3,4-diaryl-2-imino-4-thiazoli-nes 1a-j with methanesulfonyl chloride gave methanesulfonamide derivatives 2a-j. Condensation of 2-cyanopyrazine, 4-cyanopyridine, and 2-cyanopyridine with 3,4-diaryl-2- imino-4-thiazolines 1h-m in the presence of sodium methoxide afforded amidine derivatives 3a-j. Compounds 2a-j and 3a-j were screened against various human cancer cell lines (COLO-205, HEP-2, A-549, IMR-32) and their percentage growth inhibition profile determined at 1 x 10(-5)M. The anti-inflammatory activity of these compounds was assessed using the carrageenan-induced paw edema model. Compound 2i exhibited 34.7% anti-inflammatory activity at 50 mg/kg p.o., which is comparable to standard care drug phenyl butazone (37% activity at 50 mg/kg p.o.).

引用

页码：357 / 366

页数：10

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