Synthesis and biological evaluation of some novel 6-aryl-2-(p-sulfamylphenyl)-4,5-dihydropyridazin-3(2H)-ones as anti-cancer, antimicrobial, and anti-inflammatory agents

被引：39

作者：

Ahmad, Shamim ^{[1
]}

Rathish, I. G. ^{[1
]}

Bano, Sameena ^{[1
]}

Alam, M. S. ^{[1
]}

Javed, Kalim ^{[1
]}

机构：

[1] Jamia Hamdard, Fac Sci, Dept Chem, New Delhi 110062, India

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2010年 / 25卷 / 02期

关键词：

Pyridazinones; benzenesulfonamides; anti-cancer; anti-inflammatory; antimicrobial; CARBONIC-ANHYDRASE; DISCOVERY; ANTIBACTERIAL; SULFONAMIDES; ANTIFUNGAL; INHIBITORS; POTENT; SCREEN;

D O I：

10.3109/14756360903155781

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：

A series of 6-aryl-2-(p-sulfamylphenyl)-4,5-dihydropyridazin-3(2H)-ones (2a-j) were synthesized by condensation of the appropriate beta-aroylpropionic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol and tested for anti-cancer, anti-inflammatory, and antimicrobial actions. According to the protocol of the National Cancer Institute (NCI) in vitro disease-oriented human cells screening panel assay, compound 2g showed high activity against HL-60 (TB) (leukemia), SR (leukemia), NCI-H522 (non-small-cell lung cancer), and BT-549 (breast cancer) with a GI(50) value of less than 2 mu M. Two compounds (2c and 2f) were found to have promising anti-inflammatory activity, while a fair number of compounds showed good antifungal activity.

引用

页码：266 / 271

页数：6

共 21 条

[1]

Bisen P. S., 1994, HDB MICROBIOLOGY

[2] SOME PRACTICAL CONSIDERATIONS AND APPLICATIONS OF THE NATIONAL-CANCER-INSTITUTE IN-VITRO ANTICANCER DRUG DISCOVERY SCREEN [J].

BOYD, MR ;

PAULI, KD .

DRUG DEVELOPMENT RESEARCH, 1995, 34 (02) :91-109

[3]

Boyd MR, 1997, CANC DRUG DISCOVERY, P23

[4]

Chohan ZH, 2008, J ENZYM INHIB MED CH, V23, P120, DOI [10.1080/14756360701384195, 10.1080/14756360701384195 ]

[5] Antibacterial, antifungal and cytotoxic properties of novel N-substituted sulfonamides from 4-hydroxycoumarin [J].

Chohan, Zahid H. ;

Shaikh, Ali U. ;

Rauf, Abdul ;

Supuran, Claudiu T. .

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2006, 21 (06) :741-748

[6]

Coates WJ., 1996, COMPREHENSIVE HETERO, V6, P1, DOI DOI 10.1016/B978-008096518-5.00117-9

[7] Synthesis and aldose reductase inhibitory activity of a new series of benzo[h]cinnolinone derivatives [J].

Costantino, L ;

Rastelli, G ;

Cignarella, G ;

Barlocco, D .

FARMACO, 2000, 55 (08) :544-552

[8] ABT-963 [2-(3,4-Difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one], a highly potent and selective disubstituted pyridazinone cyclooxgenase-2 inhibitor [J].

Harris, RR ;

Black, L ;

Surapaneni, S ;

Kolasa, T ;

Majest, S ;

Namovic, MT ;

Grayson, G ;

Komater, V ;

Wilcox, D ;

King, L ;

Marsh, K ;

Jarvis, MF ;

Nuss, M ;

Nellans, H ;

Pruesser, L ;

Reinhart, GA ;

Cox, B ;

Jacobson, P ;

Stewart, A ;

Coghlan, M ;

Carter, G ;

Bell, RL .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2004, 311 (03) :904-912

[9]

Khan MSY, 2000, INDIAN J CHEM B, V39, P614

[10]

Khan MSY, 2002, INDIAN J CHEM B, V41, P2160

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