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.
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 microM. Two compounds (2c and 2f) were found to have promising anti-inflammatory activity, while a fair number of compounds showed good antifungal activity.
Ahmad
Shamim
S
Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
Rathish
I G
IG
Bano
Sameena
S
Alam
M S
MS
Javed
Kalim
K
D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001424:Bacterial Infections / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007249:Inflammation / Q000188:drug therapy*; D009181:Mycoses / Q000188:drug therapy*; D054547:National Cancer Institute (U.S.); D009369:Neoplasms / Q000188:drug therapy*; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D014481:United States
D000893:Anti-Inflammatory Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D011724:Pyridazines; D013449:Sulfonamides