title: Anti-breast cancer activity of some novel 1,2-dihydropyridine, thiophene and thiazole derivatives.
abstract: A variety of novel 1,2-dihydropyridines 10-17, thiophenes 18-21 and thiazole 22 having a biologically active sulfone moiety were obtained via the reaction of 2-cyano-N'-[1-(4-(piperidin-1-ylsulfonyl) phenyl) ethylidene] acetohydrazide 3 with a variety of reagents. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in-vitro anticancer activity against human breast cancer cell line (MCF7). Compounds 15 and 11 with IC(50) values (20.6, 25.5 μM) exhibited better activity than Doxorubicin as a reference drug with IC(50) value (32.02 μM), while compound 14 is nearly as active as Doxorubicin as positive control.
authors.affiliation: Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University. P.O. Box 2457, Riyadh 11451. Saudi Arabia.
authors.forename: Mansour S
authors.initials: MS
authors.lastname: Al-Said
authors.forename: Mahmoud S
authors.initials: MS
authors.lastname: Bashandy
authors.forename: Saleh I
authors.initials: SI
authors.lastname: Al-Qasoumi
authors.forename: Mostafa M
authors.initials: MM
authors.lastname: Ghorab
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology*; D045744:Cell Line, Tumor; D004095:Dihydropyridines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D004095:Dihydropyridines; D013844:Thiazoles; D013876:Thiophenes; C038806:1,4-dihydropyridine