title: Synthesis of some p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles and their anticancer activity.
abstract: A series of novel p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles derivatives (2a-f, 3a-f and 5-8) were synthesized by initial condensation of p-toluenesulfonylthiosemicarbazide 1 with a series of α-halogenocarbonyls in acetone or dimethylformamide (DMF)/acetone, mixture. All our synthesized compounds were submitted for further acylation reaction in the presence of acetic anhydride. The structures of newly synthesized derivatives 2a-f, 3a-f and 5-8 were confirmed by IR, (1)H-NMR, EIMS spectral data and elemental analysis. Compounds 2a, 2c, 2d, 2e and 3a showed significant anticancer activities (IC(50)<10 μM) on both prostate DU-145 and hepatocarcinoma Hep-G2 cancer cell lines.
authors.affiliation: Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania. vzaharia@umfcluj.ro
authors.forename: Valentin
authors.initials: V
authors.lastname: Zaharia
authors.forename: Adriana
authors.initials: A
authors.lastname: Ignat
authors.forename: Nicolae
authors.initials: N
authors.lastname: Palibroda
authors.forename: Bathélémy
authors.initials: B
authors.lastname: Ngameni
authors.forename: Victor
authors.initials: V
authors.lastname: Kuete
authors.forename: Charles N
authors.initials: CN
authors.lastname: Fokunang
authors.forename: Marlyse L
authors.initials: ML
authors.lastname: Moungang
authors.forename: Bonaventure T
authors.initials: BT
authors.lastname: Ngadjui
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014105:Tosyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D006834:Hydrazines; D013844:Thiazoles; D014105:Tosyl Compounds; C002030:4-toluenesulfonyl hydrazide