Synthesis of some p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles and their anticancer activity.
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.
Zaharia
Valentin
V
Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania. vzaharia@umfcluj.ro
Ignat
Adriana
A
Palibroda
Nicolae
N
Ngameni
Bathélémy
B
Kuete
Victor
V
Fokunang
Charles N
CN
Moungang
Marlyse L
ML
Ngadjui
Bonaventure T
BT
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
D000970:Antineoplastic Agents; D006834:Hydrazines; D013844:Thiazoles; D014105:Tosyl Compounds; C002030:4-toluenesulfonyl hydrazide