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Synthesis of some p-toluenesulfonyl-hydrazinothiazoles and hydrazino-bis-thiazoles and their anticancer activity.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2010 Nov; Vol. 45 (11), pp. 5080-5. Date of Electronic Publication: 2010 Aug 12. - Publication Year :
- 2010
-
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.<br /> (Copyright © 2010 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Antineoplastic Agents pharmacology
Cell Line, Tumor
Humans
Hydrazines pharmacology
Magnetic Resonance Spectroscopy
Thiazoles pharmacology
Tosyl Compounds pharmacology
Antineoplastic Agents chemical synthesis
Hydrazines chemical synthesis
Thiazoles chemical synthesis
Tosyl Compounds chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 45
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 20810194
- Full Text :
- https://doi.org/10.1016/j.ejmech.2010.08.017