Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Microwave Assisted Synthesis, Characterization of Some New Isatin and Thiophene Derivatives as Cytotoxic and Chemopreventive Agents

Author(s): Kiran Gangarapu, Sarangapani Manda, Sreekanth Thota, Rajeshwar Yerra, Subhas S. Karki, Jan Balzarini, Erik De Clercq, Harukuni Tokuda.


In obtaining some new cytotoxic and chemopreventive agents with potent antiproliferative activity against cancer cells, a series of new β-isatin aldehyde-N,N’-thiocarbohydrazone, bis-β-isatin thiocarbohydrazones, bis-β-isatin carbohydrazones, N,2-bis(thiophen-2-ylmethylidene) thiocarbohydrazone and N,2-bis(thiophen-2-ylmethylidene) carbohydrazone derivatives was synthesized by microwave oriented reaction and evaluated for their in vitro cytotoxic activity. The newly synthesized compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. The inhibitory effects of synthesized compounds on the proliferation of murine leukemia cells (L1210), human T-lymphocyte cells (CEM) and human cervix carcinoma cells (HeLa) were assayed by using MTT assay. The compounds were also tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-Otetradecanoylphorbol- 13-acetate (TPA). In vitro evaluation of these schiff bases revealed mild to moderate cytotoxic activity in a dose dependent manner. The results of the in vitro inhibitory activities of synthetic compounds against EBVEA activation with IC50 ranges from 485-535 (mol ratio/32pmol/TPA). Chlorine group containing derivatives did not show increased inhibitory activity against tumor promoter TPA induction. Sulphur containing derivatives also did not show a high inhibitory potency in this system.

Keywords: Carbohydrazide, Cytotoxic activity, Epstein-Barr virus antigen (EBV-EA) activation, Isatin, Thiophene-2- carboxaldehyde, Thiocarbohydrazide, Isatin–β-thiosemicarbazone derivatives, antihistamine, Cancer chemoprevention

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Article Details

Year: 2012
Page: [934 - 941]
Pages: 8
DOI: 10.2174/1570180811209050934
Price: $58