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Arzneimittelforschung 2008; 58(7): 353-357
DOI: 10.1055/s-0031-1296519
Antibiotics · Antimycotics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

Evaluation of the Antiproliferative Activity of 2-(Monohalogenophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles

Matgorzata Juszczak
1   Department of Toxicology, Institute of Agricultural Medicine, Lublin, Poland
,
Joanna Matysiak
2   Department of Chemistry, Agricultural University, Lublin, Poland
,
Wojciech Brzana
1   Department of Toxicology, Institute of Agricultural Medicine, Lublin, Poland
,
Andrzej Niewiadomy
2   Department of Chemistry, Agricultural University, Lublin, Poland
,
Wojciech Rzeski
1   Department of Toxicology, Institute of Agricultural Medicine, Lublin, Poland
3   Department of Virology and Immunology, Institute of Microbiology and Biotechnology, Maria Curie-Skłodowska University, Lublin, Poland
› Author Affiliations
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Publication History

Publication Date:
15 December 2011 (online)

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Abstract

Two 2-(monohalogenophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles were synthesized by reaction of sulfinyl bis(2,4-dihydroxythiobenzoyl) with 4-substituted 3-thiosemicarbazides and evaluated for their antiproliferative activity in tumor cells and for cytotoxicity in normal cells. Both derivatives in micro-molar concentrations elicited a prominent antiproliferative effect in tumor cells derived from cancers of the nervous system (rhabdomyosarcoma/medulloblastoma, glioma) and peripheral cancers, including breast adenocarcinoma and lung carcinoma. The anticancer effect was attributed to decreased DNA synthesis and was not connected with apoptosis induction. Both compounds were not toxic to normal human skin fibroblasts.

Key words

2-Amino-5-(2,4-dihydroxy-phenyl)-1,3,4-thiadiazoles, antiproliferative activity - apoptosis, cytotoxicity - Anticancer agents
 

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