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Bioorg Med Chem Lett ; 25(17): 3616-20, 2015 Sep 01.
Article in English | MEDLINE | ID: mdl-26152430

ABSTRACT

4-Thiazolidinone derivatives were synthesized using T3P®-DMSO media as a cyclodehydrating agent. All the molecules were tested for their cytotoxicity against leukemic cell lines. The compound 3-(4-bromophenyl)-2-(4-(dimethylamino)phenyl)thiazolidin-4-one (4e) with electron donating substituent at para position of phenyl ring displayed considerable cytotoxicity against Reh and Nalm6 cells with an IC50 value of 11.9 and 13.5 µM, respectively. Furthermore, the compound 4e tested for tumor regression studies induced by EAC in Swiss albino mouse. Both in vitro and in vivo results suggested significant antiproliferative activity of compound 4e in Reh cells and mouse tumor tissue treated with compound 4e showed multifocal areas of necrosis and numerous number of apoptotic cells.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Neoplasms/drug therapy , Thiazolidines/chemistry , Thiazolidines/pharmacology , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Drug Design , Drug Screening Assays, Antitumor , Humans , Leukemia/drug therapy , Leukemia/pathology , Mice , Neoplasms/pathology , Structure-Activity Relationship , Thiazolidines/chemical synthesis , Thiazolidines/therapeutic use
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