title: Antiproliferative and tumor inhibitory studies of 2,3 disubstituted 4-thiazolidinone derivatives.
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.
authors.affiliation: Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysuru 570006, India.
authors.forename: Kothanahally S
authors.initials: KS
authors.lastname: Sharath Kumar
authors.affiliation: Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysuru 570006, India.
authors.forename: Ananda
authors.initials: A
authors.lastname: Hanumappa
authors.affiliation: Department of Veterinary Pathology, Veterinary College, Hebbal, Bengaluru 560024, India.
authors.forename: Maruthai
authors.initials: M
authors.lastname: Vetrivel
authors.affiliation: Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysuru 570006, India.
authors.forename: Mahesh
authors.initials: M
authors.lastname: Hegde
authors.affiliation: Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysuru 570006, India.
authors.forename: Yarabhally R
authors.initials: YR
authors.lastname: Girish
authors.affiliation: Department of Veterinary Pathology, Veterinary College, Hebbal, Bengaluru 560024, India.
authors.forename: Thinnali R
authors.initials: TR
authors.lastname: Byregowda
authors.affiliation: Department of Veterinary Pathology, Veterinary College, Hebbal, Bengaluru 560024, India.
authors.forename: Suguna
authors.initials: S
authors.lastname: Rao
authors.affiliation: Department of Biochemistry, Indian Institute of Science, Bengaluru 560012, India.
authors.forename: Sathees C
authors.initials: SC
authors.lastname: Raghavan
authors.affiliation: Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysuru 570006, India. Electronic address: rangappaks@gmail.com.
authors.forename: Kanchugarakoppal S
authors.initials: KS
authors.lastname: Rangappa
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007938:Leukemia / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D053778:Thiazolidines
keywords: 4-Thiazolidinone; EAC; Reh; T3P; Tumor regression