Antiproliferative and tumor inhibitory studies of 2,3 disubstituted 4-thiazolidinone derivatives

• Published in: Bioorganic & medicinal chemistry letters Vol. 25; no. 17; pp. 3616 - 3620
• Main Authors: Sharath Kumar, Kothanahally S., Hanumappa, Ananda, Vetrivel, Maruthai, Hegde, Mahesh, Girish, Yarabhally R., Byregowda, Thinnali R., Rao, Suguna, Raghavan, Sathees C., Rangappa, Kanchugarakoppal S.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.09.2015
• Subjects: 4-Thiazolidinone; Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Cell Line, Tumor; Cell Proliferation - drug effects; Drug Design; Drug Screening Assays, Antitumor; EAC; Humans; Leukemia - drug therapy; Leukemia - pathology; Mice; Neoplasms - drug therapy; Neoplasms - pathology; Reh; Structure-Activity Relationship; T3P; Thiazolidines - chemical synthesis; Thiazolidines - chemistry; Thiazolidines - pharmacology; Thiazolidines - therapeutic use; Tumor regression; T3P; Reh; 4-Thiazolidinone; EAC; Tumor regression
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2015.06.069

[Display omitted] 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 13.5μM, 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.