Synthesis and in vivo anticancer and antiangiogenic effects of novel thioxothiazolidin-4-one derivatives against transplantable mouse tumor

Chandrappa, S. and Chandru, H. and Sharada, A. C. and Vinaya, K. and Ananda Kumar, C. S. and Thimmegowda, N. R. and Nagegowda, P. and Karuna Kumar, M. and Rangappa, K. S. (2010) Synthesis and in vivo anticancer and antiangiogenic effects of novel thioxothiazolidin-4-one derivatives against transplantable mouse tumor. Medicinal Chemistry Research, 19 (3). pp. 236-249. ISSN 1554-8120

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Abstract

A series of novel thioxothiazolidin-4-one derivatives 5(a--g) were synthesized by the coupling of different amines containing aliphatic, substituted aromatic, and heterocyclic moieties, such as oxadiazol, pyrazole, isoxazole, and piperazine with 2-(5-(4-chlorophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)acetic acid. All compounds were characterized by 1H NMR, LCMS, FTIR and elemental analysis. In this study, we investigated the possibility that these novel thioxothiazolidin-4-one derivatives 5(a--g) inhibits tumor growth and tumor induced angiogenesis using mouse Ehrlich Ascites Tumor (EAT) as a model system. Our results demonstrated that the compounds significantly reduced ascites tumor volume, cell number, and increased the life span of EAT-bearing mice. In addition, the compounds manifested strong antiangiogenic effects and suppressed tumor induced endothelial proliferation in the mice peritoneum. From our findings, it is noted that the derivatives 5(a--e) may be possible candidates for anticancer therapy with the ability to inhibit tumor angiogenesis and tumor cell proliferation.

Item Type:	Article
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	LA manjunath user
Date Deposited:	15 Jul 2019 10:05
Last Modified:	17 Jun 2022 11:08
URI:	http://eprints.uni-mysore.ac.in/id/eprint/5203

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