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Aldol derivatives of Thioxoimidazolidinones as potential anti-prostate cancer agents

Publication Type : Journal Article

Publisher : Elsevier

Source : European Journal of Medicinal Chemistry, 2011

Url :

Campus : Amritapuri

School : School of Biotechnology

Verified : No

Year : 2011

Abstract : The paper discusses the synthesis and stereochemical aspects of the anti aldol products, 3-(substituted phenyl)-5-[(substituted phenyl) hydroxy methyl]-5-methyl-4-oxo-2-thioxoimidazolidines. The stereochemistry observed in the aldol reactions with benzaldehydes was explained by transition state model of the endocyclic (E)-enolate formed from the rigid 4-oxo-2-thioxoimidazolidine skeleton. Proton NMR and ROESY spectral analyses were carried out to identify the syn and anti conformations of the aldol diastereomers. Configurations of the enantiomers of the representative anti aldol product 3-(4-chlorophenyl)-5-[(4-chlorophenyl) hydroxy methyl]-5-methyl-4-oxo-2-thioxoimidazolidine was determined by single crystal XRD studies. The compounds were screened in vitro against prostate cancer cell lines, PC-3 and LNCaP and the most potent derivatives were identified.

Cite this Research Publication : Gopal L. Khatik, Jamine Kaur, Varun Kumar, Kulbushan Tikoo, Venugopalan P. and Vipin A. Nair, "Aldol derivatives of Thioxoimidazolidinones as potential anti-prostate cancer agents", European Journal of Medicinal Chemistry 2011, 46, 3291-3301

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