Baravkar, S.B. and Wagh, M.A. and Paul, D. and Santra, M.K. and Sanjayan, G.J. (2018) Synthesis and anticancer activity of conformationally constrained Smac mimetics containing pseudo b turns. Tetrahedron Letters , 59. pp. 3473-3476.

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Abstract

Herein, we report synthesis and in vitro anticancer activity of conformationally constrained Smac mimetics containing reverse turn inducing motifs “Ant-Pro” and “sAnt-Pro”. The synthesis of Smac analogs with diverse hydrophobic groups at the C-terminus was carried out using solution phase peptide synthesis. The synthesis of Ant-Pro containing analogs 3a–j was carried out by ring opening of benzoxazinones 7a–c, whereas, their sulfonamide counterparts 4a–h were synthesized by using routine acid-amine coupling reaction. In vitro anticancer studies against breast cancer cell line MDA-MB-231 revealed that some of the new analogs had better anticancer activity than the standard AVPI Smac tetrapeptide.

Item Type:	Article
Depositing User:	Mr. Rameshwar Nema
Date Deposited:	10 Feb 2020 11:32
Last Modified:	10 Feb 2020 11:32
URI:	http://nccs.sciencecentral.in/id/eprint/595

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