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Synthesis of ether analogues derived from HUN-7293 and evaluation as inhibitors of VCAM-1 expression.

Schreiner, Erwin and Kern, Michael and Steck, Andrea and Foster, Carolyn-Ann (2004) Synthesis of ether analogues derived from HUN-7293 and evaluation as inhibitors of VCAM-1 expression. Bioorganic & Medicinal Chemistry Letters, 14 (19). pp. 5003-5006. ISSN 0960-894X

Abstract

The cyclic depsipeptide HUN-7293 (1) and its D-lactate analogue 2 are highly potent inhibitors of inducible cell adhesion molecule expression. We report the synthesis of ether analogues varying in stereochemistry and side chain at the former hydroxyl acid position by employing a 'cut and paste chemistry' methodology starting from 1. As an additional fruit of this synthetic effort, a cyclodepsipeptide featuring a tertiary amine instead of a tertiary amide between PrLEU and MALA was obtained. Results on the inhibitory profile of these compounds in assays of VCAM-1 and ICAM-1 protein expression are discussed.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: HUN-7293; VCAM-1 expression; Ether analogues
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Date Deposited: 14 Dec 2009 13:55
Last Modified: 14 Dec 2009 13:55
URI: https://oak.novartis.com/id/eprint/731

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