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Synthesis of novel beta-lactone inhibitors of fatty acid synthase.

Abstract：

:Fatty acid synthase (FAS) is necessary for growth and survival of tumor cells and is a promising drug target for oncology. Here, we report on the syntheses and activity of novel inhibitors of the thioesterase domain of FAS. Using the structure of orlistat as a starting point, which contains a beta-lactone as the central pharmacophore, 28 novel congeners were synthesized and examined. Structural features such as the length of the alpha- and beta-alkyl chains, their chemical composition, and amino ester substitutions were altered and the resulting compounds explored for inhibitory activity toward the thioesterase domain of FAS. Nineteen congeners show improved potency for FAS in biochemical assays relative to orlistat. Three of that subset, including the natural product valilactone, also display an increased potency in inducing tumor cell death and improved solubility compared to orlistat. These findings support the idea that an orlistat congener can be optimized for use in a preclinical drug design and for clinical drug development.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Richardson RD,Ma G,Oyola Y,Zancanella M,Knowles LM,Cieplak P,Romo D,Smith JW

doi

10.1021/jm800321h

subject

Has Abstract

pub_date

2008-09-11 00:00:00

pages

5285-96

issue

17

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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