Synthesis of novel β-lactone inhibitors of fatty acid synthase

RD Richardson, G Ma, Y Oyola…

Index: Ma, Gil; Zancanella, Manuel; Oyola, Yatsandra; Richardson, Robyn D.; Smith, Jeffrey W.; Romo, Daniel Organic Letters, 2006 , vol. 8, # 20 p. 4497 - 4500

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Citation Number: 45

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 β-lactone as the central pharmacophore, 28 novel congeners were synthesized and examined. Structural features such as the length of the α-and β-alkyl ...

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