Novel thiodiketopiperazine fungal metabolites as epidermal growth factor receptor antagonists

Tetrahedron Letters
1997.0

Abstract

The organic extract of the fermentation broth of an unidentified fungus was found to contain three epidermal growth factor (EGF) receptor antagonists: SCH 64874 (1), SCH 64875 (2), SCH 64877 (3). These compounds belong to a family of thiodiketopiperazine derivatives and are esters of an eight carbon aliphatic acid, 2,4-dimethyl-3- hydroxyhexanoic acid and a thiodiketopiperazine, aranotin, They exhibited potent EGF receptor antagonist activity. The ICs0 in EGF receptor assays for compounds l, 2 and 3 are 1.0, 1.0 and 1.25 gg/ml, respectively. © 1997, Elsevier Science Ltd. All rights reserved.

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