Zaragozic acids D and D2: potent inhibitors of squalene synthase and of Ras farnesyl-protein transferase

  • J Nat Prod. 1993 Nov;56(11):1923-9. doi: 10.1021/np50101a009.
C Dufresne  1 ,  K E Wilson ,  S B Singh ,  D L Zink ,  J D Bergstrom ,  D Rew ,  J D Polishook ,  M Meinz ,  L Huang ,  K C Silverman
Affiliations
  • 1. Merck Research Laboratories, Rahway, New Jersey.
PMID: 8289063 DOI: 10.1021/np50101a009
Abstract

Two new zaragozic acids, D and D2, have been isolated from the keratinophilic fungus Amauroascus niger. Zaragozic acids D [4] and D2 [5] are related to the previously described zaragozic acids A [1], B [2], and C [3] and are potent inhibitors of squalene synthase. Furthermore, all the zaragozic acids (A, B, C, D, and D2) are also active against Farnesyl Transferase. Zaragozic acids D and D2 inhibit Farnesyl Transferase with IC50 values of 100 nM, while zaragozic acids A and B are less potent.

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