PREUSSOMERINS AND DEOXYPREUSSOMERINS - NOVEL INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE

被引：85

作者：

SINGH, SB ^{[1
]}

ZINK, DL ^{[1
]}

LIESCH, JM ^{[1
]}

BALL, RG ^{[1
]}

GOETZ, MA ^{[1
]}

BOLESSA, EA ^{[1
]}

GIACOBBE, RA ^{[1
]}

SILVERMAN, KC ^{[1
]}

BILLS, GF ^{[1
]}

PELAEZ, F ^{[1
]}

CASCALES, C ^{[1
]}

GIBBS, JB ^{[1
]}

LINGHAM, RB ^{[1
]}

机构：

[1] MERCK SHARP & DOHME ESPANA,E-28027 MADRID,SPAIN

来源：

JOURNAL OF ORGANIC CHEMISTRY | 1994年 / 59卷 / 21期

关键词：

D O I：

10.1021/jo00100a035

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Farnesylation of Ras (p21) by farnesyl-protein transferase (FPTase) precedes association of Ras with the plasma membrane which is essential for Ras-mediated cell-transforming activity. Our continuing search for FPTase inhibitors led us to isolate a number of novel preussomerins and deoxypreussomerins from the extracts of a dung-inhabiting coelomycetous fungus from Chaco Province, Argentina. Isolation, structure elucidation, chemistry, and structure-activity relationships of the natural products and derivatives have been described.

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页码：6296 / 6302

页数：7

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