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
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.
引用
收藏
页码:6296 / 6302
页数:7
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