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

Authors
SINGH SB ZINK DL LIESCH JM BALL RG GOETZ MA BOLESSA EA GIACOBBE RA SILVERMAN KC BILLS GF PELAEZ F CASCALES C GIBBS JB LINGHAM RB
Citation
Sb. Singh et al., PREUSSOMERINS AND DEOXYPREUSSOMERINS - NOVEL INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE, Journal of organic chemistry, 59(21), 1994, pp. 6296-6302
Citations number
37
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Journal of organic chemistry → ACNP
ISSN journal
00223263
Volume
59
Issue
21
Year of publication
1994
Pages
6296 - 6302
Database
ISI
SICI code
0022-3263(1994)59:21<6296:PAD-NI>2.0.ZU;2-9
Abstract
Farnesylation of Ras (p21) by farnesyl-protein transferase (FPTase) pr ecedes 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 a nd deoxypreussomerins from the extracts of a dung-inhabiting coelomyce tous fungus from Chaco Province, Argentina. Isolation, structure eluci dation, chemistry, and structure-activity relationships of the natural products and derivatives have been described.