SYNTHESIS AND EVALUATION OF PYRAZOLO [3,4-B]QUINOLINE RIBOFURANOSIDESAND THEIR DERIVATIVES AS INHIBITORS OF ONCOGENIC RAS

Authors
WOLIN R WANG D KELLY J AFONSO A JAMES L KIRSCHMEIER P MCPHAIL AT
Citation
R. Wolin et al., SYNTHESIS AND EVALUATION OF PYRAZOLO [3,4-B]QUINOLINE RIBOFURANOSIDESAND THEIR DERIVATIVES AS INHIBITORS OF ONCOGENIC RAS, Bioorganic & medicinal chemistry letters, 6(2), 1996, pp. 195-200
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
2
Year of publication
1996
Pages
195 - 200
Database
ISI
SICI code
0960-894X(1996)6:2<195:SAEOP[>2.0.ZU;2-H
Abstract
A series of pyrazolo[3,4-b]quinoline ribofuranosides were prepared usi ng the glycosylation methodology of Vorbruggen. Oxidative cleavage of the ribose moiety in 6 furnished the dialdehyde intermediate 36, which cyclizes upon reductive amination providing the morpholino compound 3 7. Derivatives from both the ribose and morpholino series were evaluat ed for their ability to inhibit the nucleotide exchange process of onc ogenic Ras.(1a)