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ChemInform Abstract: Novel Tricyclic Aminoacetyl and Sulfonamide Inhibitors of RAS Farnesyl Protein Transferase.

✍ Scribed by F. G. NJOROGE; B. VIBULBHAN; C. S. ALVAREZ; W. R. BISHOP; J. PETRIN; R. J. DOLL; V. GIRIJAVALLABHAN; A. K. GANGULY

Publisher
John Wiley and Sons
Year
2010
Weight
30 KB
Volume
28
Category
Article
ISSN
0931-7597

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✦ Synopsis

Novel Tricyclic Aminoacetyl and Sulfonamide Inhibitors of RAS Farnesyl Protein Transferase.

-It is shown that derivatization of the amino group with a phthaloyl moiety increases inhibitory activity of the title compounds, cf. (IIIc) and (IIId). The potent inhibitors (III) and (V) are non-peptidic, do not contain sulfhydryl groups, properties that render them pharmacokinetically more stable. -(NJOROGE, F.

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