Gerard Charles Sanz

TL;DR: The heterogeneity of histological changes associated with antitumor effects suggested that R115777, and possibly farnesyl protein transferase inhibitors as a class, alter processes of transformation related to tumor-host interactions in addition to inhibiting tumor-cell proliferation.

TL;DR: In this article, the authors defined the novel compounds of formula (I), wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C?1-12?alkyl, Ar?1, Ar2C?1-, Ar2, Ar1, C1-6alkyl-oxy, Ar 2, Ar 3, Ar 4, 4,4-dimethyl-oxazolyl, C 1-6-alkyloxy, C 2-6kenyl, Halo, cyano, amino,

TL;DR: The data characterize R115866 as a potent, orally active inhibitor of RA metabolism, capable of enhancing RA levels and displaying retinoidal actions, supporting the idea that the actions of R 115866 result from increased availability of endogenous RA and improved RAR triggering.

TL;DR: In this paper, the authors defined a class of pharmaceutically acceptable acid additions salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; -A- is a bivalent radical of formula; R?1 and R2? each independently are hydrogen, hydroxy, halo, cyano, C?1-6?alkyl, C 1-6alkyloxy, Ar-oxy, C1- 6alkylthio, mono- or di(C 1- 6

TL;DR: In conclusion, R116010 is a highly potent and selective inhibitor of all-trans-retinoic acid metabolism, which is able to enhance the biological activity of all the transmissible acid, thereby exhibiting antitumour activity.