216086-64-5Relevant articles and documents
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase
Augeri, David J.,Janowick, Dave,Kalvin, Douglas,Sullivan, Gerry,Larsen, John,Dickman, Daniel,Ding, Hong,Cohen, Jerry,Lee, Jang,Warner, Robert,Kovar, Peter,Cherian, Sajeev,Saeed, Badr,Zhang, Haichao,Tahir, Steve,Ng, Shi-Chung,Sham, Hing,Rosenberg, Saul H.
, p. 1069 - 1074 (1999)
Potent and orally bioavailable nonthiol-containing inhibitors of protein farnesyltransferase are described. Oral bioavailability was achieved by replacement of the pyridyl ether moiety of 1 with a 2-substituted furan ether to give 4. Potency was regained with 2,5-disubstituted furan ethers while maintaining the bioavailability inherent in 4. p-Chlorophenylfuran ether 24 is 0.7 nM in vitro (FTase) and is 32% bioavailable in the mouse, 30% bioavailable in rats, and 21% bioavailable in dogs.
