Synthesis of a stable and orally bioavailable englerin analogue. Issue 11 (1st June 2016)

• Record Type: Journal Article
• Authors: Fash, David M.; Peer, Cody J.; Li, Zhenwu; Talisman, Ian J.; Hayavi, Sima; Sulzmaier, Florian J.; Ramos, Joe W.; Sourbier, Carole; Neckers, Leonard; Figg, W. Douglas; Beutler, John A.; Chain, William J.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 11(2016)
• Page Start: 2641
• Page End: 2644
• Publication Date: 2016-06-01
• Subjects: Englerins -- Cancer -- Bioavailability -- Sesquiterpenes; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.04.016
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Synthesis of analogues of englerin A with a reduced propensity for hydrolysis of the glycolate moiety led to a compound which possessed the renal cancer cell selectivity of the parent and was orally bioavailable in mice.