On the introduction of a trifluoromethyl substituent in the epothilone setting: chemical issues related to ring forming olefin metathesis and earliest biological findings.
The disclosure herein describes the synthesis of 10,11-dehydro-13,14-desoxy-27-trifluoro-[17]epothilone B via a stereoselective ring-closing metathesis and provides early biological evaluation data pertinent to this compound. [reaction: see text]
Rivkin
Alexey
A
Laboratories for Bioorganic Chemistry, Sloan-Kettering Institute for Cancer Research, 1275 York Avenue, New York, NY 10021, USA.
Biswas
Kaustav
K
Chou
Ting-Chao
TC
Danishefsky
Samuel J
SJ
D000475:Alkenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D002455:Cell Division / Q000187:drug effects; D006801:Humans; D007202:Indicators and Reagents; D015394:Molecular Structure; D014407:Tumor Cells, Cultured
D000475:Alkenes; D007202:Indicators and Reagents