Synthesis of metabolically blocked paclitaxel analogues.
The stereospecific syntheses of the metabolically blocked 6-alpha-F, Cl, Br paclitaxel, and 6-alpha-F-10-acetyldocetaxel are described and in vitro and in vivo activity is presented.
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA. mark.wittman@bms.com
M D
MD
Wittman
T J
TJ
Altstadt
C
C
Fairchild
S
S
Hansel
K
K
Johnston
J F
JF
Kadow
B H
BH
Long
W C
WC
Rose
D M
DM
Vyas
M J
MJ
Wu
M E
ME
Zoeckler
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D004355:Drug Stability; D006801:Humans; D020128:Inhibitory Concentration 50; D017239:Paclitaxel / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D043823:Taxoids; D014407:Tumor Cells, Cultured
C429407:6-fluoro-10-acetyldocetaxel; D000972:Antineoplastic Agents, Phytogenic; D043823:Taxoids; D017239:Paclitaxel