Synthesis and biological activity of macrocyclic taxane analogues.
A series of paclitaxel analogues possessing a macrocyclic structure between the 7 and 10 positions has been prepared. These compounds possess in vitro activity against a paclitaxel resistant cell line and have in vivo activity comparable to paclitaxel.
Tarrant
James G
JG
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5100, Wallingford, CT 06492-7660, USA. jim_tarrant@nrgn.com
Cook
Donald
D
Fairchild
Craig
C
Kadow
John F
JF
Long
Byron H
BH
Rose
William C
WC
Vyas
Dolatrai
D
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D019008:Drug Resistance, Neoplasm; D006801:Humans; D020128:Inhibitory Concentration 50; D008175:Lung Neoplasms / Q000188:drug therapy; D047028:Macrocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy; D017239:Paclitaxel / Q000031:analogs & derivatives*; D013329:Structure-Activity Relationship; D043823:Taxoids / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D050257:Tubulin Modulators
D000970:Antineoplastic Agents; D047028:Macrocyclic Compounds; D043823:Taxoids; D050257:Tubulin Modulators; D017239:Paclitaxel