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Synthesis and structure-activity relationships of new second-generation taxoids
1Department of Chemistry, State University of New York at Stony Brook, 11794-3400, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 2000
Abstract:
A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as "advanced second generation taxoids".