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Synthesis and structure-activity relationships of new second-generation taxoids |
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| Authors: | Ojima I Wang T Miller M L Lin S Borella C P Geng X Pera P Bernacki R J |
| Affiliation: | a Department of Chemistry, State University of New York at Stony Brook, Stony Brook, NY 11794-3400, U.S.A. b Department of Experimental Therapeutics, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, U.S.A. |
| Abstract: | A series of second-generation taxoids bearing a substitutent 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“. |
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