title: Synthesis and structure-activity relationships of new second-generation taxoids.
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".
authors.affiliation: Department of Chemistry, State University of New York at Stony Brook, 11794-3400, USA.
authors.forename: I
authors.initials: I
authors.lastname: Ojima
authors.forename: T
authors.initials: T
authors.lastname: Wang
authors.forename: M L
authors.initials: ML
authors.lastname: Miller
authors.forename: S
authors.initials: S
authors.lastname: Lin
authors.forename: C P
authors.initials: CP
authors.lastname: Borella
authors.forename: X
authors.initials: X
authors.lastname: Geng
authors.forename: P
authors.initials: P
authors.lastname: Pera
authors.forename: R J
authors.initials: RJ
authors.lastname: Bernacki
mesh_terms: D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D017239:Paclitaxel / Q000031:analogs & derivatives; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D017239:Paclitaxel