title: Synthesis and biological evaluation of C-3'NH/C-10 and C-2/C-10 modified paclitaxel analogues.
abstract: Concurrent modifications on the C-3'NH/C-10, and C-2/C-10 positions on paclitaxel were carried out as a way of investigating possible synergistic effects. The biological activities of these analogues were evaluated in both a microtubule assembly assay and human ovarian cancer (A2780) and prostate cancer (PC3) cytotoxicity assay. In some cases the doubly modified analogues were more active than would have been predicted based on the activity of the singly modified analogues, indicating probable synergistic effects.
authors.affiliation: Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA.
authors.forename: Erkan
authors.initials: E
authors.lastname: Baloglu
authors.forename: Jeannine M
authors.initials: JM
authors.lastname: Hoch
authors.forename: Sabarni K
authors.initials: SK
authors.lastname: Chatterjee
authors.forename: Rudravajhala
authors.initials: R
authors.lastname: Ravindra
authors.forename: Susan
authors.initials: S
authors.lastname: Bane
authors.forename: David G I
authors.initials: DG
authors.lastname: Kingston
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000096:biosynthesis; D014407:Tumor Cells, Cultured
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D007202:Indicators and Reagents; D014404:Tubulin; D017239:Paclitaxel