Design, synthesis, and bioactivity of simplified paclitaxel analogs based on the T-Taxol bioactive conformation.
A strategy for the design and synthesis of simplified paclitaxel analogs based on the T-Taxol conformation is presented. The resulting compounds have both cytotoxic and tubulin polymerization activities, although less so than those of paclitaxel itself.
Ganesh
Thota
T
Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA.
Norris
Andrew
A
Sharma
Shubhada
S
Bane
Susan
S
Alcaraz
Ana A
AA
Snyder
James P
JP
Kingston
David G I
DG
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D003198:Computer Simulation; D004121:Dimethyl Sulfoxide / Q000737:chemistry; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008968:Molecular Conformation; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D012995:Solubility; D014404:Tubulin / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D014404:Tubulin; D017239:Paclitaxel; D004121:Dimethyl Sulfoxide