New synthetic inhibitors of microtubule depolymerization.
A new class of borneol esters that might be considered as biological analogs of paclitaxel regarding their action on microtubules has been found. By structure-activity optimizations, compounds stabilizing microtubules much better than paclitaxel while showing a remarkably reduced cytotoxic activity were obtained. This dissoziation will open completely new therapeutic areas.
Klar
U
U
Research Laboratories of Schering AG, Berlin, Germany.
Graf
H
H
Schenk
O
O
Röhr
B
B
Schulz
H
H
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology; D001704:Biopolymers; D001892:Camphanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism*; D008958:Models, Molecular; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D000972:Antineoplastic Agents, Phytogenic; D001704:Biopolymers; D001892:Camphanes; C022871:isoborneol; D017239:Paclitaxel