Antimicrotubular effect of calvatic acid and of some related compounds

✍ Scribed by Elena Gadoni; Ludovica Gabriel; Antonella Olivero; Claudia Bocca; Antonella Miglietta

• Book ID: 102788370
• Publisher: John Wiley and Sons
• Year: 1995
• Tongue: English
• Weight: 628 KB
• Volume: 13
• Category: Article
• ISSN: 0263-6484
• DOI: 10.1002/cbf.290130403

✦ Synopsis

A structure-activity relationship has been established between calvatic acid and some related synthetic compounds, and their ability to inhibit GTP-induced microtubular protein polymerization in vifro. These compounds were effective in a dose-and a time-dependent manner. The most active drug was the p-chloro substituted compound, which showed its inhibitory activity without any preincubation period, which the others needed. Since if cysteine was present, polymerization was no longer affected, an involvement of titratable -SH groups of tubulin could be suggested. In contrast, taxol-induced polymerization was only slightly inhibited by these compounds, and colchicine-binding activity was not generally impaired.