Antimicrotubular effect of calvatic acid and of some related compounds.
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 vitro. 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.
Gadoni
E
E
Department of Experimental Medicine and Oncology, Section of General Pathology, University of Turin, Corso Raffaello 30, 10125 Torino, Italy.
Gabriel
L
L
Olivero
A
A
Bocca
C
C
Miglietta
A
A
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001391:Azo Compounds / Q000494:pharmacology*; D001565:Benzoates / Q000494:pharmacology; D002417:Cattle; D004305:Dose-Response Relationship, Drug; D066298:In Vitro Techniques; D008868:Microtubule Proteins / Q000737:chemistry*; D009570:Nitriles / Q000494:pharmacology; D011108:Polymers; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D001391:Azo Compounds; D001565:Benzoates; D008868:Microtubule Proteins; D009570:Nitriles; D011108:Polymers; C010057:calvatic acid