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  • Title: Synthesis and binding to tubulin of colchicine spin probes.
    Author: Sharma PN, Brossi A, Silverton JV, Chignell CF.
    Journal: J Med Chem; 1984 Dec; 27(12):1729-33. PubMed ID: 6094813.
    Abstract:
    Spin probes of deacetylcholchicine (1), 4-(hydroxymethyl)colchicine (2), and colchifoline (3) have been synthesized to study the binding site for colchicine on tubulin. Acylation of 1-3 with (+/-)-2,2,5,5-tetramethyl-1-pyrrolidinyloxy-3-carboxylic acid (4) afforded diastereomeric mixtures of the esters 5-8 and the amides 9 and 10. Pure diastereomers of 3 were synthesized with 4a and 4b, which inhibited the binding of colchicine by 60%. In the presence of calf brain microtubular protein, the colchifoline spin labels underwent reduction of the nitroxide group, which precluded their use to study the topography of the colchicine binding site.
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