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Synthesis of a [ 3 H]‐labelled derivative of the microtubular poison taxol
Author(s) -
Chenu J.,
Takoudju M.,
Wright M.,
Senilh V.,
Guénard D.
Publication year - 1987
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580241012
Subject(s) - chemistry , acetylation , acetic anhydride , microtubule , derivative (finance) , tubulin , radiolysis , stereochemistry , radiochemistry , organic chemistry , biochemistry , catalysis , aqueous solution , biology , financial economics , economics , gene , microbiology and biotechnology
A labelled derivative of the microtubule poison taxol has been developed on acetylation of the 7‐OH function of taxol with [ 3 H] acetic anhydride. The [ 3 H] 7‐acetyl taxol synthesized was chemically and radiochemically pure and has not undergone radiolysis during 1.5 years. This compound was also stable in the presence of microtubule proteins. The ID 50 of 7‐acetyl taxol for stabilization of microtubules was two times the ID 50 of taxol. Hence it can be used as a probe for biological studies. The acetylation of the hydroxyl group at position C‐7 is a general method applicable to other taxol derivatives as starting compounds.