C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 271/22 (2006.01) C07C 69/78 (2006.01) C07C 233/58 (2006.01) C07C 233/87 (2006.01) C07C 235/14 (2006.01) C07D 493/04 (2006.01)
Patent
CA 2379676
A method for designing paclitaxel alternative compounds which stabilize the tubulin polymerization process has been found. These compounds in solution possess steric conformational properties of natural paclitaxel and are capable of binding to the tubulin protein at the same site where paclitaxel is known to bind. The compounds of the present invention stabilize tubulin polymerization in a way that is mechanistically equivalent to activity mechanism of paclitaxel. The compounds of the present invention have increased solubility, simpler synthesis, and the possibility for specificity and optimization due to the combinatorial reactions over natural paclitaxel.
L'invention concerne un procédé permettant la conception de composés de remplacement du paclitaxel, qui stabilisent le processus de polymérisation de la tubuline. Ces composés en solution présentent les caractéristiques de conformation stérique du paclitaxel naturel et sont capables de se fixer à la protéine de tubuline au même site de liaison que le paclitaxel. Ces composés stabilisent la polymérisation de la tubuline par un mécanisme correspondant au mécanisme d'activité du paclitaxel. Comparés au paclitaxel naturel, ces composés présentent une solubilité accrue, sont plus faciles à synthétiser et offrent des possibilités de réactions combinatoires permettant une spécificité et d'une optimisation.
Arad Dorit
Bollon Arthur P.
Poland Bradley W.
Young David C.
Arad Dorit
Bollon Arthur P.
Cytoclonal Pharmaceutics Inc.
Kirby Eades Gale Baker
Poland Bradley W.
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