C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 209/12 (2006.01) A61K 31/404 (2006.01) A61P 43/00 (2006.01) C07F 9/24 (2006.01) C07F 9/572 (2006.01)
Patent
CA 2383988
Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting and destruction chemotherapeutic agents or to have anti-angiogenesis activity resulting in the selective prevention and/or destruction of tumor cell vasculature.
L'invention concerne des ligands indoliques substitués par triméthoxyphényle, qui présentent une cytotoxicité impressionnante ainsi qu'une remarquable capacité d'inhiber la polymérisation de la tubuline. Ces composés, ainsi que les dérivés qui leur sont associés, sont d'excellents candidats cliniques pour le traitement du cancer chez l'homme. De plus, certains de ces ligands, utilisés comme promédicaments, peuvent être des agents chimiothérapeutiques de ciblage et de destruction vasculaires sélectifs d'une tumeur, ou posséder une action anti-angiogénique donnant lieu à la prévention et/ou destruction sélective du système vasculaire d'une cellule tumorale.
Del Pilar Mejia Maria
Pinney Kevin G.
Wang Feng
Baylor University
Ridout & Maybee Llp
LandOfFree
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