C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 49/76 (2006.01) A61K 31/38 (2006.01) A61K 31/66 (2006.01) C07C 45/29 (2006.01) C07C 45/46 (2006.01) C07C 45/67 (2006.01) C07C 49/786 (2006.01) C07C 49/82 (2006.01) C07C 49/825 (2006.01) C07C 49/84 (2006.01) C07F 9/12 (2006.01)
Patent
CA 2407672
The benzophenone derivative of combretastatin A-1, designated "hydroxyphenstatin", was synthesized by compiling a protected bromobenzene and a benzaldehyde to form a benzhydrol which was subsequently oxidized to the ketone. Hydroxyphenstatin was converted to a sodium phosphate prodrug by dibenzyl phosphite phosphorylation and subsequent benzyl cleavage: Hydroxyphenstatin and the prodrugs thereof were found to be a potent inhibitor of tubulin polymerization and to demonstrate surprisingly effective antineoplastic activity against a series of human cancer cells and murine P388 lymphocytic leukemia cells.
Pour produire par synthèse le dérivé benzophénone de combretastatine A-1 appelé "hydroxyphenstatine", on a couplé un bromobenzène protégé et un benzaldéhyde pour former un benzhydrol qui a ensuite été oxydé en cétone. L'hydroxyphenstatine a été transformée en un promédicament au phosphate de sodium par une phosphorylation au dibenzyl phosphite suivie d'un clivage du benzyle. On a remarqué que l'hydroxyphenstatine et les promédicaments issus de cette dernière sont un inhibiteur puissant de la polymérisation de la tubuline et présentent une activité antinéoplastique étonnamment efficace contre une série de cellules cancéreuses humaines et de cellules leucémiques lymphocytiques P388 de souris.
Grealish Matthew P.
Pettit George R.
Acti Ng For And On Behalf Of Arizona State University Arizona Board Of Regents A. Body Corporate Of The State Of Arizo
Borden Ladner Gervais Llp
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