The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Aug. 17, 2004

Filed:

Apr. 24, 2003
Applicant:
Inventors:

George R. Pettit, Paradise Valley, AZ (US);

Matthew P. Grealish, San Diego, CA (US);

Assignee:

Arizona Board of Regents, Tempe, AZ (US);

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07C 4/976 ; A01N 3/500 ;
U.S. Cl.
CPC ...
C07C 4/976 ; A01N 3/500 ;
Abstract

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.


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