Baylor University

Oxigene, Inc.

Mallinath Hadimani

Kevin G Pinney

David J Chaplin

Zhi Chen

Klaus Edvardsen

Joseph Anthony Prezioso

Vani P Mocharla

James Michael Dorsey

Charles M Garner

Usha Ghatak, Legal Representative

Usha R Ghatak, Legal Representative

Jimmy Kessler

Feng Wang

Raymond Kessler

A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Tubulin binding ligands and corresponding prodrug constructs

Tubulin binding agents and corresponding prodrug constructs

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 prodrugs, 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.

Indole-containing and combretastatin-related anti-mitotic and anti-tubulin polymerization agents

Growing community of inventors

Waco, TX, United States of America

Mallinath Hadimani