William Marsh Rice University

Stephan Rigol

Kyriacos Costa Nicolaou

Kiran Kumar Pulukuri

Dionisios Vourloumis

Rohan Diliprao Erande

Gabriel Bellavance

Marek Buchman

In one aspect, the present disclosure provides disorazole analogs of the formula: Formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. 

Synthesis of disorazoles and analogs thereof as potent anticancer agents

In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. 

Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith

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Houston, TX, United States of America

Stephan Rigol