William Marsh Rice University

Rohan Diliprao Erande

Kyriacos Costa Nicolaou

Dionisios Vourloumis

Debashis Mandal

Kiran Kumar Pulukuri

Stephan Rigol

Jun Yin

Phillipp Klahn

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

In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein R, R, R, R, X, X, X, and Aare 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. 

Desacetoxytubulysin H and analogs thereof

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Houston, TX, United States of America

Rohan Diliprao Erande