Northwestern University

Huiying Han

Gary E Schiltz

Atul D Jain

Sarki A Abdulkadir

Rama K Mishra

Javier Izquierdo-Ferrer

Disclosed are substituted heterocycle compounds including substituted pyrazoles, substituted pyrimidines, and substitute triazoles. The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC and may be utilized as therapeutics for treating cancer and cell proliferative disorders.

Substituted heterocycles as c-MYC targeting agents

Disclosed are proteolysis-targeting chimeric molecules (PROTACs) that induce degradation of c-MYC protein. The disclosed PROTACs typically include a first targeting moiety that binds to c-MYC (M) which may be derived from a substituted heterocycle that binds to c-MYC such as a substituted pyrazole. The first targeting moiety typically is linked via a bond or a linker (L) to a second targeting moiety that binds to an E3 ubiquitin ligase (M). As such, the disclosed PROTACS may be described as having a formula M-L-Mor M-L-M.

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Chicago, IL, United States of America

Huiying Han