Abstract:In our efforts to identify molecules that selectively reduce the expression of BMI1, a stem cell gene, we discovered and characterized the first‐in‐class series of small molecules that modulate the expression of BMI1 protein in cancer cells. Structure‐activity and structure‐property relationships associated with this series were investigated through medicinal chemistry efforts. These studies revealed important structural features required for achieving anti‐tumor activity and acceptable pharmacokinetic propert… Show more
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