The
transcriptional
repressor BCL6 is an oncogenic driver found
to be deregulated in lymphoid malignancies. Herein, we report the
optimization of our previously reported benzimidazolone molecular
glue-type degrader
CCT369260
to
CCT373566
, a highly potent probe suitable for sustained depletion of BCL6
in vivo
. We observed a sharp degradation SAR, where subtle
structural changes conveyed the ability to induce degradation of BCL6.
CCT373566
showed modest
in vivo
efficacy
in a lymphoma xenograft mouse model following oral dosing.
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