Highlights d KI-ARv-03 reduces AR protein levels and AR-driven transcription d KI-ARv-03 is deduced to be a potent, ultraselective inhibitor of CDK9 d Optimization led to the orally bioavailable and selective CDK9 inhibitor KB-0742 d KB-0742 displays potent anti-tumor activity in cancer models in vitro and in vivo
Brønsted acid promotes internal cinnamylations of tryptophan to form structurally complex pyrroloindolines within unique collections of ansa-bridged composite macrocycles.
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