Design, stereoselective synthesis, and biological evaluation of novel tri-cyclic compounds as inhibitor of apoptosis proteins (IAP) antagonists
M Asano, K Hashimoto, B Saito, Z Shiokawa… - Bioorganic & medicinal …, 2013 - Elsevier
We recently reported the discovery of octahydropyrrolo [1, 2-a] pyrazine A as a lead
compound for an inhibitor of apoptosis proteins (IAP) antagonist. To develop IAP antagonists
with favorable PK profiles, we designed novel tri-cyclic compounds, octahydro-1 H-
cyclopropa [4, 5] pyrrolo [1, 2-a] pyrazines 1 and 2 based on co-crystal structural analysis of
A with cellular IAP-1 (cIAP-1). The additional cyclopropane moiety was used to block the
predicted metabolic site of compound A without detriment to the binding affinity for cIAP …
compound for an inhibitor of apoptosis proteins (IAP) antagonist. To develop IAP antagonists
with favorable PK profiles, we designed novel tri-cyclic compounds, octahydro-1 H-
cyclopropa [4, 5] pyrrolo [1, 2-a] pyrazines 1 and 2 based on co-crystal structural analysis of
A with cellular IAP-1 (cIAP-1). The additional cyclopropane moiety was used to block the
predicted metabolic site of compound A without detriment to the binding affinity for cIAP …
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