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Cancer Therapy

Trans-3,4'-bispyridinylethylenes proposed as potent inhibitors for cancer therapy

Published in Cancer Weekly, April 17th, 2006

Trans-3,4'-bispyridinylethylenes were proposed as potent inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer.

"A novel series of Akt/PKB inhibitors derived from a screening lead (1) has been prepared. The novel trans-3,4'-bispyridinylethylenes described herein are potent inhibitors of Akt/PKB with IC50 values in the low double-digit nanomolar range against Akt1," scientists in the United States reported.

"Compound 2q shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor to modest selectivity against closely related kinases in the AGC and CMGC families. The...

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