Design and Synthesis of Poly(ADP-ribose) polymerase Inhibitors: Impact of Adenosine Pocket-Binding Motif Appendage to the 3-Oxo-2,3-dihydrobenzofuran-7-carboxamide on Potency and Selectivity

Poly(ADP-ribose) polymerase (PARP) inhibitors are a class of anticancer drugs that block the catalytic activity of PARP proteins. Optimization of our lead compound 1 ((Z)-2-benzylidene-3-oxo-2,3-dihydrobenzofuran-7-carboxamide; PARP-1 IC(50) = 434 nM) led to a tetrazolyl analogue (51, IC(50) = 35 nM...

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Publicado no:J Med Chem
Main Authors: Velagapudi, Uday Kiran, Langelier, Marie-France, Delgado-Martin, Cristina, Diolaiti, Morgan E., Bakker, Sietske, Ashworth, Alan, Patel, Bhargav A., Shao, Xuwei, Pascal, John M., Talele, Tanaji T.
Formato: Artigo
Idioma:Inglês
Publicado em: 2019
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7378964/
https://ncbi.nlm.nih.gov/pubmed/31042381
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01709
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