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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...
Guardat en:
| Publicat a: | J Med Chem |
|---|---|
| Autors principals: | , , , , , , , , , |
| Format: | Artigo |
| Idioma: | Inglês |
| Publicat: |
2019
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| Matèries: | |
| Accés en línia: | 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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