Altering Nitrogen Heterocycles of AZD2461 Affords High Affinity Poly(ADP-ribose) Polymerase-1 Inhibitors with Decreased P-Glycoprotein Interactions

[Image: see text] Poly(ADP-ribose) polymerase inhibitors (PARPi) are targeted therapeutics with enhanced selectivity and cytotoxicity in BRCA1/2 mutant cancer cells. AZD2461, a congener of FDA approved olaparib, is a potent PARPi with high affinity for PARP-1 and nonsubstrate for P-glycoprotein (P-g...

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Detalles Bibliográficos
Autores principales: Reilly, Sean W., Puentes, Laura N., Hsieh, Chia-Ju, Makvandi, Mehran, Mach, Robert H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6120739/
https://www.ncbi.nlm.nih.gov/pubmed/30198004
http://dx.doi.org/10.1021/acsomega.8b00896

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