Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors

The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biological study of these compounds provided potent compounds 17a, 33b, 33c, 33d, and 33g with low nanomolar IC50s against PARP-1 enzyme.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-06, Vol.24 (12), p.2669-2673
Hauptverfasser:	Chen, Jianyang, Peng, Haixia, He, Jinxue, Huan, Xiajuan, Miao, Zehong, Yang, Chunhao
Format:	Artikel
Sprache:	eng
Schlagworte:	Antitumor Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Inhibitory Concentration 50 Isoquinolines - chemistry Isoquinolines - pharmacology Isoquinolinone-based tricycles Molecular Structure PARP-1 inhibitors Poly(ADP-ribose) Polymerase Inhibitors Poly(ADP-ribose) Polymerases - chemistry
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biological study of these compounds provided potent compounds 17a, 33b, 33c, 33d, and 33g with low nanomolar IC50s against PARP-1 enzyme.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.04.061