Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly (adenosine-diphosphate-ribose) polymerase-1 (PARP-1) inhibitor

…, MF Mahon, MD Lloyd, MD Threadgill

Index: Lord, Anna-Marie; Mahon, Mary F.; Lloyd, Matthew D.; Threadgill, Michael D. Journal of Medicinal Chemistry, 2009 , vol. 52, # 3 p. 868 - 877

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Citation Number: 51

Abstract

Poly (ADP-ribose) polymerase-1 is an important target enzyme in drug design; inhibitors have a wide variety of therapeutic activities. A series of quinoline-8-carboxamides was designed to maintain the required pharmacophore conformation through an intramolecular hydrogen bond. 3-Substituted quinoline-8-carboxamides were synthesized by Pd-catalyzed couplings (Suzuki, Sonogashira, Stille) to 3-iodoquinoline-8-carboxamide, an efficient ...

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