1052115-52-2Relevant academic research and scientific papers
Design, synthesis and evaluation of phthalazinone thiohydantoin-based derivative as potent PARP-1 inhibitors
Zhong, Yi,Meng, Ying,Xu, Xi,Zhao, Lulu,Li,You, Qidong,Bian, Jinlei
, (2019)
Two new series of compounds were designed and synthesized as potent PARP-1 inhibitors. These compounds were evaluated for PARP-1 enzyme and cellular inhibitory activities. All efforts lead to the identification of 9k (named as LG-12) with efficient potency both for PARP-1 and BRCA1 deficient MDA-MB-436 cells. Additionally, the novel PARP-1 inhibitor LG-12 is an efficient chemosensitizer, which could potentiate the anti-cancer effect of TMZ. Our data presented herein provide a comprehensive preclinical in vitro evaluation of the potential therapeutic efficacy and potency of chemotherapeutic agent-PARP-1 inhibitor combinations for LG-12. The combined results indicated that LG-12 could be a promising candidate for further study.
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent
Zhu, Gui-Dong,Gandhi, Viraj B.,Gong, Jianchun,Thomas, Sheela,Luo, Yan,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Johnson, Eric F.,Frost, David,Donawho, Cherrie,Jarvis, Ken,Bouska, Jennifer,Marsh, Kennan C.,Rosenberg, Saul H.,Giranda, Vincent L.,Penning, Thomas D.
scheme or table, p. 3955 - 3958 (2009/04/07)
Poly(ADP-ribose) polymerases (PARPs) play significant roles in various cellular functions including DNA repair and control of RNA transcription. PARP inhibitors have been demonstrated to potentiate the effect of cytotoxic agents or radiation in a number o
