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Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2005 May 2 , DOI: 10.1016/j.bmcl.2005.03.026 Vincent M. Loh , Xiao-ling Cockcroft , Krystyna J. Dillon , Lesley Dixon , Jan Drzewiecki , Penny J. Eversley , Sylvie Gomez , Janet Hoare , Frank Kerrigan , Ian T.W. Matthews , Keith A. Menear , Niall M.B. Martin , Roger F. Newton , Jane Paul , Graeme C.M. Smith , Julia Vile , Alan J. Whittle
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2005 May 2 , DOI: 10.1016/j.bmcl.2005.03.026 Vincent M. Loh , Xiao-ling Cockcroft , Krystyna J. Dillon , Lesley Dixon , Jan Drzewiecki , Penny J. Eversley , Sylvie Gomez , Janet Hoare , Frank Kerrigan , Ian T.W. Matthews , Keith A. Menear , Niall M.B. Martin , Roger F. Newton , Jane Paul , Graeme C.M. Smith , Julia Vile , Alan J. Whittle
Screening of the Maybridge compound collection identified 4-arylphthalazinones as micromolar inhibitors of PARP-1 catalytic activity. Subsequent optimisation of both inhibitory activity and metabolic stability led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-ones with low nanomolar, cellular activity as PARP-1 inhibitors and promising metabolic stability in vitro.
中文翻译：
邻苯二氮。第1部分：设计和合成一系列新型的强力（ADP-核糖）聚合酶抑制剂。
Maybridge化合物集合的筛选确定了4-芳基邻苯二氮酮为PARP-1催化活性的微摩尔抑制剂。抑制活性和代谢稳定性的随后优化导致了一系列新的间位取代的4-苄基2H-酞菁-1-酮，具有低纳摩尔分子的细胞活性，作为PARP-1抑制剂，并有望在体外实现代谢稳定性。
更新日期：2017-01-31
中文翻译：
邻苯二氮。第1部分：设计和合成一系列新型的强力（ADP-核糖）聚合酶抑制剂。
Maybridge化合物集合的筛选确定了4-芳基邻苯二氮酮为PARP-1催化活性的微摩尔抑制剂。抑制活性和代谢稳定性的随后优化导致了一系列新的间位取代的4-苄基2H-酞菁-1-酮，具有低纳摩尔分子的细胞活性，作为PARP-1抑制剂，并有望在体外实现代谢稳定性。
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