Identification and SAR of novel pyrrolo(1,2-a)pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).

Pescatore G; Branca D; Fiore

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Identification and SAR of novel pyrrolo(1,2-a)pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).

机译：新型吡咯并（1,2-a）吡嗪-1（2H）-1衍生物作为聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂的鉴定和SAR。

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Herein we describe the discovery of a novel series of pyrrolo[1,2-a]pyrazin-1(2H)-one PARP inhibitors. Optimization led to compounds that display excellent PARP-1 enzyme potency and inhibit the proliferation of BRCA deficient cells in the low double-digit nanomolar range showing excellent selectivity over BRCA proficient cancer cells.

机译：在这里，我们描述了一系列新型的吡咯并[1,2-a]吡嗪-1（2H）-1 PARP抑制剂的发现。优化导致化合物显示出优异的PARP-1酶效能，并在低两位数纳摩尔范围内抑制BRCA缺陷细胞的增殖，从而显示出比BRCA熟练的癌细胞优异的选择性。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共6页
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Pescatore G; Branca D; Fiore;
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1. Identification and SAR of novel pyrrolo(1,2-a)pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1). [J] . Pescatore G, Branca D, Fiore Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：新型吡咯并（1,2-a）吡嗪-1（2H）-1衍生物作为聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂的鉴定和SAR。
2. Development of substituted 6-(4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl)-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells. [J] . Ferrigno F, Branca D, Kinzel Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：作为有效的聚（ADP-核糖）聚合酶-1（PARP-1）的取代的6-（4-氟-3-（哌嗪-1-基羰基）苄基）-4,5-二甲基哒嗪-3（2H）-的开发在BRCA缺陷细胞中有活性的抑制剂。
3. Development of substituted 6-(4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl)-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells. [J] . Ferrigno F, Branca D, Kinzel Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：作为有效的聚（ADP-核糖）聚合酶-1（PARP-1）的取代的6-（4-氟-3-（哌嗪-1-基羰基）苄基）-4,5-二甲基哒嗪-3（2H）-的开发在BRCA缺陷细胞中有活性的抑制剂。
4. Identification of Novel Phosphorylation Sites in Poly (ADP-Ribose) Polymerase-1 and Poly (ADP-Ribose) Glycohydrolase Using Mass Spectrometry [C] . Sylvie Bourassa, Isabelle Kelly, Jean-Philippe Gagne, ASMS Conference on Mass Spectrometry and Allied Topics . 2008

机译：使用质谱法鉴定聚（ADP-核糖）聚合酶-1和聚（ADP-核糖）甘油糖酶的新型磷酸化位点
5. Evaluation of selected antioxidants and inhibitors of poly (ADP-ribose) polymerase-1 (PARP-1) as protective agents against mustard toxicity in vitro. [D] . Pino, Maria A. 2010

机译：评价选定的抗氧化剂和聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂作为体外抗芥子油毒性的保护剂。
6. Structure-Based Pharmacophore Modeling Virtual Screening Molecular Docking and Biological Evaluation for Identification of Potential Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors [O] . Yunjiang Zhou, Shi Tang, Tingting Chen, 2019

机译：基于结构的药理学建模虚拟筛选分子对接和生物学评估以鉴定潜在的聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂。
7. Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking and Biological Evaluation for Identification of Potential Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors [O] . Yunjiang Zhou, Shi Tang, Tingting Chen, 2019

机译：基于结构的药疗法建模，虚拟筛选，分子对接和鉴定潜在聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂的生物学评价
8. Treatment of BRCA1/2 Hereditary Breast Cancer and Sporadic Breast Cancer with Poly(ADP-ribose) PARP-1 Inhibitors and Chemotherapy [R] . DeSoto, J. A. 2008

机译：聚（aDp-核糖）paRp-1抑制剂和化疗治疗BRCa1 / 2遗传性乳腺癌和散发性乳腺癌

Identification and SAR of novel pyrrolo(1,2-a)pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).

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