Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.

Suppr

超能文献

作者信息

Tao Ming, Park Chung Ho, Bihovsky Ron, Wells Gregory J, Husten Jean, Ator Mark A, Hudkins Robert L

机构信息

Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380-4245, USA.

出版信息

Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. doi: 10.1016/j.bmcl.2005.10.099. Epub 2005 Nov 15.

DOI:10.1016/j.bmcl.2005.10.099

PMID:16290935

Abstract

A series of novel pyrrolocarbazoles was synthesized as potential PARP-1 inhibitors. Pyrrolocarbazole 1 was identified as a potent PARP-1 inhibitor (IC50 = 36 nM) from our internal database. Synthesis of analogs around this template with the aid of modeling studies led to the identification of the truncated imide 14. Compound 14 (IC50 = 40 nM), with deleted B-ring, was found to be an equipotent PARP-1 inhibitor.

摘要

相似文献

Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. doi: 10.1016/j.bmcl.2005.10.099. Epub 2005 Nov 15.

Novel poly(ADP-ribose) polymerase-1 inhibitors.新型聚（ADP - 核糖）聚合酶 -1抑制剂

Bioorg Med Chem Lett. 2007 Jan 15;17(2):542-5. doi: 10.1016/j.bmcl.2006.10.010. Epub 2006 Oct 10.

Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).新型吡咯并咔唑内酰胺类似物作为聚（ADP - 核糖）聚合酶 -1（PARP -1）的强效细胞渗透性抑制剂的合成及构效关系

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1151-5. doi: 10.1016/j.bmcl.2005.11.086. Epub 2005 Dec 15.

Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.酞嗪酮2：新型高效聚（ADP - 核糖）聚合酶抑制剂的优化与合成

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1040-4. doi: 10.1016/j.bmcl.2005.10.081. Epub 2005 Nov 15.

Novel poly(ADP-ribose) polymerase-1 inhibitors.新型聚（ADP-核糖）聚合酶-1 抑制剂。

Bioorg Med Chem Lett. 2012 Jan 1;22(1):222-4. doi: 10.1016/j.bmcl.2011.11.032. Epub 2011 Nov 17.

Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.酞嗪酮。第1部分：新型高效聚（ADP-核糖）聚合酶抑制剂系列的设计与合成。

Bioorg Med Chem Lett. 2005 May 2;15(9):2235-8. doi: 10.1016/j.bmcl.2005.03.026.

Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.新型聚（ADP - 核糖）聚合酶的烷氧基苯甲酰胺抑制剂

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3942-5. doi: 10.1016/j.bmcl.2008.06.025. Epub 2008 Jun 12.

Discovery of 1-substituted benzyl-quinazoline-2,4(1H,3H)-dione derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors.发现1-取代苄基喹唑啉-2,4(1H,3H)-二酮衍生物作为新型聚（ADP-核糖）聚合酶-1抑制剂。

Bioorg Med Chem. 2015 Feb 15;23(4):681-93. doi: 10.1016/j.bmc.2014.12.071. Epub 2015 Jan 8.

Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.三环苯并咪唑作为有效的聚（ADP - 核糖）聚合酶 -1抑制剂。

J Med Chem. 2003 Jan 16;46(2):210-3. doi: 10.1021/jm0255769.

Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).含非芳酰胺的三环衍生物的合成与评价作为聚（ADP-核糖）聚合酶-1（PARP-1）抑制剂。

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2250-3. doi: 10.1016/j.bmcl.2010.02.014. Epub 2010 Feb 8.

引用本文的文献

Preparation of dibenzo[e,g]isoindol-1-ones via Scholl-type oxidative cyclization reactions.通过肖尔型氧化环化反应制备二苯并[e,g]异吲哚-1-酮

J Org Chem. 2014 Sep 5;79(17):8049-58. doi: 10.1021/jo501185f. Epub 2014 Aug 25.

Marine pyrrolocarbazoles and analogues: synthesis and kinase inhibition.海洋吡咯并咔唑类化合物及其类似物：合成与激酶抑制作用。

Mar Drugs. 2009 Dec 1;7(4):754-86. doi: 10.3390/md7040754.

Poly(ADP-ribose) polymerase-1 activity facilitates the dissociation of nuclear proteins from platinum-modified DNA.聚（ADP - 核糖）聚合酶 -1 的活性促进核蛋白与铂修饰的 DNA 解离。

Bioorg Med Chem. 2008 Dec 1;16(23):10121-8. doi: 10.1016/j.bmc.2008.09.074. Epub 2008 Oct 14.

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验