CAS: 5805-52-7; 1H-Benzimidazole-2-Carboxamide

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CAS号148-79-8 噻菌灵 | CAS号4856-97-7 2-羟甲基苯并咪唑 | CAS号2849-93-6 1H-苯并咪唑-2-羧酸 | CAS号64-17-5 乙醇 | CAS号7181-87-5 1,3-二甲基-1H-苯并[d...

📜1H-苯并咪唑-2-甲酰氯置于ammonium Hydroxide体系中,化学反应 5.0H,反应生成 (9CI)-1H-苯并咪唑-2-羧酰胺
参考文献:Structure-Based Design Of Novel Benzimidazole Derivatives As Pin1 Inhibitors
标题:Structure-Based Design Of Novel Benzimidazole Derivatives As Pin1 Inhibitors
摘要:肽丙烯酰基脯氨酸顺反异构酶pin1在肿瘤发生过程中扮演着关键角色,能够放大和转导多个致癌信号通路.阻断pin1提供了一种独特的方式来破坏多个致癌通路并诱导细胞凋亡.为了开发有效的pin1抑制剂,设计并合成了一系列苯并咪唑衍生物.在这些衍生物中,化合物6H和13G表现出最强的pin1抑制活性,Ic50值分别为0.64和0.37μm.体外抗增殖实验表明,化合物6D,6G,6H,6N,6O和7C对人前列腺癌pc-3细胞表现出中等的抗增殖活性.综合来看,这些独特的苯并咪唑衍生物展示出很大的潜力,可以进一步作为有效的pin1抑制剂进行深入研究,提高其效力.
DOI:10.3390/molecules24071198

专利信息

专利号:US-9993570-B2
优先权日:2014-01-05
标题:Radiolabeled tracers for poly (ADP-ribose) polymerase-1 (PARP-1), methods and uses therefor
发明人：MACH ROBERT; CHU WENHUA; ZHOU DONG; MICHEL LOREN; CHEN DELPHINE
权利人:UNIV WASHINGTON
摘要:Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC 50 =6.3 nM). Synthesis of [ 18 F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [ 18 F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [ 18 F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.

专利号:US-7179918-B2
优先权日:2001-06-11
标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人：CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:US-7094909-B2
优先权日:2001-06-11
标 题 :HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人：KUCERA DAVID JOHN; SCOTT ROBERT WILLIAM
权利人:AGOURON PHARMA
摘要:The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, n nwhich are useful as inhibitors of the HIV protease enzyme.

专利号:CN-112538087-B
优先权日:2020-12-30
标 题 :Synthesis method of imidazopyridine compound