CAS: 194423-15-9; N-(4-((3-Bromophenyl)Amino)Quinazolin-6-yl)Acrylamide

该化合物是一个化学化合物,在医学化学领域引起注意,特别是因其具有选择性抑制某些蛋白质动脉的作用而引起注意,该化合物的特点是能够调节特定的信号路径,使其成为癌症研究和其他治疗领域的兴趣对象;PD 168393,因其高度能性和选择性而闻名,对于尽量减少生物系统中的离目标影响至关重要;该化合物通常在有机溶剂中表现出良好的溶解性,便于其在各种实验环境中使用;此外,其分子结构包括有助于其生物活动和药用基因特性的功能组;与药物开发中的许多化合物一样,了解其行动,功效和安全特征机制对于潜在的治疗应用至关重要;

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CAS号79-10-7 丙烯酸 | CAS号169205-78-1 N4-(3-溴苯基)喹唑啉-4,6-二胺 | CAS号814-68-6 丙烯酰氯 | CAS号17420-30-3 2-氰基-4-硝基苯胺 | CAS号169205-77-0 N-(3-溴苯基)-6-硝基喹...

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    📜2-氰基-4-硝基苯胺置于吡啶,铁粉,溶剂黄146体系中,用 乙醚,乙醇 用作溶剂,化学反应 9.0H,反应生成N-[4-[(3-溴苯基)氨基]-6-喹唑啉]-2-丙酰胺
    参考文献:6-取代的4-(3-溴苯基氨基)喹唑啉类化合物是表皮生长因子受体(egfr)和人表皮生长因子受体(her-2)酪氨酸激酶的不可逆抑制剂,具有增强的抗肿瘤活性.
    标题:6-取代的4-(3-溴苯基氨基)喹唑啉类化合物是表皮生长因子受体(egfr)和人表皮生长因子受体(her-2)酪氨酸激酶的不可逆抑制剂,具有增强的抗肿瘤活性.
    摘要:已经制备了一系列新的6-取代的4-(3-溴苯基氨基)喹唑啉衍生物,其可以用作表皮生长因子受体(egfr)和人表皮生长因子受体(her-2)酪氨酸激酶的不可逆抑制剂.这些抑制剂在c-6位具有带有水溶性增溶取代基的丁炔酰胺,巴豆酰胺和甲基丙烯酰胺迈克尔受体.这些化合物是通过将6-氨基-4-(3-溴苯基氨基)喹唑啉与不饱和酰氯或混合酸酐酰化而制备的.我们显示,由于迈克尔加成的分子内催化和/或质子化碱性基团的诱导作用,将碱性官能团附接到迈克尔受体上导致更大的反应性.加上改善的水溶性,产生具有增强的生物学特性的化合物.我们目前分子模型和实验证据,这些抑制剂与目标酶共价相互作用.一种化合物16A在裸鼠的人表皮样癌(a431)异种移植模型中显示具有出色的口服活性.
    Doi:10.1021/jm0005555

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    专利信息


    专利号:US-11406709-B2
    优先权日:2014-09-15
    标 题 :Therapeutic and research application of PDCL3
    发明人：RAHIMI NADER
    权利人:UNIV BOSTON
    摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

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    主要参考文献


    1: da Rocha JF, Bastos L, Domingues SC, Bento AR, Konietzko U, da Cruz E Silva OAB, Vieira SI. APP Binds to the EGFR Ligands HB-EGF and EGF, Acting Synergistically with EGF to Promote ERK Signaling and Neuritogenesis. Mol Neurobiol. 2021 Feb;58(2):668-688. doi: 10.1007/s12035-020-02139-2. Epub 2020 Oct 2. 305(12):F1747-64. doi: 10.1152/ajprenal.00307.2013. Epub 2013 Oct 16.
    3: Poole NM, Nyindodo-Ogari L, Kramer C, Coons LB, Cole JA. Effects of tick saliva on the migratory and invasive activity of Saos-2 osteosarcoma and MDA- MB-231 breast cancer cells. Ticks Tick Borne Dis. 2013 Feb;4(1-2):120-7. doi: 10.1016/j.ttbdis.2012.09.003. Epub 2012 Nov 16. 606(1-3):1-8. doi: 10.1016/j.ejphar.2009.01.015. Epub 2009 Jan 21. 296(4):C735-45. doi: 10.1152/ajpcell.00246.2008. Epub 2009 Feb 11. 3(3):367-80. doi: 10.1586/14737140.3.3.367. 19(2A):919-24.

    合成参考文献


    参考文献:10.1158/1541-7786.mcr-05-0119
    摘要:Eum SY, Lee YW, Hennig B, Toborek M. Interplay between epidermal growth factor receptor and Janus kinase 3 regulates polychlorinated biphenyl-induced matrix metalloproteinase-3 expression and transendothelial migration of tumor cells. Mol Cancer Res. 2006 Jun;4(6):361–70. doi: 10.1158/1541-7786.mcr-05-0119.
    参考文献:10.1385/1-59745-012-x:61
    摘要:Wong ES, Guy GR. Regulator of epidermal growth factor signaling: Sprouty. Methods Mol Biol. 2006;327():61–83. doi: 10.1385/1-59745-012-x:61.
    参考文献:10.1073/pnas.0603948103
    摘要:Bose R, Molina H, Patterson AS, Bitok JK, Periaswamy B, Bader JS, Pandey A, Cole PA. Phosphoproteomic analysis of Her2/neu signaling and inhibition. Proc Natl Acad Sci U S A. 2006 Jun 27;103(26):9773–8.
    参考文献:10.1158/1078-0432.ccr-10-3283
    摘要:Pollack BP, Sapkota B, Cartee TV. Epidermal growth factor receptor inhibition augments the expression of MHC class I and II genes. Clin Cancer Res. 2011 Jul 01;17(13):4400–13. doi: 10.1158/1078-0432.ccr-10-3283.
    参考文献:10.1021/jm901558p
    摘要:Carmi C, Cavazzoni A, Vezzosi S, Bordi F, Vacondio F, Silva C, Rivara S, Lodola A, Alfieri RR, La Monica S, Galetti M, Ardizzoni A, Petronini PG, Mor M. Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion. J Med Chem. 2010 Mar 11;53(5):2038–50. doi: 10.1021/jm901558p.
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