CAS: 211555-04-3; 2-Bromo-4-((6,7-Dimethoxyquinazolin-4-yl)Amino)Phenol

📜6-硝基藜芦酸置于sodium Tetrahydroborate,氯化亚砜,Copper(II) Sulfate,三乙胺,三氯氧磷体系中,用 甲醇 用作溶剂,化学反应 13.83H,反应生成2-溴-4-(6,7-二甲氧基喹唑啉-4-基氨基)苯酚
参考文献:Treatment Of Atherosclerosis In Apolipoprotein E-Deficient Mice With 4-(3'-Bromobenzoyl)-6,7-Dimethoxyquinazoline (Whi-P164),A Potent Inhibitor Of Triglyceride Synthesis
标题:Treatment Of Atherosclerosis In Apolipoprotein E-Deficient Mice With 4-(3'-Bromobenzoyl)-6,7-Dimethoxyquinazoline (Whi-P164),A Potent Inhibitor Of Triglyceride Synthesis
摘要:我们鉴定了一种新型有机化合物,4-(3'-溴苯甲酰)-6,7-二甲氧基喹唑啉(化合物whi-P164),作为甘油三酯(tg)合成的强效抑制剂.在脂质合成的体外模型中,Whi-P164(而不是三种结构相似的对照二甲氧基喹唑啉化合物中的任何一种)以浓度依赖的方式抑制了caco-2人肠细胞中富含tg的细胞内脂滴的积累.在小鼠中,Whi-P164在剂量范围为0.5至80 Mg/kg的给药下没有引起与发病率或死亡率相关的急性毒性.在小鼠的药代动力学研究中,Whi-P164在腹腔注射后迅速从血浆中清除,终末消除半衰期为26.1 +/-1.3分钟,而在静脉注射后为33.3 +/-11.3分钟.以40 Mg/kg的whi-P164(而不是三种结构相似的对照二甲氧基喹唑啉化合物)每天腹腔注射一次,连续7天治疗,阻断了apoe缺乏小鼠和野生型c57B1/6小鼠的肝脏tg合成.在高脂/高胆固醇西方饮食条件下维持的apoe缺乏小鼠中,Whi-P164在7天的治疗后显著减少了肝脏中的脂质积累,而在1个月的治疗后显著减少了主动脉中的脂质积累.我们在apoe缺乏小鼠中的结果表明,肝细胞和泡沫细胞中的脂质积累是相关事件,使用whi-P164抑制tg合成为治疗动脉粥样硬化提供了一种有效的手段.
Doi:10.1097/00005344-200002000-00002

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.

专利号:US-6258820-B1
优先权日:1999-03-19
标题 :Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines