CAS: 1985-12-2; 4-Bromophenylisothiocyanate

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📜4-Bromophenyl Dithiocarbamic Acid Triethylammonium置于三光气体系中,用 氯仿 用作溶剂,化学反应生成4-溴苯基异硫氰酸酯
参考文献:通过药物再利用发现喹唑啉衍生物作为一类新的强效和体内有效的 Lsd1 抑制剂
标题:通过药物再利用发现喹唑啉衍生物作为一类新的强效和体内有效的 Lsd1 抑制剂
摘要:组蛋白赖氨酸特异性去甲基化酶 1 (Lsd1) 是一种重要的表观遗传调节剂,并以不同的方式参与恶性转化和肿瘤发病机制.因此,Lsd1的抑制为癌症治疗提供了一个有吸引力的治疗靶点.基于药物再利用策略,我们筛选了我们内部针对 Lsd1 的化学库,发现 Egfr 抑制剂厄洛替尼(一种 Fda 批准的肺癌药物)对 Lsd1 的效力较低(ic 50 = 35.80 μm).在此,我们报告了我们进一步的药物化学努力,以获得高度水溶性的厄洛替尼类似物5K (>100 Mg/ml),其对 Lsd1 的抑制活性显着增强 (Ic 50 = 0.69 μm) 以及更高的特异性.在 Mgc-803 细胞中,5K抑制 Lsd1 的去甲基化,表明其对酶的细胞活性.此外,5K具有显着的抑制集落形成,抑制迁移和诱导mgc803细胞凋亡的能力.此外,在 Mgc-803 异种移植小鼠模型中,5K治疗导致肿瘤大小分别在 40
Doi:10.1016/j.Ejmech.2021.113778

专利信息

专利号:WO-0027627-A1
优先权日:1998-11-12
标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles
发明人：WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO
权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO
摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.

专利号:US-2003009034-A1
优先权日:2001-03-22
标题 :Transition metal mediated process
发明人：WISHART NEIL; RITTER KURT
摘要:This invention relates to a transition metal mediated process for the preparation of optionally substituted 2-amino-benzoxazoles and or 2-amino-benzimidazoles, which are useful as therapeutic agents or as intermediates in the synthesis of therapeutic agents.

专利号:US-2003109714-A1
优先权日:2001-03-22
标题 :Transition metal mediated process
发明人：WISHART NEIL; RUDOLPH ALENA; RITTER KURT
摘要:This invention relates to a transition metal mediated process for the preparation of optionally substituted 2-amino-benzoxazoles and or 2-amino-benzimidazoles, which are useful as therapeutic agents or as intermediates in the synthesis of therapeutic agents.

专利号:CH-629169-A5
优先权日:1976-03-15
标 题 :Process for the preparation of compounds which have antimicrobial activity and epidermal tolerability from wastes from the synthesis of 4-chloro-2-methylphenol

专利号:CN-109053631-A
优先权日:2018-08-27
标 题:A kind of synthesis method of benzo[1,3]oxazine-2-thione by isothiocyanate and 2-sulfonylalkylphenol

专利号:CN-115960074-A
优先权日:2022-05-27
标题 :A class of fluorine-containing ferroelectric liquid crystal molecules containing a heteroatom six-membered alicyclic ring and its synthesis method