CAS: 60480-83-3; 2,4-Dimethylphenylhydrazine Hydrochloride

上下游产品

2,4-Xylidine methyl 4,6-H-indole-2-carboxylate 1-(2,4-dimethylphenyl)-4-methyl-5-(4-methoxyphenyl)-1H-pyrazole-3-carboxylic acid ethyl ester

📜2,4-二甲基苯胺置于盐酸,Sodium Nitrite,Tin(II) Chloride Dihdyrate体系中,用 水 作为反应溶剂,化学反应 4.5H,反应生成 2,4-二甲基苯肼盐酸盐
参考文献:作为微管蛋白抑制剂的(1-芳基-1 H-吡唑-4-基)(3,4,5-三甲氧基苯基)甲酮衍生物的合成及生物学评价
标题:作为微管蛋白抑制剂的(1-芳基-1 H-吡唑-4-基)(3,4,5-三甲氧基苯基)甲酮衍生物的合成及生物学评价
摘要:设计并合成了一系列(1-芳基-1 H-吡唑-4-基)(3,4,5-三甲氧基苯基)甲酮(8A-P,9A-P)和酮肟(10C)衍生物作为抗微管蛋白剂.评估所有目标化合物对三种肿瘤细胞系(a549,Ht-1080,Sgc-7901)的体外抗增殖活性.此类化合物中最有前途的化合物是(1-(对甲苯基)-1 H-吡唑-4-基)(3,4,5-三甲氧基苯基)甲酮(9C)和其酮肟衍生物(10C),可显着抑制肿瘤细胞生长,Ic 50值为0.054-0.16μm.同时,化合物9C表现出微管蛋白聚合的有效抑制活性.与其抗微管蛋白活性相一致,化合物9C可以破坏性地破坏微管网络,并在g2 / M期显着阻止sgc-7901细胞周期.结构-活性关系(sar)和构象分析表明,C环c4位的甲基对于活性至关重要,而b环c5位的氨基在维持生物活性方面起着负面作用.此外,进行了分子对接研究以阐明其在微管蛋白异二聚体中秋水仙碱位点的结合模式.
DOI:10.1016/j.Ejmech.2018.05.058

专利信息

专利号:US-8030311-B2
优先权日:2005-04-14
标题:Phenylacetamides suitable as protein kinase inhibitors
发明人：BOLD GUIDO; FURET PASCAL; GUAGNANO VITO; MCCARTHY CLIVE; VAUPEL ANDREA
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.