CAS: 20074-79-7; Diethyl 4-Aminobenzylphosphonate

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diethyl p-nitrobenzylphosphonate O,O-diethyl benzylphosphonate 15H22NO5PC15H22NO5P α-bromo-p-toluidine{4-[bis-(2-chloro-ethyl)-amino]-benzyl}-phosphonic acid diethyl ester {4-[bis-(2-iodo-ethyl)-amino]-benzyl}-phosphonic acid diethyl ester diethyl 4-(hydroxy)benzylphosphonate diethyl-4-(trifluoroacetylamino)phenylmethyl-phosphonate

📜1-(氯甲基)-4-硝基苯置于palladium On Activated Charcoal,氢气体系中,用 乙醇 用作溶剂,化学反应 18.0H,反应生成4-氨基苄基磷酸二乙酯
参考文献:7H-吡咯并[2,3-D]吡啶衍生物作为有效的fak抑制剂的发现:设计,合成,生物学评估和分子对接研究.
标题:7H-吡咯并[2,3-D]吡啶衍生物作为有效的fak抑制剂的发现:设计,合成,生物学评估和分子对接研究.
摘要:黏着斑激酶(fak)是负责各种肿瘤类型发展的细胞内非受体酪氨酸激酶.为了探索新的有效抑制剂,在基于结构的设计策略的基础上,设计并合成了两个系列的2,4-二取代-7 H-吡咯并[2,3-D ]嘧啶衍生物.生物学评估表明,这些新化合物中的大多数可以有效抑制fak激酶,从而导致有希望的抑制剂对抗u-87Mg,A-549和mda-Mb-231癌细胞的增殖.其中,优化的化合物18H 在u-87Mg,A-549和mda-Mb-231细胞中均有效抑制酶(ic 50 = 19.1 Nm),并显示出比tae-226更强的效力,Ic 50分别为0.35,0.24和0.34μm.化合物18H是多靶激酶抑制剂.此外,化合物18H 对正常人细胞株hk2的细胞毒性也较小(ic 50 = 3.72μm).根据流式细胞术和伤口愈合试验结果,化合物18H有效诱导mda-Mb-231细胞凋亡和g0 / G1期阻滞,并抑制u
Doi:10.1016/j.Bioorg.2020.104092

专利信息

专利号:US-9096624-B2
优先权日:2009-06-01
标 题:Amino pyrimidine anticancer compounds
发明人：CREW ANDREW P; SHERMAN DAN; APPARI RAMA DEVI; CHEN XIN; CHILUKURI RAMESH; DONG HANQING; FERRARO CATERINA; FOREMAN KENNETH; GUPTA RAMESH C; LI AN-HU; STOLZ KATHRYN M; VOLK BRIAN; ZAHLER ROBERT
权利人:OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula 1, as shown below and defined herein: n n n n n n n n n n n n and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.

专利号:US-9133224-B2
优先权日:2010-11-29
标 题:Macrocyclic kinase inhibitors
发明人：CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W
权利人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.