CAS: 53267-93-9; Boc-Tyr(Me)-Oh

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草酸单叔丁酯置于n-甲基吗啉,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,Lithium Hydroxide体系中,用 四氢呋喃,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 2.0H,反应生成 Boc-O-甲基-L-酪氨酸
参考文献:三肽基呋喃酮酮作为人20S蛋白酶体β5亚基选择性抑制剂的设计与合成
标题:三肽基呋喃酮酮作为人20S蛋白酶体β5亚基选择性抑制剂的设计与合成
摘要:设计合成了一系列以呋喃酮为c末端的三肽蛋白酶体抑制剂.针对β1,β2和β5亚基的生化评估表明,它们选择性地作用于β5亚基,Ic 50抑制微摩尔范围内的胰凝乳蛋白酶样(ct-L)活性.配体20S蛋白酶体混合物的lc-Ms / Ms分析表明,最有效的化合物11M(ic 50 = 0.18μm)对20S蛋白酶体未进行共价修饰.但是,在洗脱分析中发现它以缓慢可逆的方式起作用,并且可逆性远低于mg132,这表明这些三肽呋喃酮与20S蛋白酶体形成可逆共价键的可能性.选择了几种化合物用于针对多种癌细胞系的抗增殖测定,并且化合物11M在所有测试的细胞系中显示出与阳性对照(mg132)相当的效能.此外,大鼠的药代动力学(pk)数据表明11M的行为与临床使用的卡非佐米类似(c Max,2007μg/ L; Auc 0-T,680μg / L.h; V Ss,0.66 L / Kg).所有这些数据表明11M是一
DOI:10.1016/j.Ejmech.2020.112160

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:WO-9834113-A1
优先权日:1997-02-04
标题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein
发明人：OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; HOUGHTEN RICHARD A; BLONDELLE SYLVIE E; SCHONER CHRISTA C
权利人:TREGA BIOSCIENCES INC
摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.

专利号:US-6359144-B1
优先权日:1997-02-04
标 题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein
发明人：OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; BLONDELLE SYLVIE E; SCHONER CHRISTA C; HOUGHTEN RICHARD A
权利人:LION BIOSCIENCE AG
摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.

专利号:EP-0412508-B1
优先权日:1989-08-07
标 题:Analogues of vasopressin, their preparation and pharmaceutical use
发明人：PROCHAZKA ZDENKO; BLAHA IVO; ZERTOVA MIROSLAVA; SLANINOVA JIRINA; VELEK JIRI; SKOPKOVA JANA; LEBL MICHAL; BARTH TOMISLAV; MALETINSKA LENKA; VILHARDT HANS
权利人:CESKOSLOVENSKA AKADEMIE VED
摘要:The invention relates to analogues of 8-D-homoarginine-vasopressin of the general formula in which the meanings are: X L-O-methyltyrosine L-p-ethylphenylalanine D-p-ethylphenylalanine L-p-methylphenylalanine or D-p-methylphenylalanine and R cysteine or beta -mercaptopropionic acid to a process for the preparation thereof by solid-phase synthesis and to the pharmaceutical use thereof. The analogues of vasopressin have a selectively increased affinity for uterine oxytocin receptors, where they have an antagonistic action to oxytocin. The analogues of deaminovasopressin furthermore have a significantly reduced antidiuretic activity compared with [8-D-arginine]-deaminovasopressin.