TSRI-265
Chemical Name: N1,N3-Bis[2-[5(S)-carboxy-5-[4-(trifluoromethyl)benzyloxycarboxamido]pentylamino]-2-oxoethyl]benzene-1,3-dicarboxamide
项目整合开发状态: Preclinical
项目研究机构: Scripps Research Institute (Originator)
合成路线:Reaction of 4-(trifluoromethyl)benzyl alcohol (I) with DSC followed by coupling with partially protected lysine (II) affords carbamate (III),which is converted into derivative (V) first by Boc removal with HCl/dioxane in dichloromethane followed by coupling with Boc-Gly-OH (IV) by means of EDCl and DIEA.Boc removal of compound (V) with HCl/dioxane in dichloromethane,followed by condensation with isophthaloyl dichloride (VI) by means of DIEA in DMF,gives compound (VII),which is finally subjected to methyl ester saponification with LiOH in THF/MeOH to provide the desired product.
📌 参考资料/链接：
参考文献标题:Identification of a novel class of small-molecule antiangiogenic agents through the screening of combinatorial libraries which function by inhibiting the binding and localization of proteinase MMP2 to integrin alphavbeta3
文献作者:Boger,D.L.; Goldberg,J.; Silletti,S.; Kessler,T.; Cheresh,D.A.
参考来源:J Am Chem Soc 2001,123(7),1280