Facile synthesis of cyclopentapeptide, cyclo[Arg(NO2)-Gly-Asp(OBn)-D-Phe-Lys(Fmoc)], and its application in synthesis of integrin-targeting anticancer conjugate. Issue 21 (2nd November 2017) - Ma, Da-You
ABSTRACT: An efficient approach for integrin-targeting c RGDfK conjugate synthesis has been developed using a new protected cyclopentapeptide, c R(NO2 )GD(Bn)fK(Fmoc), as the key intermediate. c R(NO2 )GD(Bn)fK(Fmoc) was conveniently prepared in high yield. The Fmoc group of this cyclopentapeptide was selectively removed under mild conditions which makes it an ideal intermediate for c RGDfK conjugate synthesis as was well demonstrated in this paper by the synthesis of c RGDfK chlorambucil conjugate. GRAPHICAL ABSTRACT: