Facile synthesis of cyclopentapeptide,cyclo[Arg(NO2)-Gly-Asp(OBn)-D-Phe-Lys(Fmoc)], and its application in synthesis of integrin-targeting anticancer conjugate |
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| Authors: | Da-You Ma Tao Zhong Long-Long Wang Li-Jun Liu Ying-Xiong Wang |
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| Institution: | 1. School of Pharmaceutical Sciences, Central South University, Changsha, Hunan, China;2. School of Life Sciences, Central South University, Changsha, Hunan, China;3. Shanxi Engineering Research Center of Biorefinery, Chinese Academy of Sciences, Institute of Coal Chemistry, Taiyuan, Shanxi, China |
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| Abstract: | An efficient approach for integrin-targeting cRGDfK conjugate synthesis has been developed using a new protected cyclopentapeptide, cR(NO2)GD(Bn)fK(Fmoc), as the key intermediate. cR(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 cRGDfK conjugate synthesis as was well demonstrated in this paper by the synthesis of cRGDfK chlorambucil conjugate. |
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| Keywords: | Chlorambucil conjugate cR(NO2)GD(Bn)fK(Fmoc) cRGDfK integrin |
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