Synthesis and characterization of HPMA copolymer-5-FU conjugates

N-（2-Hydroxypropyl） methacrylamide copolymer-5-fluorouracil （PHPMA-FU） conjugates were synthesized by a novel and simplified synthetic route, and characterized by UV, FTIR and HPLC analyses. The conjugated content of 5-fluorouracil （5-FU） was 3.41 ± 0.07 wt%. The stabilities of PHPMA-FU conjugates under different conditions were studied. The results showed that HPMA copolymer was a potential carrier for tumor-targeting delivery of 5-FU.

Synthesis and theoretical study of first generation CCK-functional dendrimers

A convenient synthesis and theoretical study of five CCK-functional dendrimers is described. The dendritic cores were linked with the CCK（Trp-Met-Asp（OBn）-PheNH2） fragment by forming amide bonds to give five target molecules. The structures of CCK-functional dendrimers were characterized by NMR, MS spectrum and predicted using molecular mechanics and PM3 semi- empirical molecular orbital theory.

Convergent synthesis of second generation CCK-functional dendrimers

This paper describes the facile synthesis and characterization of novel dendrimers bearing 9 and 12 CCK peptide fragments on the surface by a convergent method. The structures of dendrimers are characterized by NMR and MS spectrum.

Synthesis and in vivo distribution of 2-deoxy-2-aminodiglucose-prednisolone conjugate(DPC)

In order to develop a novel kidney-targeted drug delivery system,a small molecular carrier（2-deoxy-2-aminodiglucose） was synthesized,and then the 2-deoxy-2-aminodiglucose-prednisolone conjugate（DPC） was synthesized to verify the kidney targeting capability of the carrier.Both 2-deoxy-2-aminodiglucose and DPC were confirmed by NMR and MS spectrum.The tissue distribution studies showed that DPC presented an excellent kidney targeting property in vivo,compared with prednisolone group, 4.9-fold of drug concentration in kidney was observed in the DPC group.Thus,it indicated that 2-deoxy-2-aminodiglucose could be a potential carrier for kidney-targeted drug delivery.

Alternative Methylation for the Synthesis of （＋）-Perophoramidine

An alternative NI-methylation strategy was reported in the late-stage of the total synthesis of （＋）-perophoramidine. Preparation of （＋）-perophoramidine was featured by an acid-catalyzed isomerization of amidine 5 to its C=N double bond tautorner 8, followed by two steps of NJ-methylation with NaHMDS/MeOTf and oxidation with MnO2. In contrast, direct methylation of amidine 5 afforded the NZ3-methylation conformers 9a and 9b, Further oxidation of 9a and 9b led to N23-methylated perophoramidine.

Prednisolone succinate-glucosamine conjugate:Synthesis,characterization and in vitro cellular uptake by kidney cell lines

Prednisolone succinate-glucosamine（PSG） conjugate,a prodrug for prednisolone,was synthesized and confirmed by NMR and MS spectrum.The stabilities of the prodrug in PBS（pH 2.50,5.00,7.20,and 7.89） were studied.Cytotoxicity and uptake assay of the prodrug were perfomed on HK-2 and MDCK cell lines.The results showed that compared with prednisolone,the PSG not only did not increase the cytotoxicity but also improved the uptake to 2.2 times of prednisolone by the cells.Thus,it indicated that glucosamine might be a potential carrier for kidney-targeting delivery of prednisolone.