[Synthesis and antisense properties of 2’β-F- and 2’α-F-2’-deoxy-uridines modified oligonucleotides with 4’-C-(2-methoxyethoxy) substituent].

Chemical modification is critical for the therapeutic applications of antisense oligonucleotides. Novel 4’-C-MOE and 2’-fluoro- modified monomer 2’-F-4’-C-MOE-ara U and its epimeric 2’-F-4’-C-MOE-r U were synthesized from 2’-fluorinated arabinourine (2’-F-ara U) and 2’-fluorouridine(2’-F-r U), respectively. Their phosphoramidites were synthesized and successfully incorporated into oligodeoxynucleotides.

[Metabolite profiling of two anti-HIV lead compounds in rat liver microsomes].

The metabolite profiling of DAPA-7012 and DAAN-4442, the lead compounds from two new kinds of non-nucleoside reverse transcriptase inhibitors (NNRTIs), was performed using an ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS/MS), with the assistance of a metabolite data processing software. By utilizing the mass defect filter (MDF) technique, the data acquired from the 0 h-incubation and the 2 h-incubation were compared and analyzed with the MetaboLynx software. After incubation, 14 metabolites of DAPA-7012 and 14 metabolites of DAAN-4442 were found in rat liver microsome.

[Design, synthesis and biologic evaluation of diarylbenzimidazole derivatives as novel HIV-1 non-nucleoside reverse transcriptase inhibitors].

Twenty seven new diarylbenzimidazole derivatives (A1-A21, B1-B6) were designed, synthesized, and evaluated in MT-2 cell line as potential HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) agents with a new skeleton based on molecular modeling technique and hit 1,2-diarylbenzimidazole A1 (EC50 69.9 miromol x L(-1)). Hence, 1,2-diarylbenzimidazoles A6 and B3, and 1,6-diarylbenzimidazole B6 showed obvious potency against HIV-1 replication in MT-2 cell line with EC50 values of 15.

[The research on accuracy of computer-assisted surgery].

The computer-assisted surgery system is a complex system. All of the errors can be attributed to the loss of correspondence between the world coordinate system in the operation room and the virtual world coordinate system obtained from the multi-model medical images. The system's accuracy is composed of the accuracy of the localizer and that of registration.