整合酶（integrase）对于人免疫缺陷病毒（HIV）-1逆转录病毒的复制来说是必不可少的，因而成为抗艾滋病（AIDS）药物设计的一个理性的靶点。最近文献报道了大量具有抗整合酶活性的化合物，当前最大的挑战就是如何将这些作用于整合酶靶点的先导化合物转变成为临床上有效的抗AIDS药物。

The complex [Mn(L)(NO3)2(H2O2)] (1) (L=2H-5-hydroxy-1, 2, 5-oxadiazo[3, 4-f]1,10-phenanthroline) was synthesized and characterized by elemental analysis, IR and UV. The crystal and molecular structure of 1 was determined by single-crystal X-ray diffraction; crystal data: light yellow, monoclinic, space group P21/n, Z=4, a=7.432(2)

Aseries of bleomycin analogues was prepared with a facile synthetic method. All the compounds were shown to display significant antitumor activity against HeLa and BGC-823 cell lines in vitro. The binding properties with CT-DNAand cleavage efficiency to pBR322 DNAwere investigated, the results indicate that there is a positive relationship between DNAcleavage efficiency and the binding affinity to DNA, and the antitumor activity of the bleomycin analogues is enhanced as the hydrophobicity of the C-terminus substituent side chain increased.

Replication of HIV-1 requires specific interactions of Tat protein with TAR RNA. Disruption of Tat-TAR RNA interaction could inhibit HIV-1 replication. Here four target compounds were designed and synthesized to bind to TAR RNA for blocking the interaction of Tat-TAR RNA. The core molecule 6,60-diamino-6,60-dideoxy-a,a-trehalose was obtained from selective bromination of, a,a-trehalose at C-6,60, followed by acetylation, azide displacement, deacetylation, and reduction. Coupling of the core molecule with the protected amino acid, then deprotection and guanidinylation generated the novel a,a-trehalose derivatives. Their abilities to inhibit Tat-TAR RNA interaction in human cells were determined by a Tat-dependent HIV-1 LTR-driven CAT assays.

Synthesis of unimolecularly circular G-quadruplex has been accomplished for the first time during our investigation on the template basis of G-quadruplex through chemical ligations of guanine-rich linear sequencesofoligodeoxyribonucleotides. Theuniqueness of this newly designed circularization course is its self-recognition and self-templating on the scale of individual strand of zligodeoxyribonucleotide in which the same linear sequence serves both as a template and as a substrate simultaneously. The results from our exonuclease and DNAse hydrolysis studies confirm that there is indeed absence of open termini within the structure of the identified circular product. Our subsequent investigation on the loopsize effect indicates that the unimolecularly circular G-uadruplex possessing two or more thymine nucleotides within their connecting loops is readily attainable, while the linear sequence with a single thymine nucleotide between guanine tracts is not a proper precursor for our ligation reaction. In addition, conformation dependency of the circularization course as well as the effects of alkali ions, pH values and concentration of potassium ions on the circularization reaction are examined during our investigation. The implication of our current studies and possible application of the obtained unimolecularly circular G-quadruplex in certain biological processes are also discussed in this report.