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A series of Andro derivatives were described and evaluated for their anti-HIV activity in vitro . Compound 10 and 16b , of which TI were >10, had some anti-HIV-1 activity in vitro . Therein, compound 10 which was the best potent compound, could serve as a new lead for further development of anti-AIDS agents.

A series of novel derivatives of indirubin were synthesized and evaluated for their anti-proliferative activity against human cancer cell lines of SGC7901, A549, HL-60, SK-BR-3 and HCT116. Most of the compounds displayed more potent activity than Sunitinib. In addition, the derivatives showed improved water solubility, which may be favorable to their pharmacokinetic performances.

Fatty acid modified glucagon-like peptide-1 (7-36) amide was synthesized efficiently on Rink-Amide-MBHA resin by microwave-assisted solid phase method. The method of thermal and controlled microwave irradiation provided impressive enhancements in product yield, selectivity, and reaction rate. The coupling time was dramatically decreased to 6 min, and the desired products were obtained in high yield and purity.

A series of imidazo[1,2-a]pyrimidine derivatives substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized in order to improve their anti-inflammatory activities. Biological tests suggested that these compounds have anti-inflammatory activities with COX-2 selectivity to some extent.

A new isochroman-4-one, 7, 8-dihydroxy-3-methylisochroman-4-one was isolated from water soluble fraction of Musa sapientum L. Its structure was determined by spectroscopic evidences and its total synthesis has also been reported. The compound showed potent antihypertensive activity.

A microwave-assisted solid phase synthesis for endothelin 1 is presented. Reduced endothelin 1 was synthesized efficiently on Wang resin under microwave irradiation using Fmoc/tBu orthogonal protection strategy. The whole peptide was cleaved from the resin and two disulphide bridges were formed under air oxidation at room temperature. The purity and efficiency of synthesizing the peptide is much higher than other methods used before.

A convenient method for the synthesis of ezetimibe analogs as cholesterol absorption inhibitors was described. The key step in the synthesis was the intramolecular ring formation through Mitsunobu reaction. Furthermore, a new series of analogs was designed and synthesized.

Tetrahydroisoquinoline derivatives were synthesized and their multidrug resistance reversal activities were evaluated in vitro. The results showed that some of the synthetic compounds had higher multidrug resistance (MDR) reversal activities than verapamil.

Human urotension-II was synthesized efficiently on Wang resin under microwave irradiation using Fmoc/tBu orthogonal protection strategy. Disulphide bridge was formed on solid phase with the irradiation of microwave, then the whole peptide was cleaved from the resin. The purity of crude peptide cyclized under microwave irradiation was higher than that under room temperature.

2-[2-(2,2,2-Trifluoroethoxy)phenoxy]ethanamine is the key intermediate of Silodosin, the α 1 -adrenoceptor antagonist for the treatment of benign prostatic hyperplasia. In order to obtain this intermediate, we developed a novel synthetic route by utilizing 2-nitrochlorobenzene as the starting material via O -alkylation, reduction, diazotization, acidolysis, etherification, condensation and hydrazinolysis. The highlight of this method lies on its convenience and economy in accessing this intermediate.