Research on promoting the asymmetric reaction of phenylacetylene with aldehydes by chloramphenicol base ligands.

A series of chiral ligands were synthesized using chloramphenicol base as starting materials. These ligands were applied to the asymmetric catalytic reactions of terminal alkynes with aldehydes to obtain a propargyl alcohol product in high yield (80-94%) with excellent enantioselectivities (82-96%).

[Triterpenoid saponins from roots of Phytolacca acinosa].

A new triterpenoid saponin named esculentoside U(1), along with the five known compounds, was isolated and characterized from the roots of Phytolacca acinosa, a commonly used traditional Chinese medicine with anti-inflammatory and anti-rheumatoid activities. The structure of the new saponin was elucidated as 3-O-[ß-D-glucopyranosyl-(1→4)]-ß-D-xylopyranosyl]-2, 23-dihydroxyolean-11, 13(18)-diene-28, 29-dioic acid 29-methyl ester(1). The assignment of all NMR signals of 1 was performed by means of 2D-NMR experiments.

Novel pirfenidone derivatives: synthesis and biological evaluation.

In order to discover novel anti-pulmonary fibrosis agents, a series of novel pirfenidone derivatives were designed and synthesized. All compounds were investigated for their anti-pulmonary activity and characterized by 13C and 1H nuclear magnetic resonance and high-resolution mass spectrometry. Preliminary studies on their biological activity showed that all target compounds showed different degrees of inhibition on pulmonary fibrosis, and most of the derivatives were significantly better than pirfenidone.

Synthesis and Antitumor Activity of Diosgenin Hydroxamic Acid and Quaternary Phosphonium Salt Derivatives.

Diosgenin, a component separated from Dioscorea plants, is an important starting material for steroid hormone drugs and semisynthetic steroids. In the work, two series of diosgenin derivatives were designed, synthesized, and evaluated for their cellular anticancer activities. Most of the target compounds exhibited good inhibitory activities against four cell lines, Aspc-1 (human colon adenocarcinoma cells), H358 (human nonsmall cell lung cancer cells), HCT116 (human colorectal adenocarcinoma cells), and SW620 (human metastatic pancreatic cancer cells). Among them, the representative compound 2.2f exhibited 7.9-341.7-fold antiproliferative activities against the above-mentioned four cell lines compared with the lead compound diosgenin.