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 C and H 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).