1.Salicylic acid derivatives as simplified and novel GK small molecule activators.
Lianchao HUO ; Yuliang ZHANG ; Lei LEI ; Shuainan LIU ; Zhufang SHEN ; Yuling WANG ; Hongrui SONG ; Zhiqiang FENG
Acta Pharmaceutica Sinica 2013;48(4):514-20
Glucokinase (GK) is a new target for the treatment of type II diabetes mellitus (T2DM). In order to find a structure-simplified small molecule GK activator, 19 salicylic acid derivatives were designed and synthesized based on new lead compound (1). Experimental results showed that the potency of compound 8h is superior to control RO-28-0450 in GK activation.
2.Design, synthesis and antitumor activity of sorafenib analogues containing 2-picolinylhydrazide moiety.
Aifang QIN ; Yan LI ; Hongrui SONG ; Xiaoguang CHEN ; Xiaofeng JIN ; Ke WANG ; Lijing ZHANG ; Lianchao HUO ; Zhiqiang FENG
Acta Pharmaceutica Sinica 2012;47(12):1623-9
A novel series of sorafenib analogs containing 2-picolinyl hydrazide moiety were designed and synthesized. In vitro, most of synthesized compounds have antiproliferation activity on MDA-MB-231, ACHN, HepG2, Mia-PaCa-2 and SW1990 cell lines tested by MTT assay. It is worth noting that the antitumor activities of compounds 2c, 2d and 2f are more potent than that of sorafenib on pancreatic cancer cells Mia-PaCa-2 and SW1990, and the activities of compounds 3f and 3g are 2-3 times than that of sorafenib on human hepatocellular carcinoma HepG2 cell line.