1149371-92-5Relevant articles and documents
Syntheses, cytotoxic activity evaluation and HQSAR study of 1,2,3-triazole-linked isosteviol derivatives as potential anticancer agents
Liu, Cong-Jun,Liu, Yan-Ping,Yu, Shu-Ling,Dai, Xing-Jie,Zhang, Tao,Tao, Jing-Chao
, p. 5455 - 5461 (2016)
A series of novel 1,2,3-triazole-linked isosteviol derivatives were designed and synthesized via Huisgen-click reaction. Their cytotoxicities in vitro against HCT-116 and JEKO-1 cells were screened. The preliminary bioassays indicated that most of the title compounds exhibited noteworthy cytotoxic activities. Particularly, the compound 10b revealed the most potent inhibitory activities against HCT-116 cells with IC50value of 2.987?±?0.098?μM, which was better than that (3.906?±?0.261?μM) of positive control cisplatin. On the basis of these bioactivity data, hologram quantitative structure–activity relationship (HQSAR) was performed, and a statistically reliable model with good predictive power (r2?=?0.848, q2?=?0.544 and R2pred?=?0.982) was achieved. Additionally, the contribution maps derived from the optimal model explained the individual atomic contributions to the activity for each molecule.
Stereoselective synthesis, characterization, and antibacterial activities of novel isosteviol derivatives with D-ring modification
Wu, Ya,Liu, Cong-Jun,Liu, Xu,Dai, Gui-Fu,Du, Jin-Yu,Tao, Jing-Chao
, p. 2052 - 2069 (2011/02/18)
Considerable interests have been attracted by isosteviol and its derivatives because of their large variety of bioactivities. In this project, a series of novel 15- and 16-substituted isosteviol derivatives were stereoselectively prepared by means of func