1284213-88-2Relevant academic research and scientific papers
Synthesis and antimycobacterial evaluation of natural oridonin and its enmein-type derivatives
Xu, Shengtao,Pei, Lingling,Li, Dahong,Yao, Hong,Cai, Hao,Yao, Hequan,Wu, Xiaoming,Xu, Jinyi
, p. 300 - 306 (2015/07/27)
A series of enmein-type derivatives were synthesized and assayed for their antimycobacterial effects. The structures of the synthesized compounds were established by 1H NMR, 13C NMR and mass spectral analysis. All the compounds were screened for their antimycobacterial properties against Mycobacterium phlei, Mycobacterium smegmatis and Mycobacterium marinum. Compounds 2, 6g and 6i were found to exhibit potent antimycobacterial activity against M. phlei at a concentration of 0.5 μg/mL, which was comparable to that of positive drug streptomycin. Furthermore, five compounds were tested against Mycobacterium tuberculosis H37Rv based on the promising preliminary screening results. Among them, compound 10 showed potent activity with IC50 value of 17.1 μg/mL against M. tuberculosis H37Rv strain. Thus, compound 10 could emerge as a promising lead for further research work.
Synthesis and antimycobacterial evaluation of natural oridonin and its enmein-type derivatives
Xu, Shengtao,Pei, Lingling,Li, Dahong,Yao, Hong,Cai, Hao,Yao, Hequan,Wu, Xiaoming,Xu, Jinyi
, p. 300 - 306 (2015/01/09)
A series of enmein-type derivatives were synthesized and assayed for their antimycobacterial effects. The structures of the synthesized compounds were established by 1H NMR, 13C NMR and mass spectral analysis. All the compounds were screened for their antimycobacterial properties against Mycobacterium phlei, Mycobacterium smegmatis and Mycobacterium marinum. Compounds 2, 6g and 6i were found to exhibit potent antimycobacterial activity against M. phlei at a concentration of 0.5 μg/mL, which was comparable to that of positive drug streptomycin. Furthermore, five compounds were tested against Mycobacterium tuberculosis H37Rv based on the promising preliminary screening results. Among them, compound 10 showed potent activity with IC50 value of 17.1 μg/mL against M. tuberculosis H37Rv strain. Thus, compound 10 could emerge as a promising lead for further research work.
Library Construction and Biological Evaluation of Enmein-Type Diterpenoid Analogues as Potential Anticancer Agents
Li, Dahong,Xu, Shengtao,Cai, Hao,Pei, Lingling,Wang, Lei,Wu, Xiaoming,Yao, Hequan,Jiang, Jieyun,Sun, Yijun,Xu, Jinyi
, p. 812 - 818 (2013/08/25)
A library of promising enmein-type 14-O-diterpenoid derivatives was constructed from a commercially available kaurene-type oridonin by practical and efficient synthetic methods. These synthetic derivatives were evaluated for their antiproliferative activities against a set of four human cancer cell lines. The IC50 values are similar to or improved over those of the parent molecule and paclitaxel, the latter of which was used as a positive control. Compound 29 was further investigated for its apoptotic properties against human hepatocarcinoma Bel-7402 cells to better understand its mode of action. Moreover, compound 29 was shown to have potent antitumor activity invivo in studies with a murine model of gastric cancer (MGC-803 mice). These results warrant further preclinical investigations of these diterpenoid-based analogues as potential novel anticancer chemotherapeutics. Dosing with diterpenoids: A synthetic library of enmein-type diterpenoid derivatives with potent antitumor activities was constructed by using commercially available starting materials. The analogue shown here exhibits potent invitro and invivo activities and suitable chemical properties similar to or exceeding those of the parent compound, warranting further preclinical investigations for potential diterpenoid-based anticancer agents. Copyright
