1445994-79-5Relevant 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 (2014)
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 (2015/07/27)
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.
Enmein-type diterpenoid analogs from natural kaurene-type oridonin: Synthesis and their antitumor biological evaluation
Li, Dahong,Xu, Shengtao,Cai, Hao,Pei, Lingling,Zhang, Hengyuan,Wang, Lei,Yao, Hequan,Wu, Xiaoming,Jiang, Jieyun,Sun, Yijun,Xu, Jinyi
, p. 215 - 221 (2013/07/27)
A series of enmein-type diterpenoid analogs (11-20) derived from natural kaurene-type diterpenoid oridonin were synthesized and biologically evaluated. All target compounds showed improved anti-proliferative activities against four human cancer cell lines compared with natural oridonin and parent compound 10. Some compounds were more potent than positive control Taxol. Furthermore, mechanistic investigation showed that the representative compound 17 affected cell cycle and induced apoptosis at low micro-molar level in human hepatoma Bel-7402 cells, via an oxidative stress triggered mitochondria-related caspase-dependent pathway.
