- Isolation, structure elucidation, and KDD study of (-)-Celosine, a new skeleton with potent anti-atherosclerosis activity
-
Natural (-)-Celosine was isolated as a novel endocyclicditerpene with an unprecedented skeleton from Celosia cristata L. Its structure was established by comprehensive 1D and 2D NMR spectroscopic analysis in combination with single-crystal X-ray crystallographic diffraction of synthesized (+)-Celosine. (-)-Celosine was expected to have an anti-atherosclerotic activity in vivo, and myeloperoxidase (MPO) expression may be the mechanism underlying this anti-atherosclerotic activity.
- Sun, Zhenliang,Lv, Zhiliang,Hu, Bin,Zhang, Jifa,Du, Peng,Wang, Man,Xiao, Linlin,Yang, Peiming
-
-
Read Online
- Synthesis, evaluation and quantitative structure–activity relationship (QSAR) analysis of Wogonin derivatives as cytotoxic agents
-
A novel series of 49 wogonin derivatives were synthesized by introducing group at 7-, 8- or B ring of wogonin. The cytotoxic activities against HepG2, A549 and BCG-823 cancer cell lines were also investigated in vitro. Several of them showed obvious cytotoxic activities and compound 3h possessed the highest potency against HepG2, A549, and BCG-823 with IC50 values of 1.07 μM, 1.74 μM and 0.98 μM, respectively. A quantitative structure-activity relationship (QSAR) study of these synthetic derivatives as well as wogonin indicated that high solubility and low octanol/water partition coefficient are favorable, and excessive electrostatic properties and refractivity are unfavorable for the cytotoxic activities of these wogonin derivatives. These findings and results provide a base for further investigations.
- Bian, Jinlei,Li, Tinghan,Weng, Tianwei,Wang, Jubo,Chen, Yu,Li, Zhiyu
-
supporting information
p. 1012 - 1016
(2017/09/30)
-
- Chalcone derivative, preparing method, pharmaceutical composition and application
-
The invention relates to a chalcone derivative, a preparing method, a pharmaceutical composition and application, provides a compound with the general formula I, and pharmaceutically-acceptable salt or solvate or polymorphic substances or metabolites or prodrugs of the compound, and further provides a preparing method of the compound of the structure shown in the general formula I, a pharmaceutical composition including the substance, and application of the substance in preparing medicine for treating or preventing inflammation. The general formula I is shown in the description, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are H, substituted or unsubstituted C1-C4 alkyl, hydroxyl, alkoxy, amino, halogen, C1-C4 substituted acylamino and C1-C4 acyl; R11 and R12 are substituted or unsubstituted C1-C4 alkyl.
- -
-
Paragraph 0110; 0111
(2017/02/09)
-