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Structure-guided identification of potent inhibitors of ROS1 kinase for therapeutic development against non-small cell lung cancer.
J Biomol Struct Dyn
May 2024
Centre of Medical and Bio-Allied Health Sciences Research, Ajman University, Ajman, United Arab Emirates.
Proto-oncogene tyrosine-protein kinase ROS (ROS1) is a member of the sevenless receptor, which affects epithelial cell differentiation and is highly expressed in a variety of tumor cells. The elevated expression and dysfunction of ROS1 have been involved in various malignancies, such as non-small cell lung cancer (NSCLC), stomach cancer, ovarian, breast cancer, cholangiocarcinoma, colorectal cancer, adenosarcoma, oesophageal cancer, etc. ROS1 has been postulated as a potential drug target in anticancer therapeutics.
View Article and Find Full Text PDFThree new compounds from the twigs and leaves of Hickel.
Nat Prod Res
July 2023
Department of Natural Product Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, P. R. China.
Two new diterpenoids, 12,15-di--acetylhypargenin B () and taiwanin F-12--β-D-glucopyranoside (), one new monoterpenoid, ()-7-methyl-3-methyleneoct-6-ene-1,2-diyl diacetate (), together with eight known compounds (-), were obtained from the twigs and leaves of Hickel. The structures of the new compounds were elucidated by extensive spectroscopic techniques including HR-ESI-MS and 1 D and 2 D NMR experiments. Spectroscopic data of the known compound were provided for the first time.
View Article and Find Full Text PDFChemical Constituents and an Antineuroinflammatory Lignan, Savinin from the Roots of .
Evid Based Complement Alternat Med
February 2019
Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan 54538, Republic of Korea.
The phytochemical investigation on the roots of (Araliaceae) resulted in the discovery of twenty compounds whose chemical structures were elucidated by the analysis of 1D-, 2D-NMR, mass spectrometry data, other physicochemical properties, and a comparison of the spectral data with the literature. They were identified as (-)-sesamin (), helioxanthin (), savinin (), taiwanin C (), 6-methoxy-7-hydroxycoumarin (), behenic acid (), 3--caffeoyl-quinic acid (), 5--caffeoyl-quinic acid (), 1,3-di--caffeoyl-quinic acid (), 1,4-di--caffeoyl-quinic acid (), 1,5-di--caffeoyl-quinic acid (), (+)--(7,8)-guaiacylglycerol--coniferyl aldehyde ether (), (+)--(7,8)-guaiacylglycerol--coniferyl aldehyde ether (), ferulic acid (), caffeic acid (), stigmasterol (), -sitosterol (), adenosine (), syringin (), and -coniferin (). Among these isolates, compound showed inhibitory activity against lipopolysaccharide- (LPS-) induced nitric oxide (NO) and prostaglandin E2 (PGE) production with IC values of 2.
View Article and Find Full Text PDFTaiwanin E inhibits cell migration in human LoVo colon cancer cells by suppressing MMP-2/9 expression via p38 MAPK pathway.
Environ Toxicol
August 2017
Graduate Institute of Basic Medical Science, China Medical University, Taichung, Taiwan.
Taiwanin E is a natural compound which is structurally analogous to estrogen II and is abundantly found in Taiwania cryptomerioides. It has been previously reported for its anticancer effects; however, the pharmaceutical effect of Taiwanin E on Human LoVo colon cancer cells is not clear. In this study, we investigated the effects of Taiwanin E on metastasis and the associated mechanism of action on Human LoVo colon cancer cells with respect to the modulations in their cell migration and signaling pathways associated with migration.
View Article and Find Full Text PDFSilver(I)-Catalyzed Regioselective Construction of Highly Substituted α-Naphthols and Its Application toward Expeditious Synthesis of Lignan Natural Products.
Org Lett
July 2015
†Medicinal and Process Chemistry Division and ‡Molecular and Structural Biology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
A novel route has been developed for regioselective synthesis of highly substituted α-naphthols, binaphthols, and anthracenol through silver(I) catalyzed C(sp(3))-H/C(sp)-H, C(sp(2))-H/C(sp)-H functionalization of β-ketoesters and alkynes, respectively, in a single step using water as a solvent. This protocol exhibited broad substrate scope and paved the way for synthesis of anticancer arylnaphthalene lignan natural products such as diphyllin, taiwanin E, and justicidin A with excellent selectivity.
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