Various thioacetal artemisinin derivatives can inhibit the angiogenesis and might be angiogenesis inhibitors. In particular, 10 alpha-phenylthiodihydroartemisinins (5), 10 beta-benzenesulfonyl-9-epi-dihydroartemisinin (11) and 10 alpha-mercaptodihydroartemisinin (13) exhibit strong growth inhibition activity against HUVEC proliferation. Compound 11 have a good inhibitiory activity upon HUVEC tube formation, and 5 and 11 show a strong inhibitory effect on angiogenesis using CAM assay at 5 microg/egg by 90%.
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Synthesis of novel S-linked dihydroartemisinin derivatives and evaluation of their anticancer activity.
Eur J Med Chem
September 2019
Faculty of Life Sciences and Biotechnology, South Asian University, New Delhi, 110021, India. Electronic address:
We report herein the synthesis and anticancer activity of a set of novel S-linked artemisinins bearing an aliphatic/aromatic/heterocyclic nucleus as a substituent on the sulfur. The compounds were prepared from artemisinin via its lactol-form by an acid-catalyzed condensation of the desired thiol with the lactol. Both the C-10-α- and β-configured thiol ethers were synthesized with a view to making them available for the anticancer activity evaluation using a variety of cell lines.
View Article and Find Full Text PDFMalaria-infected mice live until at least day 30 after a new artemisinin-derived thioacetal thiocarbonate combined with mefloquine are administered together in a single, low, oral dose.
J Med Chem
September 2012
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218, USA.
In only three steps and in 21-67% overall yields from the natural trioxane artemisinin, a series of 21 new trioxane C-10 thioacetals was prepared. Upon receiving a single oral dose of only 6 mg/kg of the monomeric trioxane 12c combined with 18 mg/kg of mefloquine hydrochloride, Plasmodium berghei-infected mice survived on average 29.8 days after infection.
View Article and Find Full Text PDFSynthesis and antiangiogenic activity of thioacetal artemisinin derivatives.
Bioorg Med Chem
July 2004
Department of Chemistry, Yonsei University, Wonju 220-710, South Korea.
Various thioacetal artemisinin derivatives can inhibit the angiogenesis and might be angiogenesis inhibitors. In particular, 10 alpha-phenylthiodihydroartemisinins (5), 10 beta-benzenesulfonyl-9-epi-dihydroartemisinin (11) and 10 alpha-mercaptodihydroartemisinin (13) exhibit strong growth inhibition activity against HUVEC proliferation. Compound 11 have a good inhibitiory activity upon HUVEC tube formation, and 5 and 11 show a strong inhibitory effect on angiogenesis using CAM assay at 5 microg/egg by 90%.
View Article and Find Full Text PDFGrowth inhibition activity of thioacetal artemisinin derivatives against human umbilical vein endothelial cells.
Bioorg Med Chem Lett
November 2003
Department of Chemistry, Yonsei University, Wonju 220-710, South Korea.
Thioacetal artemisinin derivatives, in particular, 10alpha-phenylthiodihydroartemisinins (5), 10beta-benzenesulfonyl-9-epi-dihydroartemisinin (9) and 10alpha-mercaptodihydroartemisinin (11), exhibit good growth inhibition activity against HUVEC proliferation at the concentration level of 1 microM.
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