Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Kristina Borstnik"'
Autor:
Kristina Borstnik, Tanzina Labonte, Wonsuk Chang, Andrew J. McRiner, Adebusola A. Alagbala, Gary H. Posner, John G. D'angelo, Barbara A. Foster
Publikováno v:
Journal of Medicinal Chemistry. 49:7836-7842
The mechanisms of action of three C-10 non-acetal trioxane dimers (TDs) were examined in human (LNCaP) and mouse (TRAMP-C1A and -C2H) prostate cancer cell lines. 1 (AJM3/23), 2 (GHP-TM-III-07w), and 3 (GHP-KB-06) inhibited cell growth with 3 being th
Publikováno v:
Mini-Reviews in Medicinal Chemistry. 2:573-583
Chemical insights into artemisinin's biological mechanism of action have allowed rational design of some new trioxane and endoperoxide antimalarial drug candidates that are efficacious and safe. This review summarizes recent achievements in this area
Publikováno v:
International Journal for Parasitology. 32:1661-1667
Mechanism-based rational design and gram-scale chemical synthesis have produced some new trioxane and endoperoxide antimalarial drug candidates that are efficacious and safe. This review summarises recent achievements in this area of peroxide drug de
Autor:
Suji Xie, Ik-Hyeon Paik, Theresa A. Shapiro, Kristina Borstnik, Heung Bae Jeon, Gary H. Posner, Poonsakdi Ploypradith
Publikováno v:
Journal of Medicinal Chemistry. 45:3824-3828
Short chemical syntheses of four new antimalarial trioxanes are presented, starting with inexpensive and commercially available cyclohexanone. Almost exclusive formation of the trioxane 12alpha-stereoisomers simplifies product purification. Carboxyph
Autor:
and Adebusola Alagbala, Andrew J. McRiner, Suji Xie, Ik-Hyeon Paik, Barbara A. Foster, Gary H. Posner, Surojit Sur, Theresa A. Shapiro, Kristina Borstnik
Publikováno v:
Journal of Medicinal Chemistry. 47:1299-1301
In only four chemical steps from naturally occurring artemisinin (1), trioxane dimers 6 and 7 were prepared on a multigram scale in overall 32-44% yields. In mice, both isonicotinate N-oxide dimer 6 and isobutyric acid dimer 7 were considerably more
Autor:
Kristina Borstnik, Patrick G. Bray, Alison Miller, Paul M. O'Neill, Jill Davies, Chang Ho Oh, Gary H. Posner, Stephen A. Ward, Sarah L. Rawe
Publikováno v:
Chembiochem : a European journal of chemical biology. 6(11)
The aim of this study was to synthesise pure enantiomers of potent antimalarial 1,2,4-trioxanes, which are related to the natural antimalarial artemisinin, and then to assay each against a panel of Plasmodium falciparum strains. The working hypothesi
Publikováno v:
ChemInform. 34
Silicon nucleophilic β-addition to various 2-cycloalkenones, followed ultimately by mild and rapid α-alkylation of the corresponding cycloalkanone enolates using diverse epoxides and BF3·OEt2, produces useful γ-lactols and γ-hydroxyketones. Hype
Autor:
Suji Xie, Gary H. Posner, Surojit Sur, Andrew J. McRiner, Ik-Hyeon Paik, Theresa A. Shapiro, Kristina Borstnik
Publikováno v:
Journal of medicinal chemistry. 46(6)
In only two steps and in 70% overall yield, naturally occurring trioxane artemisinin (1) was converted on a gram scale into C-10-carba trioxane dimer 3. This new, very stable dimer was then transformed easily in one additional step into four differen
Autor:
Theresa A. Shapiro, Gary H. Posner, Thomas W. Kensler, John Northrop, Suji Xie, Kristina Borstnik, Patrick M. Dolan, Ik-Hyeon Paik
Publikováno v:
Bioorganicmedicinal chemistry. 10(1)
Joining two 10-deoxoartemisinin trioxane units via a p -diacetylbenzene linker produces new C-10 non-acetal dimers 3b and 3c . 1 H NMR spectroscopy allows unambiguous assignment of the stereochemistry at C-10 in these dimers. Successful replacement o