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作者:Jared N. Cumming , Elizabeth M. Smith ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 2012, Vol.22 (7), pp.2444-2449
摘要:Abstract(#br)From an initial lead 1 , a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers CNS-derived Aβ following oral administration to rats. Herein we report SAR development in the S3 and F′ subsites...
作者:Jared N. Cumming , Patrick Dolan ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 1997, Vol.5 (7), pp.1257-1265
摘要:Abstract(#br)A series of tetracyclic and tricyclic trioxane dimers has been prepared with ether and ester tethers of varying length and flexibility. Several of these trioxane dimers have been found to have potent and potentially therapeutically valuable antimalarial, antiprolifer...
作者:Jared N. Cumming , Suji Xie ...
来源:[J].Bioorganic & Medicinal Chemistry Letters(IF 2.338), 1998, Vol.8 (8), pp.903-908
摘要:Abstract(#br)A series of 4,8-dimethyl-4-phenylsulfonylmethyl-2,3-dioxabicyclo[3.3.1]nonanes, carrying a variety of substituents at position-8 ( 4 ) were prepared by a short and efficient method from R -(+)-limonene. Key reactions include thiol oxygen cooxidation, and alkylation a...
作者:Jared N. Cumming , Warren G. Harbison ...
来源:[J].Tetrahedron Letters(IF 2.397), 1997, Vol.38 (22), pp.3817-3820
摘要:Abstract(#br)Development of a successful synthetic route to the racemic monoterpene 7R-paeonimetaboline-I is reported; extension of this methodology in an approach to synthesis of racemic paeoniflorigenone is also summarized.
作者:Annette L. Bodley , Jared N. Cumming , Theresa A. Shapiro
来源:[J].Biochemical Pharmacology(IF 4.576), 1998, Vol.55 (5), pp.709-711
摘要:Abstract(#br)Currently, the treatment of falciparum malaria is seriously compromised by spreading drug resistance. We studied the effects of camptothecin, a potent and specific topoisomerase I inhibitor, on erythrocytic malaria parasites in vitro . In Plasmodium falciparum , camp...
作者:Jared N. Cumming , Donna Klinedinst
来源:[J].Tetrahedron(IF 2.803), 1997, Vol.53 (1), pp.37-50
摘要:Abstract(#br)Mechanism-based design and short syntheses involving novel Tebbe methylenations of a-heteroatom-substituted ketones led to preparation of heteroatom-containing bicyclic endoperoxides 4 - 6 . The crucial final photo-oxygenative cyclization step succeeded only when the...
作者:Jared N. Cumming , Donna Klinedinst
来源:[J].Tetrahedron Letters(IF 2.397), 1996, Vol.37 (6), pp.815-818
摘要:Abstract(#br)Mechanism-based design, two-step synthesis, and in vitro antimalarial testing showed thermally stable, crystalline, bicyclic endoperoxides 2a and 2b to be potent antimalarials. Their reduction by FeBr 2 proceeds via oxy-radicals and then carbon radicals that und...
作者:Jared N. Cumming , Donna Klinedinst
来源:[J].Tetrahedron Letters(IF 2.397), 1996, Vol.37 (40), pp.7225-7228
摘要:Abstract(#br)Three or four step chemical synthesis and in vitro antimalarial testing showed crystalline, thermally stable, bicyclic endoperoxides 3c and 4c to be potent antimalarials, having approximately 15% of the antimalarial activity of the clinically used, complex, sesquiter...
作者:Jared N. Cumming , Poonsakdi Ploypradith ...
来源:[J].Tetrahedron Letters(IF 2.397), 1998, Vol.39 (16), pp.2273-2276
摘要:Abstract(#br)A series of new sulfide and sulfone 1,2,4-trioxanes was prepared in only a few steps from commercial reactants. The sulfone trioxanes were found to have higher in vitro antimalarial potencies than the sulfides, with 12β-arylsulfone trioxanes 1 β being from 1 3 t...
作者:... Dasong Wang , Jared N. Cumming , Gary H. Posner
来源:[J].Spectroscopy Letters(IF 0.667), 1997, Vol.30 (2), pp.241-255
摘要:Abstract(#br)A series of rules has been developed, using mainly 1D and 2D NMR spectroscopy, for identification of relative stereochemistry in a variety of substituted antimalarial 1,2,4-trioxanes.

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