- Inhibition of x(c)(-) transporter-mediated cystine uptake by sulfasalazine analogs
[作者:Shukla, K; Thomas, AG; Ferraris, DV; Hin, N; Sattler, R; Alt, J; Rojas, C; Slusher, BS; Tsukamoto, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6184-6187 , 文章类型: Article,,卷期:2011年21-20]
- A series of sulfasalazine analogs were synthesized and tested for their ability to block cystine-glutamate antiporter system x(c)(-) using L-[(14)C]cystine as a substrate. Replacement of sulfasalazine's diazo group with ...
- Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor
[作者:Liddle, J; Atkinson, FL; Barker, MD; Carter, PS; Curtis, NR; Davis, RP; Douault, C; Dickson, MC; Elwes, D; Garton, NS; Gray, M; Hayhow, TG; Hobbs, CI; Jones, E; Leach, S; Leavens, K; Lewis, HD; McCleary, S; Neu, M; Patel, VK; Preston, AGS; Ramirez-Molina, C; Shipley, TJ; Skone, PA; Smithers, N; Somers, DO; Walker, AL; Watson, RJ; Weingarten, GG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6188-6194 , 文章类型: Article,,卷期:2011年21-20]
- The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achiev...
- Ferrocenyl chalcone difluoridoborates inhibit HIV-1 integrase and display low activity towards cancer and endothelial cells
[作者:Monserrat, JP; Al-Safi, RI; Tiwari, KN; Quentin, L; Chabot, GG; Vessieres, A; Jaouen, G; Neamati, N; Hillard, EA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6195-6197 , 文章类型: Article,,卷期:2011年21-20]
- We report here the discovery of a potent series of HIV-1 integrase (IN) inhibitors based on the ferrocenyl chalcone difluoridoborate structure. Ten new compounds have been synthesized and were generally found to have sim...
- Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet)
[作者:Nagase, H; Koyano, K; Wada, N; Hirayama, S; Watanabe, A; Nemoto, T; Nakajima, M; Nakao, K; Mochizuki, H; Fujii, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6198-6202 , 文章类型: Article,,卷期:2011年21-20]
- An improved synthetic method for triplet drugs with the 1,3,5-trioxazatriquinane skeleton was developed that used p-toluenesulfonylmethyl isocyanide (TosMIC) instead of 1,3-dithiane. Using the improved method, we synthes...
- Novel 4-azasteroidal N-glycoside analogues bearing sugar-like D ring: Synthesis and anticancer activities
[作者:Huang, LH; Wang, YG; Xu, G; Zhang, XH; Zheng, YF; He, HL; Fu, WZ; Liu, HM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6203-6205 , 文章类型: Article,,卷期:2011年21-20]
- A series of novel N-glycoside analogues with 4-azasteroid moiety bearing sugar-like D ring were conveniently synthesized by constructing the core dihydropyran ring embedded in 4-azasteroidal skeleton which was prepared f...
- Ligand based virtual screening and biological evaluation of inhibitors of chorismate mutase (Rv1885c) from Mycobacterium tuberculosis H37Rv (vol 17, pg 3053, 2007)
[作者:Agrawal, H; Kumar, A; Bal, NC; Siddiqi, MI; Arora, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6206-6206 , 文章类型: Correction,,卷期:2011年21-20]
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