- 2,3,4,5-Tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines as inhibitors of the bacterial enoyl ACP reductase, FabI
[作者：Ramnauth, J; Surman, MD; Sampson, PB; Forrest, B; Wilson, J; Freeman, E; Manning, DD; Martin, F; Toro, A; Domagala, M; Awrey, DE; Bardouniotis, E; Kaplan, N; Berman, J; Pauls, HW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5359-5362 , 文章类型： Article，,卷期：2009年19-18]
- In the search for new antibacterial agents, the enzyme FabI has been identified as an attractive target. Employing a structure guided approach, the previously reported ene-amide series of FabI inhibitors were expanded to...
- Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase
[作者：Deng, YQ; Shipps, GW; Wang, T; Popovici-Muller, J; Rosner, KE; Siddiqui, MA; Duca, J; Cooper, AB; Cable, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5363-5367 , 文章类型： Article，,卷期：2009年19-18]
- A series of 4H-pyrazolo[1,5-a]pyrimidin-7-one derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase. A number of these compounds exhibited potent activity in enzy...
- Photoregulation of thrombin aptamer activity using Bhc caging strategy
[作者：Li, YM; Shi, J; Luo, ZF; Jiang, H; Chen, XY; Wang, FL; Wu, X; Guo, QX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5368-5371 , 文章类型： Article，,卷期：2009年19-18]
- Thrombin aptamer was attempted to cage with Bhc (6-bromo-7-hydroxycoumarin-4-ylmethyl) group for controlling its specific affinity to target molecular through photolysis. By multiple-caging strategy, aptamer could be ren...
- Synthesis of novel [1,2]-diamines with antituberculosis activity
[作者：Meng, QY; Luo, HB; Chen, YL; Wang, TC; Yao, QZ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5372-5375 , 文章类型： Article，,卷期：2009年19-18]
- Guided by the metabolism information of SQ109, derivatives with substituted geranylamine moiety or substituted admantane ring of SQ109 were synthesized and evaluated as antituberculosis agents. Among all tested compounds...
- A novel class of highly potent multidrug resistance reversal agents: Disubstituted adamantyl derivatives
[作者：Min, KH; Xia, Y; Kim, EK; Jin, Y; Kaur, N; Kim, ES; Kim, DK; Jung, HY; Choi, Y; Park, MK; Min, YK; Lee, K; Lee, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5376-5379 , 文章类型： Article，,卷期：2009年19-18]
- Novel disubstituted adamantyl derivatives were synthesized and evaluated in a P-glycoprotein dependent multidrug resistance cancer cell line. The hit to lead optimization provided potent MDR reversal agents. Some potent ...
- Synthesis of gibberellin derivatives with anti-tumor bioactivities
[作者：Chen, JB; Sun, ZX; Zhang, YL; Zeng, XH; Qing, C; Liu, JP; Li, L; Zhang, HB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5496-5499 , 文章类型： Article，,卷期：2009年19-18]
- A series of gibberellin based molecules were designed and synthesized. Gibberellin derivatives bearing two alpha,beta-unsaturated ketone units showed strong anticancer activities in MTT assay towards a number of human ca...
- New Ras CAAX mimetics: Design, synthesis, antiproliferative activity, and RAS prenylation inhibition
[作者：Bolchi, C; Pallavicini, M; Fumagalli, L; Ferri, N; Corsini, A; Rusconi, C; Valoti, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5500-5504 , 文章类型： Article，,卷期：2009年19-18]
- Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing cysteine (C) by 2-hydroxymethylbenzodioxane or 2-aminomethylbenzodioxane, respectively etherified and amidified with 2'-methyl or 2'-met...
- Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2
[作者：Rachid, Z; MacPhee, M; Williams, C; Todorova, M; Jean-Claude, BJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5505-5509 , 文章类型： Article，,卷期：2009年19-18]
- The monoalkyltriazene moiety lends itself well to the design of combi-molecules. However, due to its instability under physiological conditions, efforts were directed towards stabilizing it by grafting a hydrolysable car...
- Unusual intramolecular N -> O acyl group migration occurring during conjugation of (-)-DHMEQ with cysteine
[作者：Kozawa, I; Kato, K; Teruya, T; Suenaga, K; Umezawa, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5380-5382 , 文章类型： Article，,卷期：2009年19-18]
- Previously we found that (-)-DHMEQ, a specific NF-kappa B inhibitor, covalently bound to a specific cysteine of NF-kappa B component proteins. In the course of formation of the (-)-DHMEQ and protected cysteine conjugate,...
- Efficient synthesis of (+/-)-parasitenone, a novel inhibitor of NF-kappa B
[作者：Saitoh, T; Suzuki, E; Takasugi, A; Obata, R; Ishikawa, Y; Umezawa, K; Nishiyama, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5383-5386 , 文章类型： Article，,卷期：2009年19-18]
- Dehydroxymethylepoxyquinomicin (DHMEQ, 1) is a novel nuclear factor-kappa B (NF-kappa B) inhibitor that inhibits DNA binding of NF-kappa B components including p65. To inspect its biological activity of 1, we synthesized...
- Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C
[作者：Guay, D; Beaulieu, C; Reddy, TJ; Zamboni, R; Methot, N; Rubin, J; Ethier, D; Percival, MD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5392-5396 , 文章类型： Article，,卷期：2009年19-18]
- A series of dipeptide nitriles with a thienyl alanine in P2 were identified as potent and selective cathepsin C inhibitors. Incorporation of a substituted cyclopropyl moiety in PI effectively protects these derivatives a...
- Synthesis of 2 alpha-substituted-14-epi-previtamin D-3 and its genomic activity
[作者：Sawada, D; Katayama, T; Tsukuda, Y; Saito, N; Takano, M; Saito, H; Takagi, K; Ochiai, E; Ishizuka, S; Takenouchi, K; Kittaka, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5397-5400 , 文章类型： Article，,卷期：2009年19-18]
- We synthesized and isolated 2 alpha-substituted analogs of 14-epi-previtamin D-3 after thermal isomerization at 80 degrees C for the first time. The VDR binding affinity and transactivation activity of osteocalcin promot...
- Spiropiperidine CCR5 antagonists
[作者：Rotstein, DM; Gabriel, SD; Makra, F; Filonova, L; Gleason, S; Brotherton-Pleiss, C; Setti, LQ; Trejo-Martin, A; Lee, EK; Sankuratri, S; Ji, CH; deRosier, A; Dioszegi, M; Heilek, G; Jekle, A; Berry, P; Weller, P; Mau, CI,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5401-5406 , 文章类型： Article，,卷期：2009年19-18]
- A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing o...
- Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens
[作者：Fu, LQ; Zhiteng, ZT; Cai, Z; Liu, X; He, HL; Yang, YS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5407-5410 , 文章类型： Article，,卷期：2009年19-18]
- A phosphate prodrug strategy was investigated to address the problem of poor aqueous solubility of pleuromutilin analogues. Water-soluble phosphate prodrugs 6a, 6b and 6c of pleuromutilin analogues were designed and synt...
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