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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共36条记录   The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors [作者：Innocenti, A; Pastorekova, S; Pastorek, J; Scozzafava, A; De Simone, G; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5825-5828 , 文章类型： Article，,卷期：2009年19-20] The enzymatic activities of carbonic anhydrase ( CA, EC 4.2.1.1) isozymes CA I, II, IX (catalytic domain (cdCA IX) and catalytic domain plus proteoglycan, flCA IX), XII and XIV were investigated as a function of pH for t... First generation 5-vinyl-3-pyridinecarbonitrile PKC theta inhibitors [作者：Niu, CS; Boschelli, DH; Tumey, LN; Bhagirath, N; Subrath, J; Shim, J; Wang, Y; Wu, BQ; Eid, C; Lee, J; Yang, XK; Brennan, A; Chaudhary, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5829-5832 , 文章类型： Article，,卷期：2009年19-20] A series of 5-vinyl-3-pyridinecarbonitriles were synthesized and evaluated as PKC theta inhibitors. The systematic optimization of 4-[(4-methyl-1H-indol-5-yl)amino]-5-[(E)-2-phenylvinyl]-3-pyridinecarbonitrile 3 resulted... Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols [作者：Guillon, R; Giraud, F; Loge, C; Le Borgne, M; Picot, C; Pagniez, F; Le Pape, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5833-5836 , 文章类型： Article，,卷期：2009年19-20] We previously reported on the design and synthesis of 1-[((hetero)aryl- or piperidinylmethyl) amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols showing various degrees of antifungal activity against Candida albicans ... Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors [作者：Giroux, A; Boulet, L; Brideau, C; Chau, A; Claveau, D; Cote, B; Ethier, D; Frenette, R; Gagnon, M; Guay, J; Guiral, S; Mancini, J; Martins, E; Masse, F; Methot, N; Riendeau, D; Rubin, J; Xu, DG; Yu, HP; Ducharme, Y; Friesen, RW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5837-5841 , 文章类型： Article，,卷期：2009年19-20] Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imida... Phosphoinositide-3-kinase (PI3K) inhibitors: Identification of new scaffolds using virtual screening [作者：Frederick, R; Mawson, C; Kendall, JD; Chaussade, C; Rewcastle, GW; Shepherd, PR; Denny, WA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5842-5847 , 文章类型： Article，,卷期：2009年19-20] In the present work, we used virtual screening (VS) of the ZINC database of 2.5 million compounds to seek new PI3K inhibitory scaffolds. The VS flowchart implemented various filters, including a 3D-database screen, and e... Synthetic substrate for application in both high and low throughput assays for botulinum neurotoxin B protease inhibitors [作者：Salzameda, NT; Barbieri, JT; Janda, KD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5848-5850 , 文章类型： Article，,卷期：2009年19-20] A FRET peptide substrate was synthesized and evaluated for enzymatic cleavage by the BoNT/B light chain protease. The FRET substrate was found to be useful in both a high throughput assay to uncover initial 'hits' and a ... Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase [作者：Selness, SR; Devraj, RV; Monahan, JB; Boehm, TL; Walker, JK; Devadas, B; Durley, RC; Kurumbail, R; Shieh, H; Xing, L; Hepperle, M; Rucker, PV; Jerome, KD; Benson, AG; Marrufo, LD; Madsen, HM; Hitchcock, J; Owen, TJ; Christie, L; Promo, MA; Hickory, BS; Alvira, E; Naing, W; Blevis-Bal, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5851-5856 , 文章类型： Article，,卷期：2009年19-20] The identification and evolution of a series of potent and selective p38 inhibitors is described. p38 inhibitors based on a N-benzyl pyridinone high-throughput screening hit were prepared and their SAR explored. Their de... Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate [作者：Mowbray, CE; Burt, C; Corbau, R; Gayton, S; Hawes, M; Perros, M; Tran, I; Price, DA; Quinton, FJ; Selby, MD; Stupple, PA; Webster, R; Wood, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5857-5860 , 文章类型： Article，,卷期：2009年19-20] We prepared three discreet cohorts of potent non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on the recently reported 3-cyanophenoxypyrazole lead 3. Several of these compounds displayed very promising ... Small kinase assay panels can provide a measure of selectivity [作者：Brandt, P; Jensen, AJ; Nilsson, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5861-5863 , 文章类型： Article，,卷期：2009年19-20] In this Letter, a novel strategy for assessment of ligand promiscuity is described. By using a carefully selected small set of kinases together with multivariate statistical methods, a measure of selectivity can be estim... Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase [作者：Taylor, SJ; Soleymanzadeh, F; Eldrup, AB; Farrow, NA; Muegge, I; Kukulka, A; Kabcenell, AK; De Lombaert, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5864-5868 , 文章类型： Article，,卷期：2009年19-20] A series of potent nicotinamide inhibitors of soluble epoxides hydrolase (sEH) is disclosed. This series was designed using structure-based deconstruction and a combination of two HTS hit series, resulting in hybrid anal... Parallel chemoenzymatic synthesis of sialosides containing a C5-diversified sialic acid [作者：Cao, HZ; Muthana, S; Li, YH; Cheng, JS; Chen, X,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5869-5871 , 文章类型： Article，,卷期：2009年19-20] A convenient chemoenzymatic strategy for synthesizing sialosides containing a C5-diversified sialic acid was developed. The alpha 2,3- and alpha 2,6-linked sialosides containing a 5-azido neuraminic acid synthesized by a... Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase [作者：Haque, TS; Liang, NN; Golla, R; Seethala, R; Ma, ZP; Ewing, WR; Cooper, CB; Pelleymounter, MA; Poss, MA; Cheng, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5872-5876 , 文章类型： Article，,卷期：2009年19-20] We report the synthesis and enzymatic evaluation of potent inhibitors of acetyl-CoA carboxylases (ACCs) containing biphenyl or 3-phenyl pyridine cores. These compounds inhibit both ACC1 and ACC2, or are moderately select... Cell recognition enhanced enzyme hydrolysis of a model peptide-drug conjugate [作者：Kotamraj, PR; Li, XL; Jasti, B; Russu, WA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5877-5879 , 文章类型： Article，,卷期：2009年19-20] A model peptide-drug conjugate designed upon a beta-hairpin peptide with the alpha 4 beta 1 integrin recognition sequence LDV appended to the N-terminus and a fluorescent model drug appended to the C-terminus. This model... Synthesis and evaluation of 9-aminoacridines derived from benzyne click chemistry [作者：Howell, LA; Howman, A; O'Connell, MA; Mueller, A; Searcey, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5880-5883 , 文章类型： Article，,卷期：2009年19-20] A small set of 9-aminoacridine-3- and 4-carboxamides were synthesized efficiently using the benzyne/azide click chemistry. The products bind to duplex DNA but have different antitumour activity in the HL60 cell line. (C)... Synthesis and SAR of alkanediamide-linked bisbenzamidines with anti-trypanosomal and anti-pneumocystis activity [作者：Huang, TL; Eynde, JJV; Mayence, A; Collins, MS; Cushion, MT; Rattendi, D; Londono, I; Mazumder, L; Bacchi, CJ; Yarlett, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5884-5886 , 文章类型： Article，,卷期：2009年19-20] A series of alkanediamide-linked bisbenzamidines was synthesized and tested in vitro against a drug-sensitive strain of Trypanosoma brucei brucei, a drug-resistant strain of Trypanosoma brucei rhodesiense and Pneumocysti... Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs) [作者：Burns, CJ; Bourke, DG; Andrau, L; Bu, XY; Charman, SA; Donohue, AC; Fantino, E; Farrugia, M; Feutrill, JT; Joffe, M; Kling, MR; Kurek, M; Nero, TL; Nguyen, T; Palmer, JT; Phillips, I; Shackleford, DM; Sikanyika, H; Styles, M; Su, S; Treutlein, H; Zeng, J; Wilks, AF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5887-5892 , 文章类型： Article，,卷期：2009年19-20] A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl) phen...