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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116条记录   Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappa B inhibitor, DMAPT (LC-1) [作者：Neelakantan, S; Nasim, S; Guzman, ML; Jordan, CT; Crooks, PA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4346-4349 , 文章类型： Article，,卷期：2009年19-15] A series of aminoparthenolide analogs (6-37) were synthesized and evaluated for their anti-leukemic activity. Eight compounds exhibited good anti-leukemic activity with LD50's in the low mu M range (1.5-3.0 mu M). Compou... Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase [作者：Shaw, AN; Tedesco, R; Bambal, R; Chai, DP; Concha, NO; Darcy, MG; Dhanak, D; Duffy, KJ; Fitch, DM; Gates, A; Johnston, VK; Keenan, RM; Lin-Goerke, J; Liu, NN; Sarisky, RT; Wiggall, KJ; Zimmerman, MN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4350-4353 , 文章类型： Article，,卷期：2009年19-15] The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in ... Synthesis and biological activity of heteroaryl 3-(1,1-dioxo-2H-(1,2,4)-benzothiadizin-3-yl)-4-hydroxy-2(1H)-quinolinone derivatives as hepatitis C virus NS5B polymerase inhibitors [作者：Tedesco, R; Chai, DP; Darcy, MG; Dhanak, D; Fitch, DM; Gates, A; Johnston, VK; Keenan, RM; Lin-Goerke, J; Sarisky, RT; Shaw, AN; Valko, KL; Wiggall, KJ; Zimmerman, MN; Duffy, KJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4354-4358 , 文章类型： Article，,卷期：2009年19-15] Modification of the benzo rings of 3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones into heteroaromatic systems was investigated to enhance physicochemical properties and potency pro. le of this... Metal ion CHElate-aSSisted LIGAtion (CHESS LIGA) for SNP detection on microarrays [作者：Hien, LT; Oretskaya, TS; Zatsepin, TS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4018-4021 , 文章类型： Article，,卷期：2009年19-15] We developed a metal ion chelate-assisted ligation for SNP detection by microarray. An oligonucleotide probe was separated into two 9-10-mers bearing iminodiacetic residues at the gap point. Duplex formation with the DNA... The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists [作者：Lunniss, GE; Barnes, AA; Barton, N; Biagetti, M; Bianchi, F; Blowers, SM; Caberlotto, L; Emmons, A; Holmes, IP; Montanari, D; Norris, R; Walters, DJ; Watson, SP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4022-4025 , 文章类型： Article，,卷期：2009年19-15] A novel small molecule NPY Y2 antagonist (3) identified from high throughput screening is described. A subsequent SAR study and optimisation programme based around this molecule is also described, leading to the identifi... Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors [作者：Sablone, MR; Cesta, MC; Moriconi, A; Aramini, A; Bizzarri, C; Di Giacinto, C; Di Bitondo, R; Gloaguen, I; Aschi, M; Crucianelli, M; Bertini, R; Allegretti, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4026-4030 , 文章类型： Article，,卷期：2009年19-15] We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological ac... Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors [作者：Denhart, DJ; Deskus, JA; Ditta, JL; Gao, Q; King, HD; Kozlowski, ES; Meng, Z; LaPaglia, MA; Mattson, GK; Molski, TF; Taber, MT; Lodge, NJ; Mattson, RJ; Macor, JE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4031-4033 , 文章类型： Article，,卷期：2009年19-15] A series of racemic 3-(trans-2-aminomethylcyclopentyl)indoles was synthesized and found to have potent binding to the human serotonin transporter (hSERT). The most active analog was synthesized stereospecifically and the... Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors [作者：Shi, Y; Zhang, J; Shi, MX; O'Connor, SP; Bisaha, SN; Li, C; Sitkoff, D; Pudzianowski, AT; Chong, S; Klei, HE; Kish, K; Yanchunas, J; Liu, ECK; Hartl, KS; Seiler, SM; Steinbacher, TE; Schumacher, WA; Atwal, KS; Stein, PD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4034-4041 , 文章类型： Article，,卷期：2009年19-15] The N,N'-disubstituted cyanoguanidine is an excellent bioisostere of the thiourea and ketene aminal functional groups. We report the design and synthesis of a novel class of cyanoguanidine-based lactam derivatives as pot... Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha 6*subtype [作者：Breining, SR; Bencherif, M; Grady, SR; Whiteaker, P; Marks, MJ; Wageman, CR; Lester, HA; Yohannes, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4359-4363 , 文章类型： Article，,卷期：2009年19-15] Direct comparison of pyridine versus pyrimidine substituents on a small but diverse set of ligands indicates that the pyrimidine substitution has the potential to enhance affinity and/or functional activity at alpha 6 su... Effect of varying chain length between P-1 and P-1 ' position of tripeptidomimics on activity of angiotensin-converting enzyme inhibitors [作者：Chaudhary, S; Vats, ID; Chopra, M; Biswas, P; Pasha, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4364-4366 , 文章类型： Article，,卷期：2009年19-15] One of the efficient modes of treatments of chronic hypertension and cardiovascular disorders has been to restrain the formation of angiotensin-II by inhibiting the action of angiotensin-converting enzyme (ACE) on angiot... Antitumor activity of deoxypodophyllotoxin isolated from Anthriscus sylvestris: Induction of G2/M cell cycle arrest and caspase-dependent apoptosis [作者：Yong, Y; Shin, SY; Lee, YH; Lim, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4367-4371 , 文章类型： Article，,卷期：2009年19-15] An active compound having antitumor activity was isolated from the root of Anthriscus sylvestris. Structural studies revealed that it was deoxypodophyllotoxin (DPPT), and its biological activity was evaluated in HeLa hum... Structure-based virtual screening approach to identify novel classes of Cdc25B phosphatase inhibitors [作者：Park, H; Li, M; Choi, J; Cho, H; Ham, SW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4372-4375 , 文章类型： Article，,卷期：2009年19-15] Discovery of Cdc25B phosphatase inhibitors has been actively pursued with the aim to develop anticancer agents. We have been able to identify eight novel Cdc25B inhibitors by means of a computer-aided drug design protoco... Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors [作者：Branca, D; Cerretani, M; Jones, P; Koch, U; Orvieto, F; Palumbi, MC; Rowley, M; Toniatti, C; Muraglia, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4042-4045 , 文章类型： Article，,卷期：2009年19-15] PARP inhibitors have been demonstrated to retard intracellular DNA repair and therefore sensitize tumor cells to cytotoxic agents or ionizing radiation. We report the identification of a novel class of PARP1 inhibitors, ... Assessment of new 2 '-O-acetalester protecting groups for regular RNA synthesis and original 2 '-modified proRNA [作者：Martin, AR; Lavergne, T; Vasseur, JJ; Debart, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4046-4049 , 文章类型： Article，,卷期：2009年19-15] New base-labile acyloxymethyl groups were evaluated to protect 2'-OH functions of ribonucleotides for regular RNA synthesis in order to shorten the deprotection procedure upon ammonia. These same acetalester groups were ... Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1) [作者：Miyashiro, J; Woods, KW; Park, CH; Liu, X; Shi, Y; Johnson, EF; Bouska, JJ; Olson, AM; Luo, Y; Fry, EH; Giranda, VL; Penning, TD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4050-4054 , 文章类型： Article，,卷期：2009年19-15] Based on screening hit 1, a series of tricyclic quinoxalinones have been designed and evaluated for inhibition of PARP-1. Substitutions at the 7- and 8-positions of the quinoxalinone ring led to a number of compounds wit... Ionic interactions for substituted MCH1R inhibitors studied by pK(a) values [作者：Lee, JY; Lee, H; Lim, JY; Yoo, SE; Kang, NS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4376-4379 , 文章类型： Article，,卷期：2009年19-15] MCH1R inhibitors with the quinoline moiety having the aromatic amine and aliphatic amine chain were selected, and then the effect of substituents of the quinoline ring on the ionic interaction were studied by calculating...