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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34条记录   A scaffold hopping approach to identify novel monoamine oxidase B inhibitors [作者：Geldenhuys, WJ; Funk, MO; Van der Schyf, CJ; Carroll, RT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1380-1383 , 文章类型： Article，,卷期：2012年22-3] Monoamine oxidase B (MAO-B) inhibitors are used to treat Parkinson's disease. In this study, we searched for novel MAO-B inhibitors using a scaffold hopping approach based on our experience with the thiazolidinedione (TZ... Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2) [作者：Yang, MG; Xiao, ZL; Shi, Q; Cherney, RJ; Tebben, AJ; De Lucca, GV; Santella, JB; Mo, RW; Cvijic, ME; Zhao, QH; Barrish, JC; Carter, PH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1384-1387 , 文章类型： Article，,卷期：2012年22-3] We report the synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamides (4) as CCR2 inhibitors for the potential treatment of inflammatory diseases. Several of the compounds display nanomolar binding affinity for CCR... Novel dendrimeric lipopeptides with antifungal activity [作者：Janiszewska, J; Sowinska, M; Rajnisz, A; Solecka, J; Lacka, I; Milewski, S; Urbanczyk-Lipkowska, Z,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1388-1393 , 文章类型： Article，,卷期：2012年22-3] A series of new cationic lipopeptides containing branched, amphiphilic polar head derived from (Lys)Lys(Lys) dendron and C-8 or C-12 chain at C-end were designed, synthesized and characterized. Antimicrobial in vitro act... Discovery of GS-9256: A novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity [作者：Sheng, XC; Casarez, A; Cai, R; Clarke, MO; Chen, XW; Cho, A; Delaney, WE; Doerffler, E; Ji, MZ; Mertzman, M; Pakdaman, R; Pyun, HJ; Rowe, T; Wu, QY; Xu, J; Kim, CU,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1394-1396 , 文章类型： Article，,卷期：2012年22-3] A potent and novel class of phosphinic acid derived product-like inhibitors of the HCV NS3/4A protease was discovered previously. Modification of the phosphinic acid and quinoline heterocycle led to GS-9256 with potent c... Design and synthesis of boronic acid inhibitors of endothelial lipase [作者：O'Connell, DP; LeBlanc, DF; Cromley, D; Billheimer, J; Rader, DJ; Bachovchin, WW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1397-1401 , 文章类型： Article，,卷期：2012年22-3] Endothelial lipase (EL) and lipoprotein lipase (LPL) are homologous lipases that act on plasma lipoproteins. EL is predominantly a phospholipase and appears to be a key regulator of plasma HDL-C. LPL is mainly a triglyce... Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: Significance of the para-hydroxyl orientation [作者：Baskin, R; Gali, M; Park, SO; Zhao, ZJ; Keseru, GM; Bisht, KS; Sayeski, PP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1402-1407 , 文章类型： Article，,卷期：2012年22-3] In this study, we analyzed the structure-activity relationship properties of the small molecule Jak2 inhibitor G6. We synthesized a set of derivatives containing the native para-hydroxyl structure or an alternative meta-... The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not a beta-secretase inhibitor [作者：Cheng, XR; Zhou, JW; Zhou, Y; Cheng, JP; Yang, RF; Zhou, WX; Zhang, YX; Yun, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1408-1414 , 文章类型： Article，,卷期：2012年22-3] (2)-Epigallocatechin-3-gallate (EGCG) is a major polyphenolic component of green tea. A number of studies have demonstrated EGCG has the possibility for delaying the onset or retarding the progression of Alzheimer's dise... Synthesis and antiviral activities of novel gossypol derivatives [作者：Yang, J; Zhang, F; Li, JR; Chen, G; Wu, SW; Ouyang, WJ; Pan, W; Yu, R; Yang, JX; Tien, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1415-1420 , 文章类型： Article，,卷期：2012年22-3] In this study, a series of novel gossypol derivatives were synthesized and screened in vitro for their anti-HIV-1 and anti-H5N1 activities, respectively. Replacing the aldehyde groups of gossypol with some amino acids no... Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: Identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test [作者：Tripathy, R; McHugh, RJ; Bacon, ER; Salvino, JM; Morton, GC; Aimone, LD; Huang, Z; Mathiasen, JR; DiCamillo, A; Huffman, MJ; McKenna, BA; Kopec, K; Lu, LD; Qian, J; Angeles, TS; Connors, T; Spais, C; Holskin, B; Duzic, E; Schaffhauser, H; Rosse, GC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1421-1426 , 文章类型： Article，,卷期：2012年22-3] Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine(6) (5-HT6) receptor antagonists show beneficial effect on cognition in several ... Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury [作者：Krenitsky, VP; Delgado, M; Nadolny, L; Sahasrabudhe, K; Ayala, L; Clareen, SS; Hilgraf, R; Albers, R; Kois, A; Hughes, K; Wright, J; Nowakowski, J; Sudbeck, E; Ghosh, S; Bahmanyar, S; Chamberlain, P; Muir, J; Cathers, BE; Giegel, D; Xu, L; Celeridad, M; Moghaddam, M; Khatsenko, O; Omholt, P; Katz, J; Pai, S; Fan, R; Tang, Y; Shirley, MA; Benish, B; Blease, K; Raymon, H; Bhagwat, S; Henderson, I; Cole, AG; Bennett, B; Satoh, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1427-1432 , 文章类型： Article，,卷期：2012年22-3] In this Letter we describe the optimization of an aminopurine lead (1) with modest potency and poor overall kinase selectivity which led to the identification of a series of potent, selective JNK inhibitors. Improvement ... Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor [作者：Krenitsky, VP; Nadolny, L; Delgado, M; Ayala, L; Clareen, SS; Hilgraf, R; Albers, R; Hegde, S; D'Sidocky, N; Sapienza, J; Wright, J; McCarrick, M; Bahmanyar, S; Chamberlain, P; Delker, SL; Muir, J; Giegel, D; Xu, L; Celeridad, M; Lachowitzer, J; Bennett, B; Moghaddam, M; Khatsenko, O; Katz, J; Fan, R; Bai, A; Tang, Y; Shirley, MA; Benish, B; Bodine, T; Blease, K; Raymon, H; Cathers, BE; Satoh, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1433-1438 , 文章类型： Article，,卷期：2012年22-3] In this Letter we describe the discovery of potent, selective, and orally active aminopurine JNK inhibitors. Improving the physico-chemical properties as well as increasing the potency and selectivity of a subseries with... Synthesis and neurite growth evaluation of new analogues of honokiol, a neolignan with potent neurotrophic activity [作者：Kumar, VP; Reddy, RG; Vo, DD; Chakravarty, S; Chandrasekhar, S; Gree, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1439-1444 , 文章类型： Article，,卷期：2012年22-3] A versatile synthetic route is reported towards the preparation of new analogues for potent neurotrophic agent biaryl-type lignan honokiol. A focused 24-membered library of derivatives containing five different groups at... Development of an efficient method for phosphorodiamidate bond formation by using inorganic salts [作者：Harakawa, T; Tsunoda, H; Ohkubo, A; Seio, K; Sekine, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1445-1447 , 文章类型： Article，,卷期：2012年22-3] Phosphorodiamidate morpholino oligonucleotides (PMOs) have been extensively applied in antisense strategies for gene regulation because of their high stability in serum and low toxicity. However, chain elongation of PMOs... Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein [作者：Edink, E; Akdemir, A; Jansen, C; van Elk, R; Zuiderveld, O; de Kanter, FJJ; van Muijlwijk-Koezen, JE; Smit, AB; Leurs, R; de Esch, IJP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1448-1454 , 文章类型： Article，,卷期：2012年22-3] Using structure-based optimization procedures on in silico hits, dibenzosuberyl- and benzoate substituted tropines were designed as ligands for acetylcholine-binding protein (AChBP). This protein is a homolog to the liga... Novel synthetic methods for N-cyano-1H-imidazole-4-carboxamides and their fungicidal activity [作者：Yang, WC; Li, J; Li, J; Chen, Q; Yang, GF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1455-1458 , 文章类型： Article，,卷期：2012年22-3] A novel synthetic method of N-cyanocarboxamides has been developed with advantages of mild reaction condition, simpler procedure and easy reactant-product isolation compared with the existing methods. Using this novel me... Cinobufacini induced MDA-MB-231 cell apoptosis-associated cell cycle arrest and cytoskeleton function [作者：Ma, LN; Song, B; Jin, H; Pi, J; Liu, L; Jiang, JH; Cai, JY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1459-1463 , 文章类型： Article，,卷期：2012年22-3] Cinobufacini is a traditional Chinese anti-tumor drug and widely used in clinic experiences. But little is known about its effect on the cells. In this study, the effects of cinobufacini on breast cancer MDA-MB-231 cell ...