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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71条记录   Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant [作者：Thomas, M; Huang, WS; Wen, D; Zhu, XT; Wang, YH; Metcalf, CA; Liu, SY; Chen, I; Romero, J; Zou, D; Sundaramoorthi, R; Li, F; Qi, JW; Cai, LS; Zhou, TJ; Commodore, L; Xu, QH; Keats, J; Wang, F; Wardwell, S; Ning, YY; Snodgrass, JT; Broudy, MI; Russian, K; Iuliucci, J; Rivera, VM; Sawyer, TK; Dalgarno, DC; Clackson, T; Shakespeare, WC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3743-3748 , 文章类型： Article，,卷期：2011年21-12] Ponatinib (AP24534) was previously identified as a pan-BCR-ABL inhibitor that potently inhibits the T315I gatekeeper mutant, and has advanced into clinical development for the treatment of refractory or resistant CML. In... Identification and synthesis of N '-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase [作者：Liang, ZJ; Zhang, DY; Ai, J; Chen, LM; Wang, HS; Kong, XQ; Zheng, MY; Liu, H; Luo, C; Geng, MY; Jiang, HL; Chen, KX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3749-3754 , 文章类型： Article，,卷期：2011年21-12] A series of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives were identified as moderately potent inhibitors against c-Met kinase by pharmacophore-based virtual screening and chemical synthesis methods. The structure-act... Design, synthesis, and evaluation of bromo-retrochalcone derivatives as protein tyrosine phosphatase 1B inhibitors [作者：Liu, Z; Lee, W; Kim, SN; Yoon, G; Cheon, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3755-3758 , 文章类型： Article，,卷期：2011年21-12] A series of bromo-retrochalcones was designed, synthesized and evaluated as PTP1B inhibitors based on licochalcone A and E. Compounds 6, 12, 13, 14, 25, 36, 37, 39, and 41 showed potent inhibitory effects against PTP1B, ... Glucosides with cyclic diarylpolynoid as novel C-aryl glucoside SGLT2 inhibitors [作者：Kang, SY; Kim, MJ; Lee, JS; Lee, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3759-3763 , 文章类型： Article，,卷期：2011年21-12] Novel C-aryl glucoside SGLT2 inhibitors containing cyclic diarylpolynoid motif were designed and synthesized for biological evaluation. Alkylzinc bromides have been efficiently prepared by the direct insertion of zinc me... Part 1: N-Alkylated glycines as potent alpha(2)delta ligands [作者：Thompson, LR; Blakemore, DC; Brugier, D; Bryans, JS; Chu, WLA; Maw, GN; Poinsard, C; Rawson, DJ; Warren, AN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3764-3766 , 文章类型： Article，,卷期：2011年21-12] A new series of glycine-derived ligands of the alpha(2)delta subunit of voltage gated calcium channels is described. Several novel compounds (7) based on (6) were prepared that possessed a potency <100 nM in the alpha(2)... Part 2: Design, synthesis and evaluation of hydroxyproline-derived alpha(2)delta ligands [作者：Rawson, DJ; Brugier, D; Harrison, A; Hough, J; Newman, J; Otterburn, J; Maw, GN; Price, J; Thompson, LR; Turnpenny, P; Warren, AN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3767-3770 , 文章类型： Article，,卷期：2011年21-12] Conformational constraint has been used to design a potent series of alpha(2)delta ligands derived from the readily available starting material (2S,4R)-hydroxy-L-proline. The ligands have improved physicochemistry and po... Part 3: Design and synthesis of proline-derived alpha(2)delta ligands [作者：Rawson, DJ; Brugier, D; Harrison, A; Hough, J; Newman, J; Otterburn, J; Maw, GN; Price, J; Thompson, LR; Turnpenny, P; Warren, AN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3771-3773 , 文章类型： Article，,卷期：2011年21-12] A potent series of substituted (2S,4S)-benzylproline alpha(2)delta ligands have been designed from the readily available starting material (2S,4R)-hydroxy-L-proline. The ligands have improved pharmacokinetic profile over... Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors [作者：Du, XH; Lizarzaburu, M; Turcotte, S; Lee, T; Greenberg, J; Shan, B; Fan, P; Ling, Y; Medina, JC; Houze, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3774-3779 , 文章类型： Article，,卷期：2011年21-12] Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharma... Novel C8-linked pyrrolobenzodiazepine (PBD)-heterocycle conjugates that recognize DNA sequences containing an inverted CCAAT box [作者：Brucoli, F; Hawkins, RM; James, CH; Wells, G; Jenkins, TC; Ellis, T; Hartley, JA; Howard, PW; Thurston, DE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3780-3783 , 文章类型： Article，,卷期：2011年21-12] A series of novel DNA-interactive C8-linked pyrrolobenzodiazepine (PBD)-heterocyclepolyamide conjugates has been synthesised to explore structure/sequence-selectivity relationships. One conjugate (2d) has a greater selec... Novel diarylheptanoids as inhibitors of TNF-alpha production [作者：Dhuru, S; Bhedi, D; Gophane, D; Hirbhagat, K; Nadar, V; More, D; Parikh, S; Dalal, R; Fonseca, LC; Kharas, F; Vadnal, PY; Vishwakarma, RA; Sivaramakrishnan, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3784-3787 , 文章类型： Article，,卷期：2011年21-12] Synthesis and anti-inflammatory activity of novel diarylheptanoids [5-hydroxy-1-phenyl-7-(pyridin-3-yl)-heptan-3-ones and 1-phenyl-7-(pyridin-3-yl)hept-4-en-3-ones] as inhibitors of tumor necrosis factor-alpha (TNF-alpha... Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors [作者：Kinoshita, K; Ono, Y; Emura, T; Asoh, K; Furuichi, N; Ito, T; Kawada, H; Tanaka, S; Morikami, K; Tsukaguchi, T; Sakamoto, H; Tsukuda, T; Oikawa, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3788-3793 , 文章类型： Article，,卷期：2011年21-12] Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered a promising therapeutic target for human cancers. We identified novel tetracyclic derivatives as potent ALK inhibitors. Among them, compound 27 show... Three new cytotoxic aryltetralin lignans from Sinopodophyllum emodi [作者：Sun, YJ; Li, ZL; Chen, H; Liu, XQ; Zhou, W; Hua, HM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3794-3797 , 文章类型： Article，,卷期：2011年21-12] Three new aryltetralin lignans, 4-acetyl-4-demethyl-podophyllotoxin (1) and sinolignans A, B (2-3), and two new natural products (4-5), were isolated from the roots and rhizomes of Sinopodophyllum emodi together with twe... Synthesis and spectroscopic characterization of 4-butoxyethoxy-N-octadecyl-1,8-naphthalimide as a new fluorescent probe for the determination of proteins [作者：Sun, Y; Wei, S; Yin, C; Liu, LS; Hu, CM; Zhao, YY; Ye, YX; Hu, XY; Fan, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3798-3804 , 文章类型： Article，,卷期：2011年21-12] A novel 4-butoxyethoxy-N-octadecyl-1,8-naphthalimide (BON) was synthesized as a fluorescent probe for the determination of proteins. The interactions between BON and bovine serum albumin (BSA) were studied by fluorescenc... Synthesis and SAR development of novel P2X(7) receptor antagonists for the treatment of pain: Part 1 [作者：Matasi, JJ; Brumfield, S; Tulshian, D; Czarnecki, M; Greenlee, W; Garlisi, CG; Qiu, HC; Devito, K; Chen, SC; Sun, YL; Bertorelli, R; Geiss, W; Le, VD; Martin, GS; Vellekoop, SA; Haber, J; Allard, ML,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3805-3808 , 文章类型： Article，,卷期：2011年21-12] Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X(7) receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and sel... Discovery of DA-1229: A potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes [作者：Kim, HJ; Kwak, WY; Min, JP; Lee, JY; Yoon, TH; Kim, HD; Shin, CY; Kim, MK; Choi, SH; Kim, HS; Yang, EK; Cheong, YH; Chae, YN; Park, KJ; Jang, JM; Choi, SJ; Son, MH; Kim, SH; Yoo, M; Lee, BJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3809-3812 , 文章类型： Article，,卷期：2011年21-12] A series of beta-amino amide containing substituted piperazine-2-one derivatives was synthesized and evaluated as inhibitors of dipeptidyl pepdidase-4 (DPP-4) for the treatment of type 2 diabetes. As results of intensive... Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide Vasopressin V(1b) receptor antagonists [作者：Napier, SE; Letourneau, JJ; Ansari, N; Auld, DS; Baker, J; Best, S; Campbell-Wan, L; Chan, R; Craighead, M; Desai, H; Ho, KK; MacSweeney, C; Milne, R; Morphy, JR; Neagu, I; Ohlmeyer, MHJ; Pick, J; Presland, J; Riviello, C; Zanetakos, HA; Zhao, JQ; Webbb, ML,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3813-3817 , 文章类型： Article，,卷期：2011年21-12] Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomol...