个性化文献订阅>文章检索

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57条记录   Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model [作者：Ho, KK; Beasley, JR; Belanger, L; Black, D; Chan, JH; Dunn, D; Hu, B; Klon, A; Kultgen, SG; Ohlmeyer, M; Parlato, SM; Ray, PC; Pham, Q; Rong, YJ; Roughton, AL; Walker, TL; Wright, J; Xu, K; Xu, Y; Zhang, LM; Webb, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6027-6031 , 文章类型： Article，,卷期：2009年19-21] The pro. le of a series of triazine and pyrimidine based ROCK inhibitors is described. An initial binding mode was established based on a homology model and the proposed interactions are consistent with the observed SAR.... Novel orally active morpholine N-arylsulfonamides gamma-secretase inhibitors with low CYP 3A4 liability [作者：Josien, H; Bara, T; Rajagopalan, M; Clader, JW; Greenlee, WJ; Favreau, L; Hyde, LA; Nomeir, AA; Parker, EM; Song, LX; Zhang, LL; Zhang, Q,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6032-6037 , 文章类型： Article，,卷期：2009年19-21] A new class of 2,6-disubstituted morpholine N-arylsulfonamide gamma-secretase inhibitors was designed based on the introduction of a morpholine core in lieu or piperidine in our lead series. This resulted in compounds wi... Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformation [作者：Shi, J; Stover, JS; Whitby, LR; Vogt, PK; Boger, DL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6038-6041 , 文章类型： Article，,卷期：2009年19-21] The preparation and evaluation of a series of inhibitors of Myc/Max dimerization and Myc-induced cell transformation are described providing mycmycin-1 (3) and mycmycin-2 (4). (C) 2009 Elsevier Ltd. All rights reserved. Structure-activity relationship (SAR) studies of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione: Development of potential substrate-specific ERK1/2 inhibitors [作者：Li, QB; Al-Ayoubi, A; Guo, TL; Zheng, H; Sarkar, A; Nguyen, T; Eblen, ST; Grant, S; Kellogg, GE; Zhang, SJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6042-6046 , 文章类型： Article，,卷期：2009年19-21] A series of analogs of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione, a putative substrate-specific ERK1/2 inhibitor, were synthesized and biologically characterized in human leukemia U937 cells to de... 5,5 '- and 6,6 '-Dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase [作者：Ellis, DA; Blazel, JK; Tran, CV; Ruebsam, F; Murphy, DE; Li, LS; Zhao, JJ; Zhou, YF; McGuire, HM; Xiang, AX; Webber, SE; Zhao, Q; Han, Q; Kissinger, CR; Lardy, M; Gobbi, A; Showalter, RE; Shah, AM; Tsan, M; Patel, RA; LeBrun, LA; Kamran, R; Bartkowski, DM; Nolan, TG; Norris, DA; Sergeeva, MV; Kirkovsky, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6047-6052 , 文章类型： Article，,卷期：2009年19-21] The discovery of 5,5 '- and 6,6 '-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of the HCV RNA-dependent RNA polymerase (NS5B) is described. Several of these agents also display potent antiviral activity in ... Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X(7) receptor antagonists [作者：Lee, JY; Yu, J; Cho, WJ; Ko, H; Kim, YC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6053-6058 , 文章类型： Article，,卷期：2009年19-21] Screening of library compounds has yielded pyrazolodiazepine derivatives with P2X(7) receptor antagonist activity. To explore the structure -activity relationships (SAR) of these pyrazolodiazepines as human P2X(7) recept... Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif [作者：Carro, L; Ravina, E; Dominguez, E; Brea, J; Loza, MI; Masaguer, CF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6059-6062 , 文章类型： Article，,卷期：2009年19-21] A series of 8 new tetrahydroquinazolinone derivatives was synthesized and evaluated for binding affinity to D-2 and 5-HT2A human receptors; in addition, some properties related to blood-brain barrier penetration were cal... Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors [作者：Kang, IJ; Wang, LW; Hsu, SJ; Lee, CC; Lee, YC; Wu, YS; Yueh, A; Wang, JC; Hsu, TA; Chao, YS; Chern, JH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6063-6068 , 文章类型： Article，,卷期：2009年19-21] A novel class of arylthiourea HCV inhibitors bearing various functionalities, such as cyclic urea, cyclic thiourea, urea, and thiourea, on the alkyl linker were designed and synthesized. Herein we report the synthesis an... Facile synthesis of anthracene-appended amino acids as highly selective and sensitive fluorescent Fe3+ ion sensors [作者：Lohani, CR; Kim, JM; Lee, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6069-6073 , 文章类型： Article，,卷期：2009年19-21] We designed new fluorescent chemical sensors for Fe3+ ion detection, by conjugating amino acids as receptors into an anthracene fluorophore. The conjugates were synthesized in solid phase by Fmoc-chemistry. Fluorescence ... Synthesis and evaluation of (S,S)-N,N '-bis-[3-(2,2 ',6,6 '-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity [作者：Zhang, XL; Hu, YW; Chen, SD; Luo, RS; Yue, J; Zhang, Y; Duan, WH; Wang, HH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6074-6077 , 文章类型： Article，,卷期：2009年19-21] In order to identify new and potent candidate drugs to treat tuberculosis, a library of compounds was screened, and (S,S)-N,N '-bis-[3-(2,2 ',6,6 '-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) was ... Phytochemical investigation of labdane diterpenes from the rhizomes of Hedychium spicatum and their cytotoxic activity [作者：Reddy, PP; Rao, RR; Shashidhar, J; Sastry, BS; Rao, JM; Babu, KS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6078-6081 , 文章类型： Article，,卷期：2009年19-21] A comprehensive reinvestigation of chemical constituents from the rhizomes of Hedychium spicatum led to the isolation of two new labdane-type diterpene (1, 2), together with six known compounds (3-8). Their structures we... Cellular signal-specific peptide substrate is essential for the gene delivery system responding to cellular signals [作者：Kang, JH; Toita, R; Tomiyama, T; Oishi, J; Asai, D; Mori, T; Niidome, T; Katayama, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6082-6086 , 文章类型： Article，,卷期：2009年19-21] Recently, there is a growing interest in the intracellular signal-targeting gene therapy or diagnosis, mainly by using the reaction of targeting enzymes with peptide substrates. In the present study, we proved the import... A dynamic target-based pharmacophoric model mapping the CD4 binding site on HIV-1 gp120 to identify new inhibitors of gp120-CD4 protein-protein interactions [作者：Caporuscio, F; Tafi, A; Gonzalez, E; Manetti, F; Este, JA; Botta, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6087-6091 , 文章类型： Article，,卷期：2009年19-21] A dynamic target-based pharmacophoric model mapping the CD4 binding site on HIV-1 gp120 was built and used to identify new hits able to inhibit gp120-CD4 protein-protein interactions. Two compounds showed micromolar inhi... Hydrogen sulfide induces nitric oxide release from nitrite [作者：Grossi, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6092-6094 , 文章类型： Article，,卷期：2009年19-21] Hydrogen sulfide has recently been considered to have an important role as a gasotransmitter in the cardiovascular system as well as in the central nervous system, but its action seems directly related to the presence of... Isolation of the protein tyrosine phosphatase 1B inhibitory metabolite from the marine-derived fungus Cosmospora sp SF-5060 [作者：Seo, C; Sohn, JH; Oh, H; Kim, BY; Ahn, JS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6095-6097 , 文章类型： Article，,卷期：2009年19-21] In the course of bioassay-guided study on the EtOAc extract of a culture broth of the marine-derived fungus Cosmospora sp. SF-5060, aquastatin A (1) was isolated as a protein tyrosine phosphatase 1B (PTP1B) inhibitory co... Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases [作者：Enkvist, E; Kriisa, M; Roben, M; Kadak, G; Raidaru, G; Uri, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6098-6101 , 文章类型： Article，,卷期：2009年19-21] Previously reported structural fragments that associate with the ATP-binding pocket of basophilic protein kinases were conjugated with D-arginine-containing peptides. Inhibitory potency of the resulting bisubstrate-analo...