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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62条记录   Oleanane-type triterpenoids from Panax stipuleanatus and their anticancer activities [作者：Liang, C; Ding, Y; Nguyen, HT; Kim, JA; Boo, HJ; Kang, HK; Mahn, CN; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7110-7115 , 文章类型： Article，,卷期：2010年20-23] One newly (1) and 10 known oleanane-type triterpenoids (2-11) were isolated from the methanol extract of Panax stipuleanatus rhizomes. Based on their spectroscopic data, these compounds were identified as spinasaponin A ... N-Substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators [作者：Thewlis, KM; Aldegheri, L; Harries, MH; Mookherjee, C; Oliosi, B; Ward, SE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7116-7119 , 文章类型： Article，,卷期：2010年20-23] A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesi... Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists [作者：Pizzi, DA; Leslie, CP; Mazzali, A; Seri, C; Biagetti, M; Bentley, J; Genski, T; Di Fabio, R; Contini, S; Sabbatini, FM; Zonzini, L; Caberlotto, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7120-7123 , 文章类型： Article，,卷期：2010年20-23] A novel class of benzimidazole NPY Y5 receptor antagonists was prepared exploiting a privileged spirocarbamate moiety. The structure-activity relationship of this series and efforts to achieve a profile suitable for furt... A targeted low molecular weight near-infrared fluorescent probe for prostate cancer [作者：Liu, TC; Wu, LY; Hopkins, MR; Choi, JK; Berkman, CE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7124-7126 , 文章类型： Article，,卷期：2010年20-23] Prostate-specific membrane antigen (PSMA) remains an active target for imaging and therapeutic applications for prostate cancer. Although radionuclide-based imaging is generally more sensitive and also has been deeply ex... Neo-tanshinlactone inspired synthesis, in vitro evaluation of novel substituted benzocoumarin derivatives as potent anti-breast cancer agents [作者：Sashidhara, KV; Rosaiah, JN; Kumar, M; Gara, RK; Nayak, LV; Srivastava, K; Bid, HK; Konwar, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7127-7131 , 文章类型： Article，,卷期：2010年20-23] A small library of novel benzocoumarin derivatives based on naturally occurring neo-tanshinlactone scaffold was constructed and their antiproliferative activities against breast cancer cells MCF-7 and MDA-MB-231 were eva... Synthesis and structure-activity relationships of tyrosine-based inhibitors of autotaxin (ATX) [作者：East, JE; Kennedy, AJ; Tomsig, JL; De Leon, AR; Lynch, KR; Macdonald, TL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7132-7136 , 文章类型： Article，,卷期：2010年20-23] Autotaxin (ATX) is a secreted soluble enzyme that generates lysophosphatidic acid (LPA) through its lysophospholipase D activity. Because of LPA's role in neoplastic diseases, ATX is an attractive therapeutic target due ... Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists [作者：Hawryluk, NA; Merit, JE; Lebsack, AD; Branstetter, BJ; Hack, MD; Swanson, N; Ao, H; Maher, MP; Bhattacharya, A; Wang, Q; Freedman, JM; Scott, BP; Wickenden, AD; Chaplan, SR; Breitenbucher, JG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7137-7141 , 文章类型： Article，,卷期：2010年20-23] Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identi... 1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties [作者：Lebsack, AD; Rech, JC; Branstetter, BJ; Hawryluk, NA; Merit, JE; Allison, B; Rynberg, R; Buma, J; Rizzolio, M; Swanson, N; Ao, H; Maher, MP; Herrmann, M; Freedman, J; Scott, BP; Luo, L; Bhattacharya, A; Wang, Q; Chaplan, SR; Wickenden, AD; Breitenbucher, JG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7142-7146 , 文章类型： Article，,卷期：2010年20-23] Based upon a previously reported lead compound 1, a series of 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines were synthesized and evaluated for improved physiochemical and pharmacokinetic pr... Synthesis, antioxidant and toxicological study of novel pyrimido quinoline derivatives from 4-hydroxy-3-acyl quinolin-2-one [作者：Sankaran, M; Kumarasamy, C; Chokkalingam, U; Mohan, PS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7147-7151 , 文章类型： Article，,卷期：2010年20-23] A series of novel pyrimido and other fused quinoline derivatives like 4-methyl pyrimido [5,4-c]quinoline-2,5(1H,6H)-dione (4a), 4-methyl-2-thioxo-1,2-dihydropyrimido [5,4-c]quinoline-5(6H)-one (4b), 2-amino-4-methyl-1,2-... Highly brominated metabolites from marine red alga Laurencia similis inhibit protein tyrosine phosphatase 1B [作者：Qin, JC; Su, H; Zhang, YM; Gao, JM; Zhu, L; Wu, XA; Pan, HY; Li, XA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7152-7154 , 文章类型： Article，,卷期：2010年20-23] Five new highly brominated metabolites, 3',5',6',6-tetrabromo-2,4-dimethyldiphenyl ether (1), 1,2,5-tribromo-3-bromoamino-7-bromomethylnaphthalene (2), 2,5,8-tribromo-3-bromoamino-7-bromomethylnaphthalene (3), 2,5,6-trib... Synthetic analogs of indole-containing natural products as inhibitors of sortase A and isocitrate lyase [作者：Lee, YJ; Han, YR; Park, W; Nam, SH; Oh, KB; Lee, HS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6882-6885 , 文章类型： Article，,卷期：2010年20-23] Guided by the inhibitory activities of indole-containing natural products against isocitrate lyase (ICL) from Candida albicans and sortase A (SrtA) from Staphylococcus aureus, a series of compounds structurally analogous... 5-Amino-pyrazoles as potent and selective p38 alpha inhibitors [作者：Das, J; Moquin, RV; Dyckman, AJ; Li, TL; Pitt, S; Zhang, R; Shen, DR; McIntyre, KW; Gillooly, K; Doweyko, AM; Newitt, JA; Sack, JS; Zhang, HJ; Kiefer, SE; Kish, K; McKinnon, M; Barrish, JC; Dodd, JH; Schieven, GL; Leftheris, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6886-6889 , 文章类型： Article，,卷期：2010年20-23] The synthesis and structure-activity relationships (SAR) of p38 alpha MAP kinase inhibitors based on a 5-amino-pyrazole scaffold are described. These studies led to the identification of compound 2j as a potent and selec... Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors [作者：Cai, JQ; Robinson, J; Belshaw, S; Everett, K; Fradera, X; van Zeeland, M; van Berkom, L; van Rijnsbergen, P; Popplestone, L; Baugh, M; Dempster, M; Bruin, J; Hamilton, W; Kinghorn, E; Westwood, P; Kerr, J; Rankovic, Z; Arbuckle, W; Bennett, DJ; Jones, PS; Long, C; Martin, I; Uitdehaag, JCM; Meulemans, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6890-6894 , 文章类型： Article，,卷期：2010年20-23] The trifluoromethylphenyl P2 motif from previously reported heteroarylnitrile series has been successfully applied for the design and synthesis of highly potent novel ketoamide-based cathepsin S inhibitors. The key in th... The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: The first clinical candidate [作者：Wang, JL; Carter, J; Kiefer, JR; Kurumbail, RG; Pawlitz, JL; Brown, D; Hartmann, SJ; Graneto, MJ; Seibert, K; Talley, JJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7155-7158 , 文章类型： Article，,卷期：2010年20-23] In this manuscript, we report the discovery of the substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors. 5c-(S) (SD-8381) was advanc... The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: The second clinical candidate having a shorter and favorable human half-life [作者：Wang, JL; Limburg, D; Graneto, MJ; Springer, J; Hamper, JRB; Liao, SB; Pawlitz, JL; Kurumbail, RG; Maziasz, T; Talley, JJ; Kiefer, JR; Carter, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7159-7163 , 文章类型： Article，,卷期：2010年20-23] In this Letter, we provide the structure-activity relationships, optimization of design, testing criteria, and human half-life data for a series of selective COX-2 inhibitors. During the course of our structure-based dru... The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part III: The three microdose candidates [作者：Wang, JL; Aston, K; Limburg, D; Ludwig, C; Hallinan, AE; Koszyk, F; Hamper, B; Brown, D; Graneto, M; Talley, J; Maziasz, T; Masferrer, J; Carter, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7164-7168 , 文章类型： Article，,卷期：2010年20-23] In this manuscript, we report the discovery of the substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors. We provide the structure-ac...