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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45条记录   Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity [作者：Yanagita, RC; Kamachi, H; Tanaka, K; Murakami, A; Nakagawa, Y; Tokuda, H; Nagai, H; Irie, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6064-6066 , 文章类型： Article，,卷期：2010年20-20] The 18-deoxy derivative (3) of a simplified analogue (1) of aplysiatoxin with antiproliferative activity was synthesized to examine the role of the phenolic hydroxyl group at position 18 in the biological activities of 1... Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases [作者：Wang, GT; Mantei, RA; Hubbard, RD; Wilsbacher, JL; Zhang, QA; Tucker, L; Hu, XM; Kovar, P; Johnson, EF; Osterling, DJ; Bouska, J; Wang, JY; Davidsen, SK; Bell, RL; Sheppard, GS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6067-6071 , 文章类型： Article，,卷期：2010年20-20] This Letter describes the lead discovery, optimization, and biological characterization of a series of substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as potent inhibitors of IGF1R, EGFR, and ErbB2. The leading compoun... Synthesis of biologically active biotinylated muramyl dipeptides [作者：Grimes, CL; Podolsky, DK; O'Shea, EK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6061-6063 , 文章类型： Article，,卷期：2010年20-20] Muramyl dipeptide (MDP) is believed to interact with an innate immune receptor, Nod2. To identify the cellular receptor for MDP, we have synthesized biotinylated MDP isomers and tested the ability of these compounds to a... A novel series of positive modulators of the AMPA receptor: Structure- based lead optimization [作者：Jamieson, C; Campbell, RA; Cumming, IA; Gillen, KJ; Gillespie, J; Kazemier, B; Kiczun, M; Lamont, Y; Lyons, AJ; Maclean, JKF; Martin, F; Moir, EM; Morrow, JA; Pantling, J; Rankovic, Z; Smith, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6072-6075 , 文章类型： Article，,卷期：2010年20-20] Starting from lead compound 1, we demonstrate how X-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bio... Validated predictive QSAR modeling of N-aryl-oxazolidinone-5-carboxamides for anti-HIV protease activity [作者：Halder, AK; Jha, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6082-6087 , 文章类型： Article，,卷期：2010年20-20] Validated predictive QSAR modeling was done on some N-aryl-oxazolidinone-5-carboxamides for higher anti-HIV protease activities. Stepwise regression developed significant models showing importance of atom based descripto... Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities [作者：Tang, HF; Yan, Y; Feng, Z; de Jesus, RK; Yang, LH; Levorse, DA; Owens, KA; Akiyama, TE; Bergeron, R; Castriota, GA; Doebber, TW; Ellsworth, KP; Lassman, ME; Li, C; Wu, MS; Zhang, BB; Chapman, KT; Mills, SG; Berger, JP; Pasternak, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6088-6092 , 文章类型： Article，,卷期：2010年20-20] A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs caused dose-dependent decreases in food intake and body weigh... Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease [作者：Korabecny, J; Musilek, K; Holas, O; Binder, J; Zemek, F; Marek, J; Pohanka, M; Opletalova, V; Dohnal, V; Kuca, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6093-6095 , 文章类型： Article，,卷期：2010年20-20] All approved drugs for Alzheimer disease (AD) in clinical practice ameliorate the symptoms of the disease. Among them, acetylcholinesterase inhibitors (AChEIs) are used to increase the cholinergic activity. Among new ACh... The selected flavonol glycoside derived from Sophorae Flos improves glucose uptake and inhibits adipocyte differentiation via activation AMPK in 3T3-L1 cells [作者：Do, TH; Trinh, NT; Tran, TP; Yim, N; Chen, QC; Bae, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6076-6081 , 文章类型： Article，,卷期：2010年20-20] Among nine flavonols (1-9) obtained from Sophorae Flos, we first isolated compounds 4, 5, 8, and 9. These isolates (1-9) were evaluated for the phosphorylation of AMPK and ACC. Administered at 10 mu M, 9 possessed high p... Novel dihydropyrimidines as a potential new class of antitubercular agents [作者：Trivedi, AR; Bhuva, VR; Dholariya, BH; Dodiya, DK; Kataria, VB; Shah, VH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6100-6102 , 文章类型： Article，,卷期：2010年20-20] A small library of 30 dihydropyrimidines was synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H(37)Rv. Two compounds, ethyl 4-[3-(4-fluorophenyl)-1-phenyl- 1H-pyrazo... Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonists [作者：Leslie, CP; Bentley, J; Biagetti, M; Contini, S; Di Fabio, R; Donati, D; Genski, T; Guery, S; Mazzali, A; Merlo, G; Pizzi, DA; Sacco, F; Seri, C; Tessari, M; Zonzini, L; Caberlotto, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6103-6107 , 文章类型： Article，,卷期：2010年20-20] A novel series of trans-8-aminomethyl-1-oxa-3-azaspiro[4.5] decan-2-one derivatives was identified with potent NPY Y5 antagonist activity. Optimization of the original lead furnished compounds 23p and 23u, which combine ... 4-Methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors [作者：Liu, KKC; Bagrodia, S; Bailey, S; Cheng, HM; Chen, H; Gao, L; Greasley, S; Hoffman, JE; Hu, QY; Johnson, TO; Knighton, D; Liu, ZY; Marx, MA; Nambu, MD; Ninkovic, S; Pascual, B; Rafidi, K; Rodgers, CML; Smith, GL; Sun, SX; Wang, HT; Yang, AL; Yuan, J; Zou, AH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6096-6099 , 文章类型： Article，,卷期：2010年20-20] Pteridinones were designed based on a non-selective kinase template. Because of the uniqueness of the PI3K and mTOR binding pockets, a methyl group was introduced to C-4 position of the peteridinone core to give compound... Thienopyrimidines as beta 3-adrenoceptor agonists: Hit-to-lead optimization [作者：Tasler, S; Baumgartner, R; Ammendola, A; Schachtner, J; Wieber, T; Blisse, M; Rath, S; Zaja, M; Klahn, P; Quotschalla, U; Ney, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6108-6115 , 文章类型： Article，,卷期：2010年20-20] Resulting from a vHTS based on a pharmacophore alignment on known beta 3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human beta 3-AR agonist, yie... Bottromycin derivatives: Efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities [作者：Kobayashi, Y; Ichioka, M; Hirose, T; Nagai, K; Matsumoto, A; Matsui, H; Hanaki, H; Masuma, R; Takahashi, Y; Omura, S; Sunazuka, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6116-6120 , 文章类型： Article，,卷期：2010年20-20] Novel bottromycin derivatives were synthesized from bottromycin A(2) via a hydrazide derivative as a common intermediate. Seventeen derivatives were subjected to in vitro evaluation against drug-resistant gram-positive b... Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor [作者：Conejo-Garcia, A; McDonough, MA; Loenarz, C; McNeill, LA; Hewitson, KS; Ge, W; Lienard, BM; Schofield, CJ; Clifton, IJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6125-6128 , 文章类型： Article，,卷期：2010年20-20] Aromatic analogues of the 2-oxoglutarate co-substrate of the hypoxia-inducible factor hydroxylases are shown to bind at the active site iron: Pyridine-2,4-dicarboxylate binds as anticipated with a single molecule chelati... Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors [作者：Chen, CH; Lee, O; Yao, CN; Chuang, MY; Chang, YL; Chang, MH; Wen, YF; Yang, WH; Ko, CH; Chou, NT; Lin, MW; Lai, CP; Sun, CY; Wang, LM; Chen, YC; Hseu, TH; Chang, CN; Hsu, HC; Lin, HC; Chang, YL; Shih, YC; Chou, SH; Hsu, YL; Tseng, HW; Liu, CP; Tu, CM; Hu, TL; Tsai, YJ; Chen, TS; Lin, CL; Chiou, SJ; Liu, CC; Hwang, CS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6129-6132 , 文章类型： Article，,卷期：2010年20-20] A series of azulene-based derivatives were synthesized as potent inhibitors for receptor tyrosine kinases such as FMS-like tyrosine kinase 3 (FLT-3). Systematic side chain modification of prototype 1a was carried out thr... Alteration of cross-linking selectivity with the 2 '-OMe analogue of 2-amino-6-vinylpurine and evaluation of antisense effects [作者：Imoto, S; Hori, T; Hagihara, S; Taniguchi, Y; Sasaki, S; Nagatsugi, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6121-6124 , 文章类型： Article，,卷期：2010年20-20] We previously reported that oligodeoxynucleotides containing 2-amino-6-vinylpurine (2-AVP: 1) exhibit efficient selective cross-linking to cytosine. In this study, the 2'-OMe nucleoside analogue (2) of 2-AVP was designed...