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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38条记录   Delivering a hydrophobic anticancer drug for photodynamic therapy by amorphous formulation [作者：Zhou, L; Wang, W; Feng, YY; Wei, SH; Zhou, JH; Yu, BY; Shen, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6172-6174 , 文章类型： Article，,卷期：2010年20-21] An amorphous formulation of hypocrellin A for photodynamic therapy is reported which can provide stable aqueous dispersion of such hydrophobic photosensitizers. In vitro studies have demonstrated the active uptake of amo... Design, synthesis, and biological evaluation of 4-(5-nitrofuran-2-yl) prop-2-en-1-one derivatives as potent antitubercular agents [作者：Tawari, NR; Bairwa, R; Ray, MK; Rajan, MGR; Degani, MS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6175-6178 , 文章类型： Article，,卷期：2010年20-21] Based on stereoelectronic feature analysis using density functional theory (DFT) at B3LYP/3-21*G level, a series of 4-(5-nitrofuran-2-yl)prop-2-en-1-one derivatives with low LUMO energies (<-0.10 eV); concentrated over t... Bombesin derivative radiolabeled with technetium-99m as agent for tumor identification [作者：de Barros, ALB; Mota, LD; Ferreira, CD; de Oliveira, MC; de Goes, AM; Cardoso, VN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6182-6184 , 文章类型： Article，,卷期：2010年20-21] A bombesin derivative was successfully radiolabeled in high labeling yield. Biodistribution studies and scintigraphic images in Ehrlich tumor-bearing mice were performed. This compound showed high accumulation in tumor t... Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities [作者：Zhan, ZJ; Yu, Q; Wang, ZL; Shan, WG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6185-6187 , 文章类型： Article，,卷期：2010年20-21] Through bioassay-guided fractionation and chromatography technique, eight indole alkaloids were furnished from the stems of Ervatamia hainanensis. All isolates were evaluated for acetylcholinesterase (AChE) inhibition ac... Inhibitory activity of four demethoxy fluorinated anthracycline analogs against five human-tumor cell lines [作者：Horton, D; Khare, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6179-6181 , 文章类型： Article，,卷期：2010年20-21] Four anthracycline analogs synthesized in our laboratory were evaluated in comparison with adriamycin (doxorubicin) for their growth-inhibitory effect against five human-tumor cell lines, including lung carcinoma, colon ... Efficient synthesis and biological evaluation of some 2,4-diamino-furo[2,3-d]pyrimidine derivatives [作者：Hu, YG; Wang, Y; Du, SM; Chen, XB; Ding, MW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6188-6190 , 文章类型： Article，,卷期：2010年20-21] The carbodiimides 2, obtained from aza-Wittig reactions of iminophosphorane 1 with aromatic isocyanates, reacted with ammonia to give ethyl 3,4-dihydro-6-methyl-4-oxo-2-arylamino-furo[2,3-d]pyrimidine-5-carboxylate 3. Fu... Synthesis and biological evaluation of indolyl glyoxylamides as a new class of antileishmanial agents [作者：Chauhan, SS; Gupta, L; Mittal, M; Vishwakarma, P; Gupta, S; Chauhan, PMS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6191-6194 , 文章类型： Article，,卷期：2010年20-21] A series of indolylglyoxylamide derivatives have been synthesized and evaluated in vitro against amastigote form of Leishmania donovani. Compound 8c has been identified as the most active analog of the series with IC50 v... Discovery of the inhibitors of tumor necrosis factor alpha with structure-based virtual screening [作者：Choi, H; Lee, Y; Park, H; Oh, DS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6195-6198 , 文章类型： Article，,卷期：2010年20-21] Tumor necrosis factor alpha (TNF-alpha) has been considered as one of the attractive drug targets for allergic diseases including asthma. We have been able to identify five novel TNF-alpha inhibitors with a drug-design p... Design, synthesis and activity of benzothiazole-based inhibitors of NO production in LPS-activated macrophages [作者：Jin, GH; Li, H; An, S; Ryu, JH; Jeon, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6199-6202 , 文章类型： Article，,卷期：2010年20-21] Series of benzothiazoles were synthesized and evaluated their inhibitory activities for NO production in lipopolysaccharide-activated macrophages. The most potent compound was the indole-containing benzothiazole 3c with ... Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors [作者：Xu, WJ; Chen, G; Zhu, WL; Zuo, ZL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6203-6207 , 文章类型： Article，,卷期：2010年20-21] A similarity search on the structural analogs of an inhibitor of BACE-1 with IC50 2.8 mu M, which contained a P1 benzothiazole group together with a triazine ring linked by a secondary amine group, was described in this ... Paraoxon, 4-nitrophenyl phosphate and acetate are substrates of alpha- but not of beta-, gamma- and zeta-carbonic anhydrases [作者：Innocenti, A; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6208-6212 , 文章类型： Article，,卷期：2010年20-21] Carbonic anhydrases (CAs, EC 4.2.1.1) belonging to alpha-, beta-, gamma- and zeta-classes and from various organisms, ranging from the bacteria, archaea to eukarya domains, were investigated for their esterase/phosphatas... New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold [作者：Maingot, L; Leroux, F; Landry, V; Dumont, J; Nagase, H; Villoutreix, B; Sperandio, O; Deprez-Poulain, R; Deprez, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6213-6216 , 文章类型： Article，,卷期：2010年20-21] In this Letter we describe the design, synthesis, screening, and optimization of a new family of ADAMTS-5 inhibitors. These inhibitors display an original 1,2,4-triazole-3-thiol scaffold as a putative zinc binding-group.... Synthesis and biological evaluation of novel triptolide analogues for anticancer activity [作者：Zhou, B; Miao, ZH; Deng, G; Ding, JA; Yang, YX; Feng, HJ; Li, YC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6217-6221 , 文章类型： Article，,卷期：2010年20-21] Three types of novel triptolide analogues with 9,11-olefin (3-5), five-membered unsaturated lactam ring (6-7) or A/B cis ring junction (8-14) were synthesized. Although with 9,11-olefin instead of 9,11-beta-epoxide, comp... 'Click' assembly of selective inhibitors for MAO-A [作者：Jia, Z; Zhu, Q,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6222-6225 , 文章类型： Article，,卷期：2010年20-21] In this Letter, an efficient strategy for the fast construction of 108 compounds library was developed using click chemistry. The fingerprint of inhibitory activity toward MAO-A/B against this library was obtained, and f... Indole- and benzothiophene-based histamine H-3 antagonists [作者：Santillan, A; McClure, KJ; Allison, BD; Lord, B; Boggs, JD; Morton, KL; Everson, AM; Nepomuceno, D; Letavic, MA; Lee-Dutra, A; Lovenberg, TW; Carruthers, NI; Grice, CA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6226-6230 , 文章类型： Article，,卷期：2010年20-21] Previous research on histamine H-3 antagonists has led to the development of a pharmacophore model consisting of a central phenyl core flanked by two alkylamine groups. Recent investigation of the replacement of the cent... Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: Improving selectivity over hERG [作者：Rankovic, Z; Cai, J; Kerr, J; Fradera, X; Robinson, J; Mistry, A; Finlay, W; McGarry, G; Andrews, F; Caulfield, W; Cumming, I; Dempster, M; Waller, J; Arbuckle, W; Anderson, M; Martin, I; Mitchell, A; Long, C; Baugh, M; Westwood, P; Kinghorn, E; Jones, P; Uitdehaag, JCM; van Zeeland, M; Potin, D; Saniere, L; Fouquet, A; Chevallier, F; Deronzier, H; Dorleans, C; Nicolai, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6237-6241 , 文章类型： Article，,卷期：2010年20-21] Several structure-guided optimisation strategies were explored in order to improve the hERG selectivity profile of cathepsin K inhibitor 1, whilst maintaining its otherwise excellent in vitro and in vivo profile. Ultimat...