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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106条记录   N-Amino acid linoleoyl conjugates: Anti-inflammatory activities [作者：Burstein, S; McQuain, C; Salmonsen, R; Seicol, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：872-875 , 文章类型： Article，,卷期：2012年22-2] Several N-linked amino acid-linoleic acid conjugates were studied for their potential as anti inflammatory agents. The parent molecule, N-linoleoylglycine was tested in an in vivo model, the mouse peritonitis assay where... Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases [作者：Sabbah, DA; Simms, NA; Brattain, MG; Vennerstrom, JL; Zhong, HZ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：876-880 , 文章类型： Article，,卷期：2012年22-2] The alpha isoform of the phosphatidylinositol-3-kinases (PI3K alpha) is often mutated, amplified and overexpressed in human tumors. In an effort to develop new inhibitors targeting this enzyme, we carried out a pharmacop... Diamidinium and iminium aromatics as new aggregators of the bacterial signaling molecule, c-di-GMP [作者：Kelsey, I; Nakayama, S; Sintim, HO,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：881-885 , 文章类型： Article，,卷期：2012年22-2] C-di-GMP has emerged as an important bacterial signaling molecule that is involved in biofilm formation. Small molecules that can form biologically inactive complexes with c-di-GMP have the potential to be used as anti-b... Structure-activity relationship of naphthaldehydethiosemicarbazones in melanogenesis inhibition [作者：Thanigaimalai, P; Rao, EV; Lee, KC; Sharma, VK; Roh, E; Kim, Y; Jung, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：886-889 , 文章类型： Article，,卷期：2012年22-2] 2-(Naphthalen-1-ylmethylene)hydrazinecarbothioamide (14, IC50 = 1.1 mu M) was discovered as a highly potent inhibitor of melanogenesis. To define the role of hydrogens (at N1 and N3) and sulfur in 14, a series of analogs... Constituents of Dalbergia sissoo Roxb. leaves with osteogenic activity [作者：Dixit, P; Chillara, R; Khedgikar, V; Gautam, J; Kushwaha, P; Kumar, A; Singh, D; Trivedi, R; Maurya, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：890-897 , 文章类型： Article，,卷期：2012年22-2] One new isoflavone glucoside, caviunin 7-O-[beta-D-apiofuranosyl-(1 -> 6)-beta-D-glucopyranoside] (10) and a new itaconic derivative, (E)-4-methoxy-2-(3,4-dihydroxybenzylidene)-4-oxobutanoic acid (15) along with series o... Synthesis and DNA cleavage studies of novel quinoline oxime esters [作者：Bindu, PJ; Mahadevan, KM; Satyanarayan, ND; Naik, TRR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：898-900 , 文章类型： Article，,卷期：2012年22-2] New 2-chloro-3-formyl quinoline oxime esters were synthesized by the reaction of 2-chloro-3-formyl quinoline oximes with various benzoyl chlorides in the presence of triethyl amine and dichloromethane at 0 degrees C. The... Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity [作者：Roughley, SD; Browne, H; Macias, AT; Benwell, K; Brooks, T; D'Alessandro, J; Daniels, Z; Dugdale, S; Francis, G; Gibbons, B; Hart, T; Haymes, T; Kennett, G; Lightowler, S; Matassova, N; Mansell, H; Merrett, A; Misra, A; Padfield, A; Parsons, R; Pratt, R; Robertson, A; Simmonite, H; Tan, K; Walls, SB; Wong, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：901-906 , 文章类型： Article，,卷期：2012年22-2] We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We de... Synthesis and evaluation of tetrahedral intermediate mimic inhibitors of 3-deoxy-D-manno-octulosonate 8-phosphate synthase [作者：Harrison, AN; Reichau, S; Parker, EJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：907-911 , 文章类型： Article，,卷期：2012年22-2] 3-Deoxy-o-manno-octulosonate 8-phosphate (KDO8P) synthase catalyses the first committed step in the biosynthesis of 3-deoxy-D-manno-octulosonate (KDO), an important component of the lipopolysaccharide of Gram-negative ba... Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: An increase in aqueous solubility via the disruption of crystal packing [作者：Wenglowsky, S; Moreno, D; Rudolph, J; Ran, YQ; Ahrendt, KA; Arrigo, A; Colson, B; Gloor, SL; Hastings, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：912-915 , 文章类型： Article，,卷期：2012年22-2] A single crystal was obtained of a lead B-Raf(V600E) inhibitor with low aqueous solubility. The X-ray crystal structure revealed hydrogen-bonded head-to-tail dimers formed by the pyrazolopyridine and sulfonamide groups o... Structures of peptide agonists for human protease activated receptor 2 [作者：Stoermer, MJ; Flanagan, B; Beyer, RL; Madala, PK; Fairlie, DP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：916-919 , 文章类型： Article，,卷期：2012年22-2] Protease activated receptor 2 (PAR2) is an unusual G-protein coupled receptor in being self-activated, after pruning of the N-terminus by serine proteases like tiypsin and tryptase. Short synthetic peptides corresponding... Design, synthesis and cytotoxic activity of novel spin-labeled rotenone derivatives [作者：Liu, YQ; Ohkoshi, E; Li, LH; Yang, L; Lee, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：920-923 , 文章类型： Article，,卷期：2012年22-2] Three series of novel spin-labeled rotenone derivatives were synthesized and evaluated for cytotoxicity against four tumor cell lines, A-549, DU-145, KB and KBvin. All of the derivatives showed promising in vitro cytotox... An alternative synthetic route for an antidiabetic drug, rosiglitazone [作者：Jawale, DV; Pratap, UR; Mane, RA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：924-928 , 文章类型： Article，,卷期：2012年22-2] A convenient and scalable four-step novel route has been developed for the synthesis of rosiglitazone (8), an antidiabetic drug. This multistep route requires 4-fluoro benzaldehyde (4), 2,4-thiazolidinedione (6) and 2-ch... Discovery of a novel chemotype of potent human ENaC blockers using a bioisostere approach. Part 1: Quaternary amines [作者：Hunt, T; Atherton-Watson, HC; Axford, J; Collingwood, SP; Coote, KJ; Cox, B; Czarnecki, S; Danahay, H; Devereux, N; Howsham, C; Hunt, P; Paddock, V; Paisley, D; Young, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：929-932 , 文章类型： Article，,卷期：2012年22-2] We report the identification of a novel series of human epithelial sodium channel (ENaC) blockers that are structurally distinct from the pyrazinoyl guanidine chemotype found in prototypical ENaC blockers such as amilori... Synthesis of substituted benzimidazolyl curcumin mimics and their anticancer activity [作者：Woo, HB; Eom, YW; Park, KS; Ham, J; Ahn, CM; Lee, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：933-936 , 文章类型： Article，,卷期：2012年22-2] A novel curcumin mimic library (14a-14h and 15a-15h) possessing variously substituted benzimidazole groups was synthesized through the aldol reaction of (E)-4-(4-hydroxy-3-methoxyphenyl)but-3-en-2-one (7) or (E)-4-(3-hyd... DNA binding and anticancer activity of naphthalimides with 4-hydroxyl-alkylamine side chains at different lengths [作者：Wang, KR; Wang, YQ; Yan, XH; Chen, H; Ma, G; Zhang, PZ; Li, JM; Li, XL; Zhang, JC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：937-941 , 文章类型： Article，,卷期：2012年22-2] A series of novel naphthalimide derivatives modified with various hydroxyl-alkylamines at 4-position have been synthesized. Their DNA binding properties were investigated by UV-Vis, fluoescence, and circular dichroism (C... Discovery and molecular docking of quinolyl-thienyl chalcones as anti-angiogenic agents targeting VEGFR-2 tyrosine kinase [作者：Rizvi, SUF; Siddiqui, HL; Nisar, M; Khan, N; Khan, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：942-944 , 文章类型： Article，,卷期：2012年22-2] Vascular endothelial growth factor Receptor-2 (VEGFR-2) kinase inhibition is one of the well established strategies to promptly tackle tumor growth by suppression of angiogenesis. In the current study, structure-based vi...