- Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders
[作者:Morley, A; Tomkinson, N; Cook, A; MacDonald, C; Weaver, R; King, S; Jenkinson, L; Unitt, J; McCrae, C; Phillips, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6031-6035 , 文章类型: Article,,卷期:2011年21-20]
- To try and generate broad spectrum human rhinovirus VP1 inhibitors with more attractive physicochemical, DMPK and safety profiles, we explored the current SAR of known VP1 compounds. This lead to the identification of sp...
- Relationship between the structures of flavonoids and their NF-kappa B-dependent transcriptional activities
[作者:Shin, SY; Woo, Y; Hyun, J; Yong, Y; Koh, D; Lee, YH; Lim, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6036-6041 , 文章类型: Article,,卷期:2011年21-20]
- It has been previously shown that some flavonoids inhibit NF-kappa B; however, the structure-activity relationships between chalcone, flavanone, flavone, and isoflavone derivatives and their TNF alpha induced NF-kappa B ...
- Design, synthesis and SAR of indazole and benzoisoxazole containing 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
[作者:Zhang, XQ; Hufnagel, H; Hou, CF; Opas, E; McKenney, S; Crysler, C; O'Neill, J; Johnson, D; Sui, ZH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6042-6048 , 文章类型: Article,,卷期:2011年21-20]
- A novel series of 4-azetidinyl-1-aryl-cyclohexanes containing indazole or benzoisoxazole moiety have been identified as potent CCR2 antagonists with high selectivity versus hERG. (C) 2011 Elsevier Ltd. All rights reserve...
- Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors
[作者:Jin, CH; Krishnaiah, M; Sreenu, D; Subrahmanyam, VB; Rao, KS; Mohan, AVN; Park, CY; Son, JY; Sheen, YY; Kim, DK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6049-6053 , 文章类型: Article,,卷期:2011年21-20]
- A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles 14a-ae, 16a, 16b, and 21a-c has been prepared and evaluated for their ALK5 inhibitory activity in an enzyme assay and in ...
- A compound isolated from Schisandra chinensis induces apoptosis
[作者:Hwang, D; Shin, SY; Lee, Y; Hyun, J; Yong, Y; Park, JC; Lee, YH; Lim, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6054-6057 , 文章类型: Article,,卷期:2011年21-20]
- Schizandra chinensis has been known to have five predominant tastes: salty, sweet, sour, astringent, and bitter. It has also been shown to have various effects on the cardiovascular system, gastrointestinal system, anti-...
- Synthesis of glycoconjugate carbonic anhydrase inhibitors by ruthenium-catalysed azide-alkyne 1,3-dipolar cycloaddition
[作者:Salmon, AJ; Williams, ML; Maresca, A; Supuran, CT; Poulsen, SA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6058-6061 , 文章类型: Article,,卷期:2011年21-20]
- Carbonic anhydrase IX (CA IX) is a recently validated target for the development of new cancer therapies. In this Letter we describe the synthesis and CA inhibition of a novel series of carbohydrate-based 1, 5-disubstitu...
- Synthesis and biological activity of desmethoxy analogues of coruscanone A
[作者:Tichotova, L; Matousova, E; Spulak, M; Kunes, J; Votruba, I; Buchta, V; Pour, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6062-6066 , 文章类型: Article,,卷期:2011年21-20]
- A series of simple desmethoxy analogues of coruscanone A was prepared via a novel version of Ti(iPrO)(4)-mediated Knoevenagel condensation of cyclopentenedione with substituted benzaldehydes and cinnamic aldehydes, and t...
- Localization of GroEL determined by in vivo incorporation of a fluorescent amino acid
[作者:Charbon, G; Wang, JY; Brustad, E; Schultz, PG; Horwich, AL; Jacobs-Wagner, C; Chapman, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6067-6070 , 文章类型: Article,,卷期:2011年21-20]
- The molecular chaperone GroEL is required for bacterial growth under all conditions, mediating folding assistance, via its central cavity, to a diverse set of cytosolic proteins; yet the subcellular localization of GroEL...
- Efficient synthesis of apricoxib, CS-706, a selective cyclooxygenase-2 inhibitor, and evaluation of inhibition of prostaglandin E2 production in inflammatory breast cancer cells
[作者:Mandal, PK; Freiter, EM; Bagsby, AL; Robertson, FM; McMurray, JS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6071-6073 , 文章类型: Article,,卷期:2011年21-20]
- An efficient synthesis of apricoxib (CS-706), a selective cyclooxygenase inhibitor, was developed using copper catalyzed homoallylic ketone formation from methyl 4-ethoxybenzoate followed by ozonolysis to an aldehyde, an...
- Isomeric acetoxy analogs of celecoxib and their evaluation as cyclooxygenase inhibitors
[作者:Rahim, MA; Rao, PNP; Bhardwaj, A; Kaur, J; Huang, ZJ; Knaus, EE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6074-6080 , 文章类型: Article,,卷期:2011年21-20]
- A group of celecoxib analogs having a SO(2)NH(2) (9a-f), or SO(2)Me (12a-f), COX-2 pharmacophore at the para-position of the N-1 phenyl ring in conjunction with a C-5 phenyl ring having a variety of substituents (4-, 3-,...
- Cloning and characterization of a type III polyketide synthase from Aspergillus niger
[作者:Li, J; Luo, YZ; Lee, JK; Zhao, HM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6085-6089 , 文章类型: Article,,卷期:2011年21-20]
- Type III polyketide synthases (PKSs) are the condensing enzymes that catalyze the formation of a myriad of aromatic polyketides in plant, bacteria, and fungi. Here we report the cloning and characterization of a putative...
- Development of a potassium ion-selective fluorescent sensor based on 3-styrylated BODIPY
[作者:Hirata, T; Terai, T; Komatsu, T; Hanaoka, K; Nagano, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6090-6093 , 文章类型: Article,,卷期:2011年21-20]
- We have developed a red-emitting fluorescent K(+) probe, B3TAC, which also shows a wavelength shift upon binding to K(+). The probe was synthesized by conjugating a cryptand-based chelator, 2-triazacrypt- and [2,2,3]-1-(...
- Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin
[作者:Jin, YF; Gill, SK; Kirchhoff, PD; Wan, BJ; Franzblau, SG; Garcia, GA; Showalter, HDH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6094-6099 , 文章类型: Article,,卷期:2011年21-20]
- A series of rifamycin S and rifampin analogues incorporating substituted 8-amino, 8-thio, and 1,8-pyrazole substituents has been synthesized. The compounds were made by activation of the C-8 phenol as a sulfonate ester, ...
- Potent inhibition of bacterial neuraminidase activity by pterocarpans isolated from the roots of Lespedeza bicolor
[作者:Woo, HS; Kim, DW; Curtis-Long, MJ; Lee, BW; Lee, JH; Kim, JY; Kang, JE; Park, KH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6100-6103 , 文章类型: Article,,卷期:2011年21-20]
- Bacterial neuraminidase has been highlighted as a key enzyme for pathogenic infection and sepsis. Six pterocarpans displaying significant levels of neuraminidase inhibitory activity were isolated from the root bark of Le...
- Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands
[作者:Demizu, Y; Takahashi, T; Kaneko, F; Sato, Y; Okuda, H; Ochiai, E; Horie, K; Takagi, K; Kakuda, S; Takimoto-Kamimura, M; Kurihara, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6104-6107 , 文章类型: Article,,卷期:2011年21-20]
- We designed and synthesized nonsecosteroidal vitamin D receptor (VDR) ligands that formed H-bonds with six amino acid residues (Tyr143, Ser233, Arg270, Ser274, His301 and His393) of the VDR ligand-binding domain. The lig...
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