- 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...
- 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...
- 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...
- 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...
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