- Hirtellanines A and B, a pair of isomeric isoflavonoid derivatives from Campylotropis hirtella and their immunosuppressive activities
[作者:Shou, QY; Tan, Q; Shen, ZW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3389-3391 , 文章类型: Article,,卷期:2009年19-13]
- A pair of isomeric isoflavonoid derivatives, Hirtellanines A (1) and B (2), has been isolated from the roots of Campylotropis hirtella (Franch.) Schindl. and their structures were elucidated on the basis of spectroscopic...
- Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors
[作者:Shen, HC; Ding, FX; Wang, SY; Xu, SY; Chen, HS; Tong, X; Tong, V; Mitra, K; Kumar, S; Zhang, XP; Chen, YL; Zhou, GC; Pai, LY; Alonso-Galicia, M; Chen, XL; Zhang, B; Tata, JR; Berger, JP; Colletti, SL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3398-3404 , 文章类型: Article,,卷期:2009年19-13]
- Spirocyclic secondary amine-derived trisubstituted ureas were identified as highly potent, bioavailable and selective soluble epoxide hydrolase (sEH) inhibitors. Despite good oral exposure and excellent ex vivo target en...
- Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors
[作者:Lahue, BR; Ma, Y; Shipps, GW; Seghezzi, W; Herbst, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3405-3409 , 文章类型: Article,,卷期:2009年19-13]
- Substituted benzimidazoles were pro. led as inhibitors of kinesin spindle protein (KSP), an increasingly important target for the development of anticancer drugs. This series demonstrated the monoastral phenotypic respon...
- Carrier PNA for shRNA delivery into cells
[作者:Kitamatsu, M; Kubo, T; Matsuzaki, R; Endoh, T; Ohtsuki, T; Sisido, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3410-3413 , 文章类型: Article,,卷期:2009年19-13]
- A peptide nucleic acid (PNA)-cell-penetrating peptide (CPP) conjugate (carrier PNA) was used as 'bridgebuilder' to connect a CPP with an shRNA. The carrier PNA successfully formed a hybrid with an shRNA bearing complemen...
- Synthesis and evaluation of 9-O-substituted berberine derivatives containing aza-aromatic terminal group as highly selective telomeric G-quadruplex stabilizing ligands
[作者:Ma, Y; Ou, TM; Tan, JH; Hou, JQ; Huang, SL; Gu, LQ; Huang, ZS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3414-3417 , 文章类型: Article,,卷期:2009年19-13]
- A series of new 9-O-substituted berberine derivatives (4a-j) as telomeric quadruplex ligands was synthesized and evaluated. The results from biophysical and biochemical assay indicated that introducing of positive charge...
- Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists
[作者:Cherney, RJ; Mo, RW; Meyer, DT; Voss, ME; Lo, YC; Yang, GJ; Miller, PB; Scherle, PA; Tebben, AJ; Carter, PH; Decicco, CP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3418-3422 , 文章类型: Article,,卷期:2009年19-13]
- Potent sulfone-containing di- and trisubstituted cyclohexanes were synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the trisubstituted derivative 54, which exhibited excellent binding ...
- Synthesis and biological evaluation of platinum-acridine hybrid agents modified with bipyridine non-leaving groups
[作者:Kheradi, AR; Saluta, G; Kucera, GL; Day, CS; Bierbach, U,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3423-3425 , 文章类型: Article,,卷期:2009年19-13]
- The use of 2,2'-bipyridines (4,4'-R-2-2,2'-bpy; R = H, Me, OMe, CF3) as non-leaving groups (L-L) in platinum-acridinylthiourea conjugates, [PtCl(L-L)(ACRAMTU)](NO3)(2), has been investigated. All bpy-substituted complexe...
- Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics
[作者:Taka, N; Matsuoka, H; Sato, T; Yoshino, H; Imaoka, I; Sato, H; Kotake, K; Kumagai, Y; Kamei, K; Ozaki, KI; Higashida, A; Kuroki, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3426-3429 , 文章类型: Article,,卷期:2009年19-13]
- We successfully discovered peptidomimetic motilin antagonists (17c and 17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (2). Furthermore, with oral administration and based on motil...
- Carbonic anhydrase activators. Activation of the membrane-associated isoform XV with amino acids and amines
[作者:Innocenti, A; Hilvo, M; Parkkila, S; Scozzafava, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3430-3433 , 文章类型: Article,,卷期:2009年19-13]
- An activation study of the membrane-associated carbonic anhydrase (CA, EC 4.2.1.1) isoform XV with a series of natural and non-natural amino acids and aromatic/heterocyclic amines is reported. Murine CA XV was strongly a...
- 2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers
[作者:El Bakali, J; Klupsch, F; Guedin, A; Brassart, B; Fontaine, G; Farce, A; Roussel, P; Houssin, R; Bernier, JL; Chavatte, P; Mergny, JL; Riou, JF; Henichart, JP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3434-3438 , 文章类型: Article,,卷期:2009年19-13]
- design and synthesis of 2,6-diphenylthiazolo[3,2-b][1,2,4] triazoles characterized by a large aromatic building block bearing cationic side chains are reported. These molecules are evaluated as telomeric G-quadruplex sta...
- Fast and easy access to efficient bifunctional chelators for MRI applications
[作者:Gugliotta, G; Botta, M; Giovenzana, GB; Tei, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3442-3444 , 文章类型: Article,,卷期:2009年19-13]
- Novel bifunctional agents based on the AAZTA (6-amino-6-methylperhydro-1,4-diazepinetetraacetic acid) structure with hydroxyl, carboxyl and chloro functional groups were prepared. The Gd-III complexes show optimal magnet...
- Synthesis and activity of quinolinylmethyl P1 ' alpha-sulfone piperidine hydroxamate inhibitors of TACE
[作者:Zhang, CC; Lovering, F; Behnke, M; Zask, A; Sandanayaka, V; Sun, LH; Zhu, Y; Xu, WX; Zhang, YH; Levin, JI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3445-3448 , 文章类型: Article,,卷期:2009年19-13]
- A series of alpha-sulfone piperidine hydroxamate TACE inhibitors 11a-n bearing a quinolinyl methyl P1' group was prepared, and their activity was compared to analogous alpha- and beta-sulfone piperidine hydroxamates with...
- Bis-neonicotinoid insecticides: Observed and predicted binding interactions with the nicotinic receptor
[作者:Ohno, I; Tomizawaa, M; Durkin, KA; Casida, JE; Kagabu, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3449-3452 , 文章类型: Article,,卷期:2009年19-13]
- The bis-pharmacophore approach applied to neonicotinoid insecticides reveals high binding affinity for heptamethylene bis-N-3,N-3'-imidacloprid fitting a nicotinic acetylcholine receptor model wherein the chloropyridine ...
- Discovery of novel phosphonate derivatives as hepatitis C virus NS3 protease inhibitors
[作者:Sheng, XC; Pyun, HJ; Chaudhary, K; Wang, JY; Doerffler, E; Fleury, M; McMurtrie, D; Chen, XW; Delaney, WE; Kim, CU,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3453-3457 , 文章类型: Article,,卷期:2009年19-13]
- A novel class of phosphonate derivatives was designed to mimic the interaction of product-like carboxylate based inhibitors of HCV NS3 protease. A phosphonic acid (compound 2) was demonstrated to be a potent HCV NS3 prot...
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