- New triazole derivatives as antifungal agents: Synthesis via click reaction, in vitro evaluation and molecular docking studies
[作者：Zou, Y; Zhao, QJ; Liao, J; Hu, HG; Yu, SC; Chai, XY; Xu, MJ; Wu, QY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2959-2962 , 文章类型： Article，,卷期：2012年22-8]
- A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (5a-5y) which are analogues of fluconazole, have been designed and synthesized via Cu(I)-catalyzed azide-alkyne cycloaddition on the ...
- From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151
[作者：Mirguet, O; Lamotte, Y; Donche, F; Toum, J; Gellibert, F; Bouillot, A; Gosmini, R; Nguyen, VL; Delannee, D; Seal, J; Blandel, F; Boullay, AB; Boursier, E; Martin, S; Brusq, JM; Krysa, G; Riou, A; Tellier, R; Costaz, A; Huet, P; Dudit, Y; Trottet, L; Kirilovsky, J; Nicodeme, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2963-2967 , 文章类型： Article，,卷期：2012年22-8]
- The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatic cell line...
- Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)
[作者：Seal, J; Lamotte, Y; Donche, F; Bouillot, A; Mirguet, O; Gellibert, F; Nicodeme, E; Krysa, G; Kirilovsky, J; Beinke, S; McCleary, S; Rioja, I; Bamborough, P; Chung, CW; Gordon, L; Lewis, T; Walker, AL; Cutler, L; Lugo, D; Wilson, DM; Witherington, J; Lee, K; Prinjha, RK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2968-2972 , 文章类型： Article，,卷期：2012年22-8]
- A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bi...
- Unambiguous structure of atractyloside and carboxyatractyloside
[作者：Sanchez, JF; Kauffmann, B; Grelard, A; Sanchez, C; Trezeguet, V; Huc, I; Lauquin, GJM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2973-2975 , 文章类型： Article，,卷期：2012年22-8]
- Atractyloside (ATR) was characterized in 1868 and until now structural studies on diterpenic moiety had been done through the characterization of ATR derivatives; while the glycosidic moiety seemed to be a beta-D-glucopy...
- Isoflavones inhibit the clonogenicity of human colon cancer cells
[作者：Hyun, J; Shin, SY; So, KM; Lee, YH; Lim, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2664-2669 , 文章类型： Article，,卷期：2012年22-8]
- Isoflavones are a class of polyphenols that contain various substituents such as hydroxy, methoxy, and glycosyl groups. Methoxy groups are known to increase cell permeability and stability, but small structural changes c...
- Design and synthesis of potent, isoxazole-containing renin inhibitors
[作者：Fournier, PA; Arbour, M; Cauchon, E; Chen, A; Chefson, A; Ducharme, Y; Falgueyret, JP; Gagne, S; Grimm, E; Han, YX; Houle, R; Lacombe, P; Levesque, JF; MacDonald, D; Mackay, B; McKay, D; Percival, MD; Ramtohul, Y; St-Jacques, R; Toulmond, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2670-2674 , 文章类型： Article，,卷期：2012年22-8]
- The design and optimization of a novel isoxazole S-1 linker for renin inhibitor is described herein. This effort culminated in the identification of compound 18, an orally bioavailable, sub-nanomolar renin inhibitor even...
- Synthesis and evaluation of substituted dibenzo[c,e]azepine-5-ones as P-glycoprotein-mediated multidrug resistance reversal agents
[作者：Tang, XB; Gu, XK; Ren, ZG; Ma, YF; Lai, YS; Peng, H; Peng, SX; Zhang, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2675-2680 , 文章类型： Article，,卷期：2012年22-8]
- A series of substituted dibenzo[c,e]azepine-5-ones (7a-h) were synthesized and evaluated as P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) reversal agents. The most potent compound 7h could significantly and s...
- Double-stranded oligonucleotides containing 5-aminomethyl-2 '-deoxyuridine form thermostable anti-parallel triplexes with single-stranded DNA or RNA
[作者：Shibata, A; Ueno, Y; Iwata, M; Wakita, H; Matsuda, A; Kitade, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2681-2683 , 文章类型： Article，,卷期：2012年22-8]
- This Letter describes the synthesis and properties of double-stranded antisense oligonucleotides connected with a pentaerythritol linker. We found that double-stranded antisense oligonucleotides with aminomethyl residues...
- Lanthanide(III) complexes of pyridine-tetraacetic acid-glycoconjugates: Synthesis and luminescence studies of mono and divalent derivatives
[作者：Gouin, SG; Roger, M; Leygue, N; Deniaud, D; Julienne, K; Benoist, E; Picard, C; Kovensky, J; Galaup, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2684-2688 , 文章类型： Article，,卷期：2012年22-8]
- A potent lanthanide chelate, fulfilling the requirements for the development of MRI contrast agents or luminescent probes, was armed with alkyne groups. We then implemented a click methodology to graft the bifunctional l...
- Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies
[作者：Watanabe, Y; Kitazawa, S; Fujii, H; Nemoto, T; Hirayama, S; Nagase, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2689-2692 , 文章类型： Article，,卷期：2012年22-8]
- A novel opioid ligand possessing a stable and cyclic imine 16 and its derivatives with an azabicyclo[2.2.2]octane skeleton were synthesized. The imine 16 showed higher affinity for the mu receptor than compound 21 with a...
- Phosphonium lipocations as antiparasitic agents
[作者：Long, TE; Lu, X; Galizzi, M; Docampo, R; Gut, J; Rosenthal, PJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2976-2979 , 文章类型： Article，,卷期：2012年22-8]
- Phosphonium lipocations were synthesized and evaluated for inhibition of the development of Plasmodium falciparum and Trypanosoma cruzi, etiological agents of malaria and Chagas disease, respectively. Optimal phthalimide...
- Copper(I) mediated facile synthesis of potent tubulin polymerization inhibitor, 9-amino-alpha-noscapine from natural alpha-noscapine
[作者：Manchukonda, NK; Sridhar, B; Naik, PK; Joshi, HC; Kantevari, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2983-2987 , 文章类型： Article，,卷期：2012年22-8]
- Facile synthesis of natural alpha-noscapine analogue, 9-amino-alpha-noscapine, a potent inhibitor of tubulin polymerization for cancer therapy, is achieved via copper(I) iodide mediated in situ aromatic azidation and red...
- Structural polymorphism of human telomere G-quadruplex induced by a pyridyl carboxamide molecule
[作者：Xu, L; Xu, ZX; Shang, Y; Feng, S; Zhou, X,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2988-2992 , 文章类型： Article，,卷期：2012年22-8]
- In this work, we described a kinetically slow (hour-scale) but thermodynamically favored G-quadruplex conversion induced by a pyridyl carboxamide molecule. This slow transition was observed through CD spectra and gels, a...
- Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease
[作者：Duan, MS; Kazmierski, W; Crosby, R; Gartland, M; Ji, JJ; Tallant, M; Wang, A; Hamatake, R; Wright, L; Wu, M; Zhang, YK; Ding, CZ; Li, XF; Liu, Y; Zhang, SM; Zhou, Y; Plattner, JJ; Baker, SJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2993-2996 , 文章类型： Article，,卷期：2012年22-8]
- A novel series of P3 oxo-modified macrocyclic hepatitis C virus NS3/4A serine protease inhibitor was designed, synthesized and biologically evaluated. The hydroxy-substituted inhibitor 10 demonstrated high potency in gen...
- Development of clickable active site-directed photoaffinity probes for gamma-secretase
[作者：Crump, CJ; Ende, CWA; Ballard, TE; Pozdnyakov, N; Pettersson, M; Chau, DM; Bales, KR; Li, YM; Johnson, DS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2997-3000 , 文章类型： Article，,卷期：2012年22-8]
- We have developed clickable active site-directed photoaffinity probes for gamma-secretase which incorporate a photoreactive benzophenone group and an alkyne handle for subsequent click chemistry mediated conjugation with...
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