- Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors
[作者：Koryakova, AG; Ivanenkov, YA; Ryzhova, EA; Bulanova, EA; Karapetian, RN; Mikitas, OV; Katrukha, EA; Kazey, VI; Okun, I; Kravchenko, DV; Lavrovsky, YV; Korzinov, OM; Ivachtchenko, AV,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3661-3666 , 文章类型： Article，,卷期：2008年18-12]
- Synthesis, biological evaluation, and SAR dependencies for a series of novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin1-yl)propyl]-1,2,4-oxadiazole-5-carboxamide inhibitors of GSK-3 beta kinase are describe...
- Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor
[作者：Kumar, V; Guo, D; Marella, M; Cassel, JA; DeHaven, RN; Daubert, JD; Mansson, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3667-3671 , 文章类型： Article，,卷期：2008年18-12]
- A series of 2-substituted sulfamoyl arylacetamides of general structure 2 were prepared as potent kappa opioid receptor agonists and the affinities of these compounds for opioid and chimeric receptors were compared with ...
- Carbonic anhydrase inhibitors: Design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes
[作者：Cecchi, A; Ciani, L; Winum, JY; Montero, JL; Scozzafava, A; Ristori, S; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3475-3480 , 文章类型： Article，,卷期：2008年18-12]
- A series of spin-labeled sulfonamides incorporating TEMPO moieties were synthesized by a procedure involving the formation of a thiourea functionality between the benzenesulfonamide and free radical fragment of the molec...
- 1-[4-(2-aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: A novel series of highly potent revertants of P-glycoprotein associated multidrug resistance
[作者：Das, U; Molnar, J; Barath, Z; Bata, Z; Dimmock, JR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3484-3487 , 文章类型： Article，,卷期：2008年18-12]
- The 1-[4-(2-aminoethoxy) phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines 5-8 are a novel cluster of highly potent P-glycoprotein dependent multidrug resistance (MDR) revertants. Using a concentration of 4 mu g/mL,...
- Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases
[作者：Xu, GZ; Searle, LL; Hughes, TV; Beck, AK; Connolly, PJ; Abad, MC; Neeper, MP; Struble, GT; Springer, BA; Emanuel, SL; Gruninger, RH; Pandey, N; Adams, M; Moreno-Mazza, S; Fuentes-Pesquera, AR; Middleton, SA; Greenberger, LM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3495-3499 , 文章类型： Article，,卷期：2008年18-12]
- We herein disclose a novel series of 4-aminopyrimidine-5-carbaldehyde oximes that are potent and selective inhibitors of both EGFR and ErbB-2 tyrosine kinases, with IC50 values in the nanomolar range. Structure-activity ...
- Development of potent and selective small-molecule human Urotensin-II antagonists
[作者：McAtee, JJ; Dodson, JW; Dowdell, SE; Girard, GR; Goodman, KB; Hilfiker, MA; Sehon, CA; Sha, DY; Wang, GZ; Wang, N; Viet, AQ; Zhang, DH; Aiyar, NV; Behm, DJ; Carballo, LH; Evans, CA; Fries, HE; Nagilla, R; Roethke, TJ; Xu, XP; Yuan, CCK; Douglas, SA; Neeb, MJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3500-3503 , 文章类型： Article，,卷期：2008年18-12]
- This work describes the development of potent and selective human Urotensin-II receptor antagonists starting from lead compound 1, (3,4-dichlorophenyl) methyl{2-oxo-2-[3-phenyl-2-(1-pyrrolidinylmethyl)1-piperidinyl]ethyl...
- 5-substituted isophthalamides as insulin receptor sensitizers
[作者：Robinson, L; Bajjalieh, S; Cairns, N; Lum, RT; Macsata, RW; Manchem, VP; Park, SJ; Rao, S; Schow, SR; Shi, S; Spevak, WR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3492-3494 , 文章类型： Article，,卷期：2008年18-12]
- A novel series of 5-substituted isophthalamides and their structure-activity relationship as insulin receptor sensitizers is discussed. (C) 2008 Elsevier Ltd. All rights reserved.
- Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines
[作者：Roach, SL; Higuchi, RI; Adams, ME; Liu, Y; Karanewsky, DS; Marschke, KB; Mais, DE; Miner, JN; Zhi, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3504-3508 , 文章类型： Article，,卷期：2008年18-12]
- A series of nonsteroidal glucocorticoid receptor (GR) ligands based on a 6-indole-1,2,3,4-tetrahydroquinoline scaffold are reported. Structure-activity relationship (SAR) of the pendent indole group identified compound 2...
- Discovery of benzamide tetrahydro-4H-carbazol-4-ones as novel small molecule inhibitors of Hsp90
[作者：Barta, TE; Veal, JM; Rice, JW; Partridge, JM; Fadden, RP; Ma, W; Jenks, M; Geng, LF; Hanson, GJ; Huang, KH; Barabasz, AF; Foley, BE; Otto, J; Hall, SE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3517-3521 , 文章类型： Article，,卷期：2008年18-12]
- Hsp90 maintains the conformational stability of multiple proteins implicated in oncogenesis and has emerged as a target for chemotherapy. We report here the discovery of a novel small molecule scaffold that inhibits Hsp9...
- The effect of different electrostatic potentials on docking accuracy: A case study using DOCK5.4
[作者：Tsai, KC; Wang, SH; Hsiao, NW; Li, M; Wang, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3509-3512 , 文章类型： Article，,卷期：2008年18-12]
- As a commonly used structure-based approach for virtual screening, molecular design and lead optimization, molecular docking can search the preferred orientation and conformation of a ligand for its optimal binding to a ...
- Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)
[作者：Sun, DQ; Wang, ZL; Di, YM; Jaen, JC; Labelle, M; Ma, J; Miao, SC; Sudom, A; Tang, L; Tomooka, CS; Tu, H; Ursu, S; Walker, N; Yan, XL; Ye, QP; Powers, JP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3513-3516 , 文章类型： Article，,卷期：2008年18-12]
- High-throughput screening of a small-molecule compound library resulted in the identification of a series of arylsulfonylpiperazines that are potent and selective inhibitors of human 11 beta-Hydroxysteroid Dehydrogenase ...
- Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G(0)/G(1) phase and thioredoxin-1 nuclear translocation
[作者：Fortin, JS; Cote, MF; Lacroix, J; Patenaude, A; Petitclerc, E; C-Gaudreault, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3526-3531 , 文章类型： Article，,卷期：2008年18-12]
- 1-(2-Chloroethyl)-3-(4-cyclohexylphenyl) urea (cHCEU) has been shown to abrogate the presence of thioredoxin-1 into the nucleus through its selective covalent alkylation. In the present letter we have evaluated the struc...
- Synthesis of BC-ring model of globostellatic acid X methyl ester, an anti-angiogenic substance from marine sponge
[作者：Kotoku, N; Tamada, N; Hayashi, A; Kobayashi, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3532-3535 , 文章类型： Article，,卷期：2008年18-12]
- Concise synthesis of BC-ring model compounds of 13E, 17E-globostellatic acid X methyl ester, an anti-angiogenic triterpene derivative from Indonesian marine sponge, was achieved through ynolate olefination and allylic ox...
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