- 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKC theta
[作者：Tumey, LN; Boschelli, DH; Lee, J; Chaudhary, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4420-4423 , 文章类型： Article，,卷期：2008年18-15]
- A series of 2-alkenyl thieno[2,3-b] pyridine inhibitors of PKC theta were synthesized as potential inflammatory modulators. This series led to the discovery of 2-alkenyl amides, which are exceptionally potent and selecti...
- Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers
[作者：Lee, HK; Lee, YS; Roh, EJ; Rhim, H; Lee, JY; Shin, KJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4424-4427 , 文章类型： Article，,卷期：2008年18-15]
- We have synthesized and evaluated alpha,alpha'-disubstituted phenylacetate derivatives that were designed as T-type calcium channel blockers. Among them, compound 10e (IC50 = 8.17 +/- 0.48 nM) showed the most potent T-ty...
- Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity
[作者：Angell, R; Aston, NM; Bamborough, P; Buckton, JB; Cockerill, S; Deboeck, SJ; Edwards, CD; Holmes, DS; Jones, KL; Laine, DI; Patel, S; Smee, PA; Smith, KJ; Somers, DO; Walker, AL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4428-4432 , 文章类型： Article，,卷期：2008年18-15]
- The biphenyl amides (BPAs) are a novel series of p38 alpha MAP kinase inhibitor. The optimisation of the series to give compounds that are potent in an in vivo disease model is discussed. SAR is presented and rationalise...
- Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes
[作者：Angell, RM; Angell, TD; Bamborough, P; Bamford, MJ; Chung, CW; Cockerill, SG; Flack, SS; Jones, KL; Laine, DI; Longstaff, T; Ludbrook, S; Pearson, R; Smith, KJ; Smee, PA; Somers, DO; Walker, AL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4433-4437 , 文章类型： Article，,卷期：2008年18-15]
- The biphenyl amides (BPAs) are a series of p38 alpha MAP kinase inhibitors. Compounds are able to bind to the kinase in either the DFG-in or DFG-out conformation, depending on substituents. X-ray, binding, kinetic and ce...
- Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors (vol 18, pg 3236, 2008)
[作者：Cumming, JN; Le, TX; Babu, S; Carroll, C; Chen, X; Favreau, L; Gaspari, P; Guo, T; Hobbs, DW; Huang, Y; Iserloh, U; Kennedy, ME; Kuvelkar, R; Li, G; Lowrie, J; McHugh, NA; Ozgur, L; Pan, J; Parker, EM; Saionz, K; Stamford, AW; Strickland, C; Tadesse, D; Voigt, J; Wanga, L; Wu, Y; Zhang, L; Zhang, Q,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4447-4447 , 文章类型： Correction，,卷期：2008年18-15]
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- Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1)
[作者：Purandare, AV; Chen, Z; Huynh, T; Pang, S; Geng, J; Vaccaro, W; Poss, MA; Oconnell, J; Nowak, K; Jayaraman, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4438-4441 , 文章类型： Article，,卷期：2008年18-15]
- This study reports the identification and Hits to Leads optimization of inhibitors of coactivator associated arginine methyltransferase (CARM1). Compound 7b is a potent, selective inhibitor of CARM1. (c) 2008 Elsevier Lt...
- Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode
[作者：Finlay, MRV; Acton, DG; Andrews, DM; Barker, AJ; Dennis, M; Fisher, E; Graham, MA; Green, CP; Heaton, DW; Karoutchi, G; Loddick, SA; Morgentin, R; Roberts, A; Tucker, JA; Weir, HM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4442-4446 , 文章类型： Article，,卷期：2008年18-15]
- A piperazine series of cyclin-dependent kinase (CDK) inhibitors have been identified. The compounds exhibit excellent physiochemical properties and a novel binding mode, whereby a bridging interaction via a water molecul...
- Synthesis and in vitro evaluation of salvinorin A analogues: Effect of configuration at C(2) and substitution at C(18) (vol 16, pg 4679, 2006)
[作者：Beguin, C; Richards, MR; Li, JG; Wang, Y; Xu, W; Liu-Chen, LY; Carlezon, WA; Cohen, BM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4448-4448 , 文章类型： Correction，,卷期：2008年18-15]
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- Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2
[作者：DiMauro, EF; Buchanan, JL; Cheng, A; Emkey, R; Hitchcock, SA; Huang, L; Huang, MY; Janosky, B; Lee, JH; Li, X; Martin, MW; Tomlinson, SA; White, RD; Zheng, XM; Patel, VF; Fremeau, RT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4267-4274 , 文章类型： Article，,卷期：2008年18-15]
- Structural modifications to the central portion of the N-arylamide oxadiazole scaffold led to the identification of N-arylpiperidine oxadiazoles as conformationally constrained analogs that offered improved stability and...
- Cytotoxic calanquinone A from Calanthe arisanensis and its first total synthesis
[作者：Lee, CL; Nakagawa-Goto, K; Yu, D; Liu, YN; Bastow, KF; Morris-Natschke, SL; Chang, FR; Wub, YC; Lee, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4275-4277 , 文章类型： Article，,卷期：2008年18-15]
- Calanquinone A (1) was isolated from an EtOAc-soluble extract of Calanthe arisanensis through bioassay-guided fractionation. Its structure was identified by spectroscopic methods. Compound 1 showed potent cytotoxicity (E...
- Design and optimization of potent, selective antagonists of Oxytocin
[作者：Brown, A; Brown, L; Ellis, D; Puhalo, N; Smith, CR; Wallace, O; Watson, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4278-4281 , 文章类型： Article，,卷期：2008年18-15]
- A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagon...
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