- Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates
[作者:Dudkin, VY; Rickert, K; Kreatsoulas, C; Wang, C; Arrington, KL; Fraley, ME; Hartman, GD; Yan, YW; Ikuta, M; Stirdivant, SM; Drakas, RA; Walsh, ES; Hamilton, K; Buser, CA; Lobell, RB; Sepp-Lorenzino, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2609-2612 , 文章类型: Article,,卷期:2012年22-7]
- Pyridyl aminothiazoles comprise a novel class of ATP-competitive Chk1 inhibitors with excellent inhibitory potential. Modification of the core with ethylenediamine amides provides compounds with low picomolar potency and...
- Pyridyl aminothiazoles as potent Chk1 inhibitors: Optimization of cellular activity
[作者:Dudkin, VY; Wang, C; Arrington, KL; Fraley, ME; Hartman, GD; Stirdivant, SM; Drakas, RA; Rickert, K; Walsh, ES; Hamilton, K; Buser, CA; Hardwick, J; Tao, WK; Beck, SC; Mao, XZ; Lobell, RB; Sepp-Lorenzino, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2613-2619 , 文章类型: Article,,卷期:2012年22-7]
- Translation of significant biochemical activity of pyridyl aminothiazole class of Chk1 inhibitors into functional CEA potency required analysis and adjustment of both physical properties and kinase selectivity profile of...
- A novel series of benzimidazole NR2B-selective NMDA receptor antagonists
[作者:Davies, DJ; Crowe, M; Lucas, N; Quinn, J; Miller, DD; Pritchard, S; Grose, D; Bettini, E; Calcinaghi, N; Virginio, C; Abberley, L; Goldsmith, P; Michel, AD; Chessell, IP; Kew, JNC; Miller, ND; Gunthorpe, MJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2620-2623 , 文章类型: Article,,卷期:2012年22-7]
- A series of novel benzimidazoles are discussed as NR2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists. High throughput screening (HTS) efforts identified a number of potent and selective NR2B antagonists such...
- Discovery of GS-9451: An acid inhibitor of the hepatitis C virus NS3/4A protease
[作者:Sheng, XC; Appleby, T; Butler, T; Cai, RB; Chen, XW; Cho, AS; Clarke, MO; Cottell, J; Delaney, WE; Doerffler, E; Link, J; Ji, MZ; Pakdaman, R; Pyun, HJ; Wu, QY; Xu, J; Kim, CU,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2629-2634 , 文章类型: Article,,卷期:2012年22-7]
- The discovery of GS-9451 is reported. Modification of the P3 cap and P2 quinoline with a series of solubilizing groups led to the identification of potent HCV NS3 protease inhibitors with greatly improved pharmacokinetic...
- 2-Amidino analogs of glycine-amiloride conjugates: Inhibitors of urokinase-type plasminogen activator
[作者:Massey, AP; Harley, WR; Pasupuleti, N; Gorin, FA; Nantz, MH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2635-2639 , 文章类型: Article,,卷期:2012年22-7]
- The relative non-toxicity of the diuretic amiloride, coupled with its selective inhibition of the protease urokinase plasminogen activator (uPA), makes this compound class attractive for structure-activity studies. Herei...
- Synthesis and antimycobacterial evaluation of N-substituted 3-aminopyrazine-2,5-dicarbonitriles (vol 22, pg 1598, 2012)
[作者:Zitko, J; Jampilek, J; Dobrovolny, L; Svobodova, M; Kunes, J; Dolezal, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2640-2640 , 文章类型: Correction,,卷期:2012年22-7]
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- Antiviral activity of novel 2 '-fluoro-6 '-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants (vol 21, pg 6328, 2011)
[作者:Wang, JN; Singh, US; Rawal, RK; Sugiyama, M; Yoo, J; Jha, AK; Scroggin, M; Huang, ZH; Murray, MG; Govindarajan, R; Tanaka, Y; Korba, B; Chu, CK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2641-2641 , 文章类型: Correction,,卷期:2012年22-7]
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