- Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors
[作者:Wang, XL; Salaski, EJ; Berger, DM; Powell, D; Hu, YB; Wojciechowicz, D; Collins, K; Frommer, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6941-6944 , 文章类型: Article,,卷期:2011年21-23]
- Structure-guided design led to the discovery of novel chemical scaffolds for B-Raf inhibitors. Both type I and type II kinase inhibitors have been explored and lead compounds with good potency and excellent selectivity h...
- Improved radiosynthesis of the apoptosis marker (18)F-ICMT11 including biological evaluation
[作者:Glaser, M; Goggi, J; Smith, G; Morrison, M; Luthra, SK; Robins, E; Aboagye, EO,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6945-6949 , 文章类型: Article,,卷期:2011年21-23]
- We improved the specific radioactivity of the apoptosis imaging isatin derivative (18)F-ICMT11. We then evaluated (18)F-ICMT11 in EL4 tumor-bearing mice 24 h after treatment with etoposide/cyclophosphamide combination th...
- Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication
[作者:Skerlj, R; Bridger, G; Zhou, YX; Bourque, E; McEachern, E; Langille, J; Harwig, C; Veale, D; Yang, W; Li, TS; Zhu, YB; Bey, M; Baird, I; Sartori, M; Metz, M; Mosi, R; Nelson, K; Bodart, V; Wong, R; Fricker, S; Mac Farland, R; Huskens, D; Schols, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6950-6954 , 文章类型: Article,,卷期:2011年21-23]
- A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, pot...
- Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu(4)) antagonist: Unexpected 'molecular switch' from a closely related mGlu(4) positive allosteric modulator
[作者:Utley, T; Haddenham, D; Salovich, JM; Zamorano, R; Vinson, PN; Lindsley, CW; Hopkins, CR; Niswender, CM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6955-6959 , 文章类型: Article,,卷期:2011年21-23]
- Herein we report the discovery and SAR of a novel antagonist of metabotropic glutamate receptor 4 (mGlu(4)). The antagonist was discovered via a molecular switch from a closely related mGlu(4) positive allosteric modulat...
- Alkaloids from Chelidonium majus and their inhibitory effects on LPS-induced NO production in RAW264.7 cells
[作者:Park, JE; Cuong, TD; Hung, TM; Lee, I; Na, M; Kim, JC; Ryoo, S; Lee, JH; Choi, JS; Woo, MH; Min, BS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6960-6963 , 文章类型: Article,,卷期:2011年21-23]
- A new alkaloid, methyl 2'-(7,8-dihydrosanguinarine-8-yl)acetate (1), together with six known alkaloids, stylopine (2), protopine (3), norchelidonine (4), chelidonine (5), berberine (6), and 8-hydroxydihydrosanguinarine (...
- Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors
[作者:Lu, S; Luo, Q; Hao, X; Li, XC; Ji, LY; Zheng, W; Wang, FY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6964-6968 , 文章类型: Article,,卷期:2011年21-23]
- Six analogs of imatinib, an Abl kinase inhibitor clinically used as a first-line therapeutic agent for chronic myeloid leukaemia (CML), have been synthesized and characterized. And their potency as Abl kinase inhibitors ...
- Identification of nonplanar small molecule for G-quadruplex grooves: Molecular docking and molecular dynamic study
[作者:Li, JL; Jin, XQ; Hu, LH; Wang, JP; Su, ZM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6969-6972 , 文章类型: Article,,卷期:2011年21-23]
- DNA G-quadruplex is an attractive drug target for anticancer therapy. Most G-quadruplex ligands have little selectivity, due to p-stacking interaction with common G-tetrads surface. Thanks to the varieties of G-quadruple...
- Antibacterial and antitubercular activity of fosmidomycin, FR900098, and their lipophilic analogs
[作者:Uh, E; Jackson, ER; Jose, GS; Maddox, M; Lee, RE; Lee, RE; Boshoff, HI; Dowd, CS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6973-6976 , 文章类型: Article,,卷期:2011年21-23]
- The nonmevalonate pathway (NMP) of isoprene biosynthesis is an exciting new route toward novel antibiotic development. Inhibitors against several enzymes in this pathway are currently under examination. A significant lia...
- III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold
[作者:Kim, SH; Anilkumar, GN; Zawacki, LG; Zeng, QB; Yang, DY; Shao, YF; Dong, GZ; Xu, XL; Yu, WS; Jiang, YH; Jenh, CH; Hall, JW; Carroll, CD; Hobbs, DW; Baldwin, JJ; McGuinness, BF; Rosenblum, SB; Kozlowski, JA; Shankar, BB; Shih, NY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6982-6986 , 文章类型: Article,,卷期:2011年21-23]
- The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. Compound 16e with single-...
- Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity
[作者:Mihalic, JT; Chen, XQ; Fan, PC; Chen, X; Fu, Y; Liang, LM; Reed, M; Tang, L; Chen, JL; Jaen, J; Li, LP; Dai, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7001-7005 , 文章类型: Article,,卷期:2011年21-23]
- A new class of MCHR1 antagonists was discovered via a high-throughput screen. Optimization of the lead structure resulted in the identification of indole 10e. This compound possesses good pharmacokinetic properties acros...
- Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)
[作者:Watterson, SH; Langevine, CM; Van Kirk, K; Kempson, J; Guo, JQ; Spergel, SH; Das, J; Moquin, RV; Dyckman, AJ; Nirschl, D; Gregor, K; Pattoli, MA; Yang, XX; McIntyre, KW; Yang, GC; Galella, MA; Booth-Lute, H; Chen, LS; Yang, Z; Wang-Iverson, D; McKinnon, M; Dodd, JH; Barrish, JC; Burke, JR; Pitts, WJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7006-7012 , 文章类型: Article,,卷期:2011年21-23]
- The synthesis, structure-activity relationships (SAR), and biological results of pyridyl-substituted azaindole based tricyclic inhibitors of IKK2 are described. Compound 4m demonstrated potent in vitro potency, acceptabl...
- Spacer length effects on in vitro imaging and surface accessibility of fluorescent inhibitors of prostate specific membrane antigen
[作者:Liu, TC; Nedrow-Byers, JR; Hopkins, MR; Berkman, CE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:7013-7016 , 文章类型: Article,,卷期:2011年21-23]
- Prostate-specific membrane antigen (PSMA), a type II transmembrane protein, has been becoming an active target for imaging and therapeutic applications for prostate cancer. Recently, the development of its various chemic...
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