- Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors
[作者:Ramurthy, S; Costales, A; Jansen, JM; Levine, B; Renhowe, PA; Shafer, CM; Subramanian, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1678-1681 , 文章类型: Article,,卷期:2012年22-4]
- Compounds belonging to several scaffolds-quinazolines, quinolines and quinoxalines-were designed and synthesized as Raf kinase inhibitors. Scaffolds were assessed for in vitro Braf(V600E) inhibition, and overall kinase s...
- Reductive activation of 5-fluorodeoxyuridine prodrug possessing azide methyl group by hypoxic X-irradiation
[作者:Tanabe, K; Ishizaki, J; Ando, Y; Ito, T; Nishimoto, SI,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1682-1685 , 文章类型: Article,,卷期:2012年22-4]
- We prepared a 5-fluorodeoxyuridine (5-FdUrd) derivative possessing azide methyl group (N-3-FdUrd) as a novel radiation-activated prodrug. The parent antitumor agent, 5-FdUrd, was released efficiently from N-3-FdUrd by hy...
- Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists
[作者:Liu, JW; Wang, YC; Johnson, MG; Li, AR; Shen, W; Wang, XM; Su, YL; Brown, M; Van Lengerich, B; Rickel, E; Martin, T; Budelsky, A; Seitz, L; Danao, J; Tang, HL; Collins, T; Medina, JC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1686-1689 , 文章类型: Article,,卷期:2012年22-4]
- Our first generation CRTH2 and DP dual antagonists, represented by AMG 009, are more potent toward the CRTH2 receptor than to the DP receptor. Here we report our efforts in the discovery of CRTH2 and DP dual antagonists ...
- Discovery of aminopiperidine-based Smac mimetics as IAP antagonists
[作者:Hennessy, EJ; Saeh, JC; Sha, L; MacIntyre, T; Wang, H; Larsen, NA; Aquila, BM; Ferguson, AD; Laing, NM; Omer, CA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1690-1694 , 文章类型: Article,,卷期:2012年22-4]
- A series of structurally unique Smac mimetics that act as antagonists of inhibitor of apoptosis proteins (IAPs) has been discovered. While most previously described Smac mimetics contain the proline ring (or a similar cy...
- Computational study of bindings of HK20 Fab and D5 Fab to HIV-1 gp41
[作者:Hartono, YD; Lazim, R; Yip, YM; Zhang, DW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1695-1700 , 文章类型: Article,,卷期:2012年22-4]
- Antibodies HK20 and D5 have been shown to target HIV-1 gp41, thereby inhibiting membrane fusion that facilitates viral entry. The binding picture is static, based on the X-ray crystal structures of the Fab regions and gp...
- Inhibition of human monoamine oxidase A and B by 5-phenoxy 8-aminoquinoline analogs
[作者:Chaurasiya, ND; Ganesan, S; Nanayakkara, NPD; Dias, LRS; Walker, LA; Tekwani, BL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1701-1704 , 文章类型: Article,,卷期:2012年22-4]
- 8-Aminoquinolines (8-AQs) are important class of anti-infective therapeutics. 5-Phenoxy 8-aminoquinoline analogs have shown improved metabolic stability compared to primaquine. In view or predictive role of monoamine oxi...
- Synthesis and antihormonal properties of novel 11 beta-benzoxazole-substituted steroids
[作者:Jin, CY; Fix, SE; Kepler, JA; Cook, CE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1705-1708 , 文章类型: Article,,卷期:2012年22-4]
- Early studies led to the identification of 11 beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17 beta,4'-oxazole] analogs with potent and more selective antiprogestational activity compared to antiglucocorticoid activity th...
- Synthesis and antikinetoplastid activity of a series of N,N '-substituted diamines
[作者:Caminos, AP; Panozzo-Zenere, EA; Wilkinson, SR; Tekwani, BL; Labadie, GR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1712-1715 , 文章类型: Article,,卷期:2012年22-4]
- A series of 25 N,N'-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity o...
- Discovery of diphenyl lactam derivatives as N-type calcium channel blockers
[作者:Doherty, GA; Bhatia, P; Vortherms, TA; Marsh, KC; Wetter, JM; Mack, H; Scott, VE; Jarvis, MF; Stewart, AO,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1716-1718 , 文章类型: Article,,卷期:2012年22-4]
- A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 dem...
- Structurally diverse disaccharide analogs of antifreeze glycoproteins and their ability to inhibit ice recrystallization
[作者:Balcerzak, AK; Ferreira, SS; Trant, JF; Ben, RN,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1719-1721 , 文章类型: Article,,卷期:2012年22-4]
- The beta-D-galactosyl-(1,3)-alpha-N-acetyl-D-galactosamine disaccharide is present in antifreeze glycoproteins (AFGPs). Analogs of this disaccharide including the beta-linked (1,3)-, (1,4)-, and (1,6)-galactosyl-N-acetyl...
- Efficient synthesis and cell-based silencing activity of siRNAS that contain triazole backbone linkages
[作者:Efthymiou, TC; Huynh, V; Oentoro, J; Peel, B; Desaulniers, JP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1722-1726 , 文章类型: Article,,卷期:2012年22-4]
- An efficient synthesis of siRNAs modified at the backbone with a triazole functionality is reported. Through the use of 4,4'-dimethoxytrityl (DMT) phosphoramidite chemistry, triazole backbone dimers were site-specificall...
- Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors
[作者:Wu, ZC; Yang, CM; Graham, TH; Verras, A; Chabin, RM; Xu, SY; Tong, XC; Xie, D; Lassman, ME; Bhatt, UR; Garcia-Calvo, MM; Shen, Z; Chen, Q; Bleasby, K; Sinharoy, R; Hale, JJ; Tata, JR; Pinto, S; Colletti, SL; Shen, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1727-1730 , 文章类型: Article,,卷期:2012年22-4]
- Efforts were dedicated to develop potent and brain penetrant prolylcarboxypeptidase (PrCP) inhibitors by replacing the amide group of original leads 1 and 2 with heterocycles. Aminopyrimidines including compound 32a were...
- Hybrid liposomes affect cellular lipid constituents and caveolae structures
[作者:Cao, K; Tanaka, K; Komizu, Y; Tamiya-Koizumi, K; Murate, T; Ueoka, R; Kyogashima, M; Usukura, J; Takahashi, T; Suzuki, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1731-1733 , 文章类型: Article,,卷期:2012年22-4]
- We examined alterations of lipid constituents induced by hybrid liposomes (HLs) in cancer cells. As early as 1 h after HL treatment, amounts of the raft/caveolae lipids sphingomyelin, ceramide, and ether-type PC were alt...
- New ionic derivatives of betulinic acid as highly potent anti-cancer agents
[作者:Suresh, C; Zhao, H; Gumbs, A; Chetty, CS; Bose, HS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1734-1738 , 文章类型: Article,,卷期:2012年22-4]
- Betulinic acid is a natural compound with high in vitro cytotoxicity toward many cancer cells. However, the poor water solubility of this compound hampers an effective in vivo cancer study. We prepared new ionic derivati...
- Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors
[作者:Song, B; Xiao, T; Qi, XL; Li, LN; Qin, KY; Nian, SY; Hu, GX; Yu, YF; Liang, G; Ye, FQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1739-1742 , 文章类型: Article,,卷期:2012年22-4]
- Monoamine oxidase-B (MAO-B) inhibitor has been used as neuroprotectants to treat the motor deficits of Parkinson's disease (PD). We designed and synthesized a class of 8-substituted benzamido-phenylxanthine derivatives a...
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