- Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors
[作者:Betancort, JM; Winn, DT; Liu, RZ; Xu, QS; Liu, JJ; Liao, WS; Chen, SH; Carney, D; Hanway, D; Schmeits, J; Li, XQ; Gordon, E; Campbell, DA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4437-4440 , 文章类型: Article,,卷期:2009年19-15]
- The synthesis and biochemical evaluation of novel cyanothiazolidine inhibitors of dipeptidyl peptidase 4 (DPP4) is described. Their main structural feature is a constrained bicyclic core that prevents the intramolecular ...
- Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors
[作者:Hammond, M; Washburn, DG; Hoang, TH; Manns, S; Frazee, JS; Nakamura, H; Patterson, JR; Trizna, W; Wu, C; Azzarano, LM; Nagilla, R; Nord, M; Trejo, R; Head, MS; Zhao, BG; Smallwood, AM; Hightower, K; Laping, NJ; Schnackenberg, CG; Thompson, SK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4441-4445 , 文章类型: Article,,卷期:2009年19-15]
- The lead serum and glucocorticoid-related kinase 1 (SGK1) inhibitors 4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid (1) and {4-[5-(2-naphthalenyl)-1H-pyrrolo[2,3-b] pyridin-3-yl]phenyl}acetic acid (2) suffer from...
- Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors
[作者:Owen, DR; Walker, JK; Jacobsen, EJ; Freskos, JN; Hughes, RO; Brown, DL; Bell, AS; Brown, DG; Phillips, C; Mischke, BV; Molyneaux, JM; Fobian, YM; Heasley, SE; Moon, JB; Stallings, WC; Rogier, DJ; Fox, DNA; Palmer, MJ; Ringer, T; Rodriquez-Lens, M; Cubbage, JW; Blevis-Bal, RM; Benson, AG; Acker, BA; Maddux, TM; Tollefson, MB; Bond, BR; MacInnes, A; Yu, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4088-4091 , 文章类型: Article,,卷期:2009年19-15]
- A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted p...
- Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system
[作者:Hughes, RO; Walker, JK; Cubbage, JW; Fobian, YM; Rogier, DJ; Heasley, SE; Blevis-Bal, RM; Benson, AG; Owen, DR; Jacobsen, EJ; Freskos, JN; Molyneaux, JM; Brown, DL; Stallings, WC; Acker, BA; Maddux, TM; Tollefson, MB; Williams, JM; Moon, JB; Mischke, BV; Rumsey, JM; Zheng, Y; MacInnes, A; Bond, BR; Yu, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4092-4096 , 文章类型: Article,,卷期:2009年19-15]
- Efforts to improve the potency and physical properties of the aminopyridiopyrazinone class of PDE5 inhibitors through modi. cation of the core ring system are described. Five new ring systems are evaluated and features t...
- Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors
[作者:Edmondson, SD; Mastracchio, A; Cox, JM; Eiermann, GJ; He, HB; Lyons, KA; Patel, RA; Patel, SB; Petrov, A; Scapin, G; Wu, JK; Xu, SY; Zhu, B; Thornberry, NA; Roy, RS; Weber, AE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4097-4101 , 文章类型: Article,,卷期:2009年19-15]
- A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, sel...
- The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms
[作者:Parkkila, S; Innocenti, A; Kallio, H; Hilvo, M; Scozzafava, A; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4102-4106 , 文章类型: Article,,卷期:2009年19-15]
- The protein tyrosine kinases (PTKs) are essential enzymes in cellular signaling processes that regulate cell growth, differentiation, migration and metabolism. Their inhibition was recently shown to constitute a new moda...
- 7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation
[作者:Li, MZ; Jin, W; Jiang, C; Zheng, C; Tang, WD; You, TP; Lou, LG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4107-4109 , 文章类型: Article,,卷期:2009年19-15]
- A series of 7-cycloalkylcamptothecin derivatives were synthesized from camptothecin with two methods. Their biological activities in vitro were evaluated with sulforhodamine-B (SRB) method on four types of human tumor ce...
- Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region
[作者:Aki, C; Chao, JP; Ferreira, JA; Dwyer, MP; Yu, YN; Chao, JH; Merritt, RJ; Lai, GF; Wu, ML; Hipkin, RW; Fan, XD; Gonsiorek, W; Fosseta, J; Rindgen, D; Fine, J; Lundell, D; Taveras, AG; Biju, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4446-4449 , 文章类型: Article,,卷期:2009年19-15]
- A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various amide modi. cations and substitution on the left side phenyl ring were prepared and found to show significant inhibitory activities tow...
- Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators
[作者:Ishikawa, M; Nonoshita, K; Ogino, Y; Nagae, Y; Tsukahara, D; Hosaka, H; Maruki, H; Ohyama, S; Yoshimoto, R; Sasaki, K; Nagata, Y; Eiki, J; Nishimura, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4450-4454 , 文章类型: Article,,卷期:2009年19-15]
- The synthesis and structure-activity-relationships (SARs) of novel 2-(pyridine-2-yl)-1H-benzimidazole glucokinase activators are described. Systematic modi. cation of benzimidazole lead 5a identified from a high-throughp...
- 4-(Phenylsulfonamidomethyl) benzamides as potent and selective inhibitors of the 11 beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice
[作者:Zhang, X; Zhou, Z; Yang, HY; Chen, JH; Feng, Y; Du, LL; Leng, Y; Shen, JH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4455-4458 , 文章类型: Article,,卷期:2009年19-15]
- Selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure-activity relationships, and ...
- On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents
[作者:Galvez-Peralta, M; Hackbarth, JS; Flatten, KS; Kaufmann, SH; Hiasa, H; Xing, CG; Ferguson, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4459-4462 , 文章类型: Article,,卷期:2009年19-15]
- The cytotoxicity and mechanism of action of a series of substituted 9-aminoacridines is evaluated using topoisomerase I and cancer cell growth inhibition assays. In previous work, compounds of this type were shown to cat...
- Tetrahydrocarbazole amides with potent activity against human papillomaviruses
[作者:Gudmundsson, KS; Boggs, SD; Sebahar, PR; Richardson, LD; Spaltenstein, A; Golden, P; Sethna, PB; Brown, KW; Moniri, K; Harvey, R; Romines, KR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4110-4114 , 文章类型: Article,,卷期:2009年19-15]
- Synthesis of a series of tetrahydrocarbazole amides with potent activity against human papillomaviruses is described. Synthetic approaches allowing for variation of the substitution pattern of the tetrahydrocarbazole and...
- Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue
[作者:Torino, D; Mollica, A; Pinnen, F; Lucente, G; Feliciani, F; Davis, P; Lai, J; Ma, SW; Porreca, F; Hruby, VJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4115-4118 , 文章类型: Article,,卷期:2009年19-15]
- Six new endomorphin analogues, incorporating constrained amino acids in place of native proline have been synthesized. Residues of (S)-azetidine-2-carboxylic acid (Aze), 3,4-dehydro-(S)-proline (Delta(3)Pro), azetidine-3...
- Synthesis and evaluation of 3 ''- and 4 ''-deoxy and -fluoro analogs of the immunostimulatory glycolipid, KRN7000
[作者:Raju, R; Castillo, BF; Richardson, SK; Thakur, M; Severins, R; Kronenberg, M; Howell, AR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4122-4125 , 文章类型: Article,,卷期:2009年19-15]
- Four 3 ''- and 4 ''-deoxy and -fluorogalactosyl ceramides were synthesized, and their ability to stimulate iNKT cells, based on levels of IL-2 production, was assessed in three NKT cell receptor hybridomas. In two of the...
- First steps in the direction of synthetic, allosteric, direct inhibitors of thrombin and factor Xa
[作者:Verghese, J; Liang, AY; Sidhu, PPS; Hindle, M; Zhou, QB; Desai, UR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4126-4129 , 文章类型: Article,,卷期:2009年19-15]
- Designing non-saccharide functional mimics of heparin is a major challenge. In this work, a library of small, aromatic molecules based on the sulfated DHP scaffold was synthesized and screened against thrombin and factor...
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