- Novel tricyclic antagonists of the prostaglandin D-2 receptor DP2 with efficacy in a murine model of allergic rhinitis
[作者:Stearns, BA; Baccei, C; Bain, G; Broadhead, A; Clark, RC; Coate, H; Evans, JF; Fagan, P; Hutchinson, JH; King, C; Lee, C; Lorrain, DS; Prasit, P; Prodanovich, P; Santini, A; Scott, JM; Stock, NS; Truong, YP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4647-4651 , 文章类型: Article,,卷期:2009年19-16]
- The synthesis of a series of tricyclic antagonists for the prostaglandin D-2 receptor DP2 (CRTH2) is disclosed. The activities of the compounds were evaluated in a human DP2 binding assay and a human whole blood eosinoph...
- Glycolipid ester-type heterodimers from Ipomoea tyrianthina and their pharmacological activity
[作者:Leon-Rivera, I; Miron-Lopez, G; Estrada-Soto, S; Aguirre-Crespo, F; Gutierrez, MD; Molina-Salinas, GM; Hurtado, G; Navarrete-Vazquez, G; Montiel, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4652-4656 , 文章类型: Article,,卷期:2009年19-16]
- Tyrianthins A (1) and B (2), two new partially acylated glycolipid ester-type heterodimers were isolated from Ipomoea tyrianthina. Scammonic acid A was determined as the glycosidic acid in both monomeric units. Tyrianthi...
- Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y(12) antagonists for inhibition of platelet aggregation
[作者:Parlow, JJ; Burney, MW; Case, BL; Girard, TJ; Hall, KA; Hiebsch, RR; Huff, RM; Lachance, RM; Mischke, DA; Rapp, SR; Woerndle, RS; Ennis, MD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4657-4663 , 文章类型: Article,,卷期:2009年19-16]
- Polymer-assisted solution-phase (PASP) parallel library synthesis was used to discover a piperazinyl-glutamate-pyridine as a P2Y(12) antagonist. Exploitation of this lead provided compounds with excellent inhibition of p...
- Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists
[作者:Washburn, DG; Hoang, TH; Frazee, JS; Johnson, L; Hammond, M; Manns, S; Madauss, KP; Williams, SP; Duraiswami, C; Tran, TB; Stewart, EL; Grygielko, ET; Glace, LE; Trizna, W; Nagilla, R; Bray, JD; Thompson, SK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4664-4668 , 文章类型: Article,,卷期:2009年19-16]
- We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency com...
- Polyethylenimine effectively induces, stabilizes, and regulates intramolecular G-quadruplexes
[作者:Sun, HX; Zhou, QJ; Xiang, JF; Tang, YL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4669-4672 , 文章类型: Article,,卷期:2009年19-16]
- The interaction between polyethylenimine (PEI) and telomeric DNA was studied. The results demonstrated that PEI could effectively induce, stabilize, and regulate intramolecular G-quadruplexes. The mechanism for these res...
- Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors
[作者:Sato, Y; Onozaki, Y; Sugimoto, T; Kurihara, H; Kamijo, K; Kadowaki, C; Tsujino, T; Watanabe, A; Otsuki, S; Mitsuya, M; Iida, M; Haze, K; Machida, T; Nakatsuru, Y; Komatani, H; Kotani, H; Iwasawa, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4673-4678 , 文章类型: Article,,卷期:2009年19-16]
- A novel class of imidazopyridine derivatives was designed as PLK1 inhibitors. Extensive SAR studies supported by molecular modeling afforded a highly potent and selective compound 36. Compound 36 demonstrated good antitu...
- Discovery of highly potent and selective biphenylacylsulfonamide-based beta(3)-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the beta(2)-adrenergic receptor: Part 6
[作者:Hattori, K; Orita, M; Toda, S; Imanishi, M; Itou, S; Nakajima, Y; Tanabe, D; Washizuka, K; Araki, T; Sakurai, M; Matsui, S; Imamura, E; Ueshima, K; Yamamoto, T; Yamamoto, N; Ishikawa, H; Nakano, K; Unami, N; Hamada, K; Matsumura, Y; Takamura, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4679-4683 , 文章类型: Article,,卷期:2009年19-16]
- As an extension of research, we have investigated modification of left-hand side (LHS) of biphenyl analogues containing an acylsulfonamide moiety in the development of potent and selective human beta(3)-adrenergic recept...
- Ulmosides A and B: Flavonoid 6-C-glycosides from Ulmus wallichiana, stimulating osteoblast differentiation assessed by alkaline phosphatase
[作者:Rawat, P; Kumar, M; Sharan, K; Chattopadhyay, N; Maurya, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4684-4687 , 文章类型: Article,,卷期:2009年19-16]
- Chemical investigation of Ulmus wallichiana stem bark resulted in isolation and identification of three new compounds (2S,3S)-(+)-3',4',5,7-tetrahydroxydihydroflavonol-6-C-beta-D-glucopyranoside (1), (2S,3S)-(+)-4',5,7-t...
- C5-Modified nucleosides exhibiting anticancer activity
[作者:Lee, YS; Park, SM; Kim, HM; Park, SK; Lee, K; Lee, CW; Kim, BH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4688-4691 , 文章类型: Article,,卷期:2009年19-16]
- We describe (i) a simple method for the synthesis of C5-modified nucleosides from 5-iodo-2'deoxyuridine and (ii) their activity against six types of human cancer cell lines (HCT15, MM231, NCI-H23, NUGC-3, PC-3, ACHN). We...
- Substituted pyrimidines as cannabinoid CB1 receptor ligands
[作者:Kim, MJ; Kim, JY; Seo, HJ; Lee, J; Lee, SH; Kim, MS; Kang, J; Kim, J; Lee, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4692-4697 , 文章类型: Article,,卷期:2009年19-16]
- Cannabinoid CB1 receptors have been the avenue of extensive studies since the first clinical results of rimonabant (SR141716)for the treatment of obesity and obesity-related metabolic disorders were reported in 2001. To ...
- Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17 alpha-hydroxylase/17,20-lyase (P-450(17 alpha))
[作者:Ahmed, S; Shahid, I; Dhanani, S; Owen, CP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4698-4701 , 文章类型: Article,,卷期:2009年19-16]
- We report the synthesis and biochemical evaluation of a range of 4-sulfonated derivatives of 4-hydroxybenzyl imidazole which has been targetted against the two components of 17 alpha-hydroxylase/17,20-lyase (P-450(17 alp...
- Semi-synthesis and anti-proliferative activity evaluation of novel analogues of Honokiol
[作者:Luo, YF; Xu, YB; Chen, LJ; Hu, J; Peng, C; Xie, DC; Shi, JY; Huang, WC; Xu, GB; Peng, M; Han, J; Li, R; Yang, SY; Wei, YQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4702-4705 , 文章类型: Article,,卷期:2009年19-16]
- A series of honokiol analogues were synthesized by modifying the 5- and/or 3'-position(s) of honokiol to assess their anti-tumor effects. Some compounds exerted more potent anti-proliferative activities than those of hon...
- Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay
[作者:Nishizaki, Y; Ishimoto, Y; Hotta, Y; Hosoda, A; Yoshikawa, H; Akamatsu, M; Tamura, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4706-4710 , 文章类型: Article,,卷期:2009年19-16]
- The effect of 32 flavonoids on androgen (AR) and glucocorticoid receptors (GR) was investigated using an MDA-kb2 human breast cancer cell line to predict potential AR and GR activities. Among them, 5-hydroxyflavone (7) h...
- Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic
[作者:Wangsell, F; Russo, F; Savmarker, J; Rosenquist, A; Samuelsson, B; Larhed, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4711-4714 , 文章类型: Article,,卷期:2009年19-16]
- Two series of drug-like BACE-1 inhibitors with a shielded tertiary hydroxyl as transition state isostere have been synthesized. The most potent inhibitor exhibited a BACE-1 IC50 value of 0.23 mu M. (C) 2009 Elsevier Ltd....
- Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors
[作者:Olimpieri, F; Tambaro, S; Fustero, S; Lazzari, P; Sanchez-Rosello, M; Pani, L; Volonterio, A; Zanda, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4715-4719 , 文章类型: Article,,卷期:2009年19-16]
- A novel family of peptidomimetics incorporating fluoroalkyl groups, mainly a trifluoromethyl, in alpha-position to a zinc(II)-binding thiol function, was synthesized in solution as well as in solid-phase. These compounds...
- Design, synthesis and biological evaluation of new potent and highly selective ROS1-tyrosine kinase inhibitor
[作者:Park, BS; El-Deeb, IM; Yoo, KH; Oh, CH; Cho, SJ; Han, DK; Lee, HS; Lee, JY; Lee, SH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4720-4723 , 文章类型: Article,,卷期:2009年19-16]
- ROS1 protein is a receptor tyrosine kinase that has been reported mainly in meningiomas and astrocytomas, and until now, there is no selective inhibitor for this kinase. In this study, we illustrate for the synthesis of ...
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