- New antifungal peptides. Synthesis, bioassays and initial structure prediction by CD spectroscopy
[作者：Olivella, MS; Rodriguez, AM; Zacchino, SA; Somlai, C; Penke, B; Farkas, V; Perczel, A; Enriz, RD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4808-4811 , 文章类型： Article，,卷期：2010年20-16]
- The synthesis, in vitro evaluation and conformational study of KKWKMRRNQFWIKIQR-NH2, HFRWRQIKIWFQNRRMKWKK-NH2 and RQPKIWFPNRRKPWKK-NH2 acting as antifungal agents are reported. These peptides displayed a moderate but sig...
- Structure and activity relationships of tartrate-based TACE inhibitors
[作者：Li, DS; Popovici-Muller, J; Belanger, DB; Caldwell, J; Dai, CY; David, M; Girijavallabhan, VM; Lavey, BJ; Lee, JF; Liu, ZD; Mazzola, R; Rizvi, R; Rosner, KE; Shankar, B; Spitler, J; Ting, PC; Vaccaro, H; Yu, WS; Zhou, GW; Zhu, ZN; Niu, XD; Sun, J; Guo, ZY; Orth, P; Chen, SY; Kozlowski, JA; Lundell, DJ; Madison, V; McKittrick, B; Piwinski, JJ; Shih, NY; Shipps, GW; Siddiqui, MA; Strickland, CO,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4812-4815 , 文章类型： Article，,卷期：2010年20-16]
- The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs dem...
- 1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists
[作者：Kern, JC; Terefenko, E; Trybulski, E; Berrodin, TJ; Cohen, J; Winneker, RC; Yudt, MR; Zhang, ZM; Zhu, YA; Zhang, PW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4816-4818 , 文章类型： Article，,卷期：2010年20-16]
- Non-steroidal 1-methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalenes and acyclic derivatives were evaluated as novel series of progesterone receptor (PR) antagonists using the T47D cell alkaline phosphatase...
- Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site
[作者：Montalban, AG; Boman, E; Chang, CD; Ceide, SC; Dahl, R; Dalesandro, D; Delaet, NGJ; Erb, E; Ernst, JT; Gibbs, A; Kahl, J; Kessler, L; Kucharski, J; Lum, C; Lundstrom, J; Miller, S; Nakanishi, H; Roberts, E; Saiah, E; Sullivan, R; Urban, J; Wang, ZJ; Larson, CJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4819-4824 , 文章类型： Article，,卷期：2010年20-16]
- We have optimized a novel series of potent p38 MAP kinase inhibitors based on an alpha-ketoamide scaffold through structure based design that due to their extended molecular architecture bind, in addition to the ATP site...
- Discovery of novel alpha 7 nicotinic receptor antagonists
[作者：Peng, YY; Zhang, QA; Snyder, GL; Zhu, HW; Yao, W; Tomesch, J; Papke, RL; O'Callaghan, JP; Welsh, WJ; Wennogle, LP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4825-4830 , 文章类型： Article，,卷期：2010年20-16]
- Two distinct families of small molecules were discovered as novel alpha 7 nicotinic acetylcholine receptor (nAChR) antagonists by pharmacophore-based virtual screening. These novel antagonists exhibited selectivity for t...
- Anti-T. cruzi activities and QSAR studies of 3-arylquinoxaline-2-carbonitrile di-N-oxides
[作者：Vicente, E; Duchowicz, PR; Benitez, D; Castro, EA; Cerecetto, H; Gonzalez, M; Monge, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4831-4835 , 文章类型： Article，,卷期：2010年20-16]
- In a continuing effort to identify new active compounds for combating Chagas disease and other neglected diseases, our research group synthesized and evaluated 23 3-arylquinoxaline-2-carbonitrile di-N-oxides against Tryp...
- Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution
[作者：Miura, T; Hidaka, K; Uemura, T; Kashimoto, K; Hori, Y; Kawasaki, Y; Ruben, AJ; Freire, E; Kimura, T; Kiso, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4836-4839 , 文章类型： Article，,卷期：2010年20-16]
- We attached 2-aminoethylamino groups to allophenylnorstatine-containing plasmepsin (Plm) inhibitors and investigated SAR of the methyl or ethyl substitutions on the amino groups. Unexpectedly, compounds 22 (KNI-10743) an...
- Fluorine-18 labeled galactosylated chitosan for asialoglycoprotein-receptor-mediated hepatocyte imaging
[作者：Yang, WJ; Mou, TT; Guo, WY; Jing, HH; Peng, C; Zhang, XZ; Ma, YC; Liu, BL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4840-4844 , 文章类型： Article，,卷期：2010年20-16]
- Galactosylated chitosan (GC) was prepared by reacting lactobionic acid with water-soluble chitosan. GC was labeled with fluorine-18 by conjugation with N-succinimidyl-4-F-18-fluorobenzoate ([F-18]SFB) under a slightly ba...
- Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus
[作者：McGuigan, C; Madela, K; Aljarah, M; Gilles, A; Brancale, A; Zonta, N; Chamberlain, S; Vernachio, J; Hutchins, J; Hall, A; Ames, B; Gorovits, E; Ganguly, B; Kolykhalov, A; Wang, J; Muhammad, J; Patti, JM; Henson, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4850-4854 , 文章类型： Article，,卷期：2010年20-16]
- We herein report a novel double pro-drug approach applied to the anti-HCV agent 2'-beta-C-methyl guanosine. A phosphoramidate ProTide motif and a 6-O-methoxy base pro-drug moiety are combined to generate lipophilic prodr...
- Morroniside cinnamic acid conjugate as an anti-inflammatory agent
[作者：Takeda, Y; Tanigawa, N; Sunghwa, F; Ninomiya, M; Hagiwara, M; Matsushita, K; Koketsu, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4855-4857 , 文章类型： Article，,卷期：2010年20-16]
- A morroniside cinnamic acid conjugate was prepared and evaluated on E-selectin mediated cell-cell adhesion as an important role in inflammatory processes. 7-O-Cinnamoylmorroniside exhibited excellent anti-inflammatory ac...
- Synthesis of potent chemical inhibitors of dynamin GTPase
[作者：Lee, S; Jung, KY; Park, J; Cho, JH; Kim, YC; Chang, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4858-4864 , 文章类型： Article，,卷期：2010年20-16]
- Dynamin is a key regulatory protein in clathrin mediated endocytosis. Compared to genetic or immunological tools, small chemical dynamin inhibitors such as dynasore have the potential to study the dynamic nature of endoc...
- Synthesis and anti-cancer activity of chalcone linked imidazolones
[作者：Kamal, A; Ramakrishna, G; Raju, P; Viswanath, A; Ramaiah, MJ; Balakishan, G; Pal-Bhadra, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4865-4869 , 文章类型： Article，,卷期：2010年20-16]
- A series of novel chalcone linked imidazolones were prepared and evaluated for their anti-cancer activity against a panel of 53 human tumour cell lines derived from nine different cancer types: leukemia, lung, colon, CNS...
- Identification of N-(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides as novel inhibitors of GlyT1
[作者：Varnes, JG; Forst, JM; Hoerter, TN; Holmquist, CR; Wilkins, DE; Tian, GC; Jonak, G; Wang, X; Potts, WM; Wood, MW; Alhambra, C; Brugel, TA; Albert, JS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4878-4881 , 文章类型： Article，,卷期：2010年20-16]
- A novel series of glycine transporter 1 (GlyT1) inhibitors is described. Scoping of the heterocycle moiety of hit 4-chlorobenzenesulfonamide 1 led to replacement of the piperidine with an azepane for a modest increase in...
- A newly synthesized, potent tyrosinase inhibitor: 5-(6-Hydroxy-2-naphthyl)-1,2,3-benzenetriol
[作者：Choi, J; Bae, SJ; Ha, YM; No, JK; Lee, EK; Lee, JS; Song, S; Lee, H; Suh, H; Yu, BP; Chung, HY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4882-4884 , 文章类型： Article，,卷期：2010年20-16]
- In searching for new agents with a depigmenting effect, we synthesized a derivative of resveratrol, 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol ( 5HNB) with a potent tyrosinase inhibitory activity. 5HNB inhibited mushroo...
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