- Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells
[作者：Petrov, RR; Ferrini, ME; Jaffar, Z; Thompson, CM; Roberts, K; Diaz, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5859-5862 , 文章类型： Article，,卷期：2011年21-19]
- Cannabinoid CB2 receptor has emerged as a very promising target over the last decades. We have synthesized and evaluated a new fluorescent probe designated NMP6 based on 6-methoxyisatin scaffold, which exhibited selectiv...
- Metal-free cleavage efficiency toward DNA by a novel PNA analog-bridged macrocyclic polyamine
[作者：Wang, MQ; Zhang, J; Zhang, Y; Zhang, DW; Liu, Q; Liu, JL; Lin, HH; Yu, XQ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5866-5869 , 文章类型： Article，,卷期：2011年21-19]
- In this report we describe the synthesis of a new class of cyclen-contained compounds with novel peptide nucleic acid (PNA) analog motif. Target bis-cyclen derivative B was prepared and characterized by ESIMS, NMR and HP...
- Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors
[作者：Zeng, HB; Belanger, DB; Curran, PJ; Shipps, GW; Miao, H; Bracken, JB; Siddiqui, MA; Malkowski, M; Wang, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5870-5875 , 文章类型： Article，,卷期：2011年21-19]
- A series of substituted imidazo[1,2-a]pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low-nanomolar Brk inhibition activity, high selec...
- Ursolic acid is a PPAR-alpha agonist that regulates hepatic lipid metabolism
[作者：Jia, Y; Bhuiyan, MJH; Jun, HJ; Lee, JH; Hoang, MH; Lee, HJ; Kim, N; Lee, D; Hwang, KY; Hwang, BY; Choi, DW; Lee, SJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5876-5880 , 文章类型： Article，,卷期：2011年21-19]
- In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-alpha in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy t...
- Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers
[作者：Woo, HM; Lee, YS; Roh, EJ; Seo, SH; Song, CM; Chung, HJ; Pae, AN; Shin, KJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5910-5915 , 文章类型： Article，,卷期：2011年21-19]
- To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 4-piperidinecarboxylate and 4-piperidinecyanide derivatives were prepared and evaluated for in vitro and in vivo activity a...
- MDM2-p53 protein-protein interaction inhibitors: A-ring substituted isoindolinones
[作者：Watson, AF; Liu, JF; Bennaceur, K; Drummond, CJ; Endicott, JA; Golding, BT; Griffin, RJ; Haggerty, K; Lu, XH; McDonnell, JM; Newell, DR; Noble, MEM; Revill, CH; Riedinger, C; Xu, Q; Zhao, Y; Lunec, J; Hardcastle, IR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5916-5919 , 文章类型： Article，,卷期：2011年21-19]
- Structure-activity relationships for the MDM2-p53 inhibitory activity of a series of A-ring substituted 2-N-benzyl-3-(4-chlorophenyl)-3-(1-(hydroxymethyl) cyclopropyl)methoxy) isoindolinones have been investigated, givin...
- Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate
[作者：Singh, RK; Mandal, T; Balsubramanian, N; Viaene, T; Leedahl, T; Sule, N; Cook, G; Srivastava, DK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5920-5923 , 文章类型： Article，,卷期：2011年21-19]
- We report, for the first time, that certain N-acetylthiourea derivatives serve as highly potent and isozyme selective activators for the recombinant form of human histone deacetylase-8 in the assay system containing Fluo...
- Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure
[作者：Kley, JT; Mack, J; Hamilton, B; Scheuerer, S; Redemann, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5924-5927 , 文章类型： Article，,卷期：2011年21-19]
- Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool co...
- Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells
[作者：Radi, M; Brullo, C; Crespan, E; Tintori, C; Musumeci, F; Biava, M; Schenone, S; Dreassi, E; Zamperini, C; Maga, G; Pagano, D; Angelucci, A; Bologna, M; Botta, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5928-5933 , 文章类型： Article，,卷期：2011年21-19]
- Neuroblastoma (NB) represents the most common extracranial paediatric solid tumor for which no specific FDA-approved treatment is currently available. The tyrosine kinase c-Src has been reported to play an important role...
- Synthesis and evaluation of furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinoline as anticancer and multidrug resistance reversal agents
[作者：Zou, ZH; Lan, XB; Qian, H; Huang, WL; Li, YM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5934-5938 , 文章类型： Article，,卷期：2011年21-19]
- Multidrug resistance in tumor cells poses a major obstacle to efficient chemotherapy. Several types of agents have been recognized as multidrug resistance inhibitors, among which the tetrahydroisoquinolines is the most s...
- Discovery of a highly potent series of TLR7 agonists
[作者：Jones, P; Pryde, DC; Tran, TD; Adam, FM; Bish, G; Calo, F; Ciaramella, G; Dixon, R; Duckworth, J; Fox, DNA; Hay, DA; Hitchin, J; Horscroft, N; Howard, M; Laxton, C; Parkinson, T; Parsons, G; Proctor, K; Smith, MC; Smith, N; Thomas, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5939-5943 , 文章类型： Article，,卷期：2011年21-19]
- The discovery of a series of highly potent and novel TLR7 agonist interferon inducers is described. Structure- activity relationships are presented, along with pharmacokinetic studies of a lead molecule from this series ...
- New betulinic acid derivatives as potent proteasome inhibitors
[作者：Qian, KD; Kim, SY; Hung, HY; Huang, L; Chen, CH; Lee, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5944-5947 , 文章类型： Article，,卷期：2011年21-19]
- In this study, 22 new betulinic acid (BA) derivatives were synthesized and tested for their inhibition of the chymotrypsin-like activity of 20S proteasome. From the SAR study, we concluded that the C-3 and C-30 positions...
- Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3 beta
[作者：Cociorva, OM; Li, B; Nomanbhoy, T; Li, Q; Nakamura, A; Nakamura, K; Nomura, M; Okada, K; Seto, S; Yumoto, K; Liyanage, M; Zhang, MC; Aban, A; Leen, B; Szardenings, AK; Rosenblum, JS; Kozarich, JW; Kohno, Y; Shreder, KR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5948-5951 , 文章类型： Article，,卷期：2011年21-19]
- The synthesis, GSK-3 beta inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone-3-carboxylic acid scaffold were studied. Kinase selectivity profili...
- Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors
[作者：Ni, YK; Gopalsamy, A; Cole, D; Hu, YH; Denny, R; Ipek, M; Liu, J; Lee, J; Hall, JP; Luong, M; Telliez, JB; Lin, LL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5952-5956 , 文章类型： Article，,卷期：2011年21-19]
- We report here the synthesis and SAR of a new series of thieno[3,2-d]pyrimidines as potent Tpl2 kinase inhibitors. The proposed binding mode suggests the potential flipped binding mode depending on the substitution. Biac...
- Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists
[作者：Zhou, DH; Gross, JL; Sze, JY; Adedoyin, AB; Bowlby, M; Di, L; Platt, BJ; Zhang, GM; Brandon, N; Comery, TA; Robichaud, AJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5957-5960 , 文章类型： Article，,卷期：2011年21-19]
- On the basis of the previously reported benzimidazole 1,3'-bipyrrolidine benzamides (1), a series of related pyrrolidin-3-yl-N-methylbenzamides were synthesized and evaluated as H(3) receptor antagonists. In particular, ...
|