- Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors
[作者:Mortensen, DS; Perrin-Ninkovic, SM; Harris, R; Lee, BGS; Shevlin, G; Hickman, M; Khambatta, G; Bisonette, RR; Fultz, KE; Sankar, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6793-6799 , 文章类型: Article,,卷期:2011年21-22]
- We report here the discovery of a novel series of selective mTOR kinase inhibitors. A series of imidazo[ 4,5-b]pyrazin-2-ones, represented by screening hit 1, was developed into lead compounds with excellent mTOR potency...
- Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition
[作者:Hu, YH; Xing, L; Thomason, JR; Xiang, J; Ipek, M; Guler, S; Li, HQ; Sabatini, J; Chockalingam, P; Reifenberg, E; Sheldon, R; Morris, EA; Georgiadis, KE; Tam, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6800-6803 , 文章类型: Article,,卷期:2011年21-22]
- Design, synthesis and structure-activity relationship of a series of biphenylsulfonamido-3-methylbutanoic acid based aggrecanase-1 inhibitors are described. In addition to robust aggrecanase-1 inhibition, these compounds...
- Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivatives
[作者:Li, YB; Xie, YY; Du, NN; Lu, Y; Xu, HZ; Wang, B; Yu, Y; Liu, YX; Song, DQ; Chen, RX,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6804-6807 , 文章类型: Article,,卷期:2011年21-22]
- Tuberculosis (TB) is a major health problem worldwide. A series of novel sansanmycin derivatives were designed, semi-synthesized and evaluated for their activity against drug-susceptible Mycobacterium tuberculosis strain...
- New bioactive macrocyclic diterpenoids from Jatropha multifida
[作者:Kanth, BS; Kumar, AS; Shinde, DB; Babu, KH; Raju, TV; Kumar, CG; Sujitha, P; Das, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6808-6810 , 文章类型: Article,,卷期:2011年21-22]
- Two new macrocyclic diterpenoids, multifidanol (1) and multifidenol (2) along with several known compounds have been isolated from the stem of Jatropha multifida. The structures of the new compounds were established from...
- Synthesis and antioxidant activities of novel 4-Schiff base-7-benzyloxy-coumarin derivatives
[作者:Zhang, Y; Zou, BQ; Chen, ZF; Pan, YM; Wang, HS; Liang, H; Yi, XH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6811-6815 , 文章类型: Article,,卷期:2011年21-22]
- 4-Schiff base-7-benzyloxy-coumarins 5a(1)-5h(2) and its derivative 6 were designed and synthesized based on the 7-benzyloxy-coumarin structure as novel antioxidants. The in vitro antioxidant activities screening revealed...
- Protein binding site analysis by means of structural interaction fingerprint patterns
[作者:Mordalski, S; Kosciolek, T; Kristiansen, K; Sylte, I; Bojarski, AJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6816-6819 , 文章类型: Article,,卷期:2011年21-22]
- We introduce a new approach to the known concept of interaction profiles, based on Structural Interaction Fingerprints (SIFt), for precise and rapid binding site description. A set of scripts for batch generation and ana...
- Molecular dynamics simulations and MM/GBSA methods to investigate binding mechanisms of aminomethylpyrimidine inhibitors with DPP-IV
[作者:Liang, DS; Gao, J; Cheng, YH; Wei, C; Zhang, H; Ji, MJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6630-6635 , 文章类型: Article,,卷期:2011年21-22]
- The aminomethylpyrimidines were investigated as a novel class of DPP-IV inhibitors. In this Letter, the binding mechanisms of how slight change of substitution or position influences the binding affinity of five represen...
- A double prodrug system for colon targeting of benzenesulfonamide COX-2 inhibitors
[作者:Ruiz, JFM; Kedziora, K; Keogh, B; Maguire, J; Reilly, M; Windle, H; Kelleher, DP; Gilmer, JF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6636-6640 , 文章类型: Article,,卷期:2011年21-22]
- The design, synthesis and delivery potential of a new type of benzenesulfonamide cyclo-oxygenase-2 (COX-2) inhibitor prodrug is investigated using celecoxib. The approach involves a double prodrug that is activated first...
- A modular approach to trim cellular targets in anticancer drug discovery
[作者:Rios-Luci, C; Dominguez-Kelly, R; Leon, LG; Diaz-Rodriguez, E; Freire, R; Pandiella, A; Cikotiene, I; Padron, JM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6641-6645 , 文章类型: Article,,卷期:2011年21-22]
- A Phenotypic Drug Discovery strategy was applied to study a set of pyrimidine analogs prepared by means of intramolecular oxidation-reduction reactions of N-substituted-N-(2,6-disubstituted-5-nitro-4-pyrimidinyl) aminoac...
- 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site
[作者:Wang, W; Devasthale, P; Wang, AY; Harrity, T; Egan, D; Morgan, N; Cap, M; Fura, A; Klei, HE; Kish, K; Weigelt, C; Sun, L; Levesque, P; Li, YX; Zahler, R; Kirby, MS; Hamann, LG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6646-6651 , 文章类型: Article,,卷期:2011年21-22]
- Design, synthesis, and SAR of 7-oxopyrrolopyridine-derived DPP4 inhibitors are described. The preferred stereochemistry of these atropisomeric biaryl analogs has been identified as Sa. Compound (+)-3t, with a K(i) agains...
- Carbazole-containing arylcarboxamides as BACE1 inhibitors
[作者:Bertini, S; Asso, V; Ghilardi, E; Granchi, C; Manera, C; Minutolo, F; Saccomanni, G; Bortolato, A; Mason, J; Moro, S; Macchia, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6657-6661 , 文章类型: Article,,卷期:2011年21-22]
- beta-Secretase (BACE1) is widely recognized as a prime drug target for the treatment of Alzheimer's disease (AD). In this Letter, we report the synthesis and the BACE1 inhibitory activity of novel, variously substituted ...
- Synthesis and anti-tumor activities of N '-benzylidene-2-(4-oxothieno[2,3-d]pyrimidin-3(4H)-yl)acetohydrazone derivatives
[作者:Lou, JP; Liu, Z; Li, Y; Zhou, M; Zhang, ZX; Zheng, S; Wang, RX; Li, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6662-6666 , 文章类型: Article,,卷期:2011年21-22]
- A compound with a cyclic thienopyrimidine moiety and an aceto-hydrazone moiety in its chemical structure was discovered in a cell-based screening to have noticeable cytotoxicity on several tumor cell lines. A total of 38...
- Functional characterization of rat glutaryl-CoA dehydrogenase and its comparison with straight-chain acyl-CoA dehydrogenase
[作者:Wu, L; Qiao, YQ; Gao, JB; Deng, GS; Yu, WH; Chen, G; Li, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6667-6673 , 文章类型: Article,,卷期:2011年21-22]
- Glutaryl-CoA dehydrogenase catalyzes the oxidative decarboxylation of the gamma-carboxylate of the substrate, glutaryl-CoA, to yield crotonyl-CoA and CO(2). The enzyme is a member of the acyl-CoA dehydrogenase (ACD) fami...
- Synthesis and acrosin inhibitory activity of substituted 4-amino-N-(diaminomethylene) benzenesulfonamide derivatives
[作者:Ding, LL; Zhu, J; Zheng, CH; Sheng, CQ; Qi, JJ; Liu, XF; Han, GQ; Zhao, JT; Lv, JG; Zhou, YJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6674-6677 , 文章类型: Article,,卷期:2011年21-22]
- A series of new substituted 4-amino-N-(diaminomethylene) benzenesulfonamides were synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds showed potent acrosin inhibitory activi...
- Synthesis of polyfunctionalized piperidone oxime ethers and their cytotoxicity on HeLa cells
[作者:Parthiban, P; Pallela, R; Kim, SK; Park, DH; Jeong, YT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6678-6686 , 文章类型: Article,,卷期:2011年21-22]
- A series of twenty 2,6-diarylpiperidin-4-one O-methyloximes were synthesized with fluoro/chloro/bromo/methyl/methoxy/ethoxy/isopropyl substituents on various positions of the phenyl at C-2 and C-6 in association with/wit...
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