- Acyl derivatives of boswellic acids as inhibitors of NF-kappa B and STATs
[作者:Kumar, A; Shah, BA; Singh, S; Hamid, A; Singh, SK; Sethi, VK; Saxena, AK; Singh, J; Taneja, SC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:431-435 , 文章类型: Article,,卷期:2012年22-1]
- Boswellic acid acylates including their epimers were synthesized and screened against a panel of human cancer cell lines. They exhibited a range of cytotoxicity against various human cancer cell lines thereby leading to ...
- Synthesis and antihyperglycemic evaluation of new 2,4-thiazolidinediones having biodynamic aryl sulfonylurea moieties
[作者:Jawale, DV; Pratap, UR; Rahuja, N; Srivastava, AK; Mane, RA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:436-439 , 文章类型: Article,,卷期:2012年22-1]
- New 2,4-thiazolidinediones with aryl sulfonylurea moieties 8a-h have been synthesized by condensing various substituted sulfonamides and 5-(isocyanatomethyl) thiazolidino-2,4-dione 6. The isocyanomethyl thiazolidinedione...
- Diamine and aminoalcohol derivatives active against Trypanosoma brucei
[作者:del Olmo, E; Diaz-Gonzalez, R; Escarcena, R; Carvalho, L; Bustos, LA; Navarro, M; San Feliciano, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:440-443 , 文章类型: Article,,卷期:2012年22-1]
- Twenty compounds selected as representative members of three series of long-chain 1,2-diamines, 2-amino-1-alkanols and 1-amino-2-alkanols structurally related to dihydrosphingosin, were synthesized and tested in vitro fo...
- Cyclic amino acid linkers stabilizing key loops of brain derived neurotrophic factor
[作者:Baeza, JL; de la Torre, BG; Santiveri, CM; Almeida, RD; Garcia-Lopez, MT; Gerona-Navarro, G; Jaffrey, SR; Jimenez, MA; Andreu, D; Gonzalez-Muniz, R; Martin-Martinez, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:444-448 , 文章类型: Article,,卷期:2012年22-1]
- Based on beta-turn-like BDNF loops 2 and 4, involved in receptor interaction, cyclic peptide replicas were designed, synthesized and tested. In addition to the native turn residues, the cyclic peptides include a linker u...
- Synthesis of dihydrofuran-fused perhydrophenanthrenes having a phenolic hydroxyl group as a novel anti-Alzheimer's disease agent
[作者:Sugimoto, K; Tamura, K; Ohta, N; Tohda, C; Toyooka, N; Nemoto, H; Matsuya, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:449-452 , 文章类型: Article,,卷期:2012年22-1]
- As a part of our research program on developing novel anti-Alzheimer's disease medicines, several dihydrofuran-fused perhydrophenanthrenes (DFs) possessing a phenolic hydroxyl group were found to exhibit potent dendritic...
- Synthesis and cytotoxic evaluation of thiourea and N-bis-benzothiazole derivatives: A novel class of cytotoxic agents
[作者:Kumbhare, RM; Dadmal, T; Kosurkar, U; Sridhar, V; Rao, JV,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:453-455 , 文章类型: Article,,卷期:2012年22-1]
- Benzothiazolyl thiocarbamides has been achieved using a catalytic amount of 4-dimethylaminopyridine (DMAP) followed by its chemoselective oxidative cyclization with 1,3-di-n-butylimidazolium tribromide[bbim][Br-3] to aff...
- Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases
[作者:Suzuki, N; Shiota, T; Watanabe, F; Haga, N; Murashi, T; Ohara, T; Matsuo, K; Omori, N; Yari, H; Dohi, K; Inoue, M; Iguchi, M; Sentou, J; Wada, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:456-460 , 文章类型: Article,,卷期:2012年22-1]
- 5-Alkenyl or 5-alkynyl-4-anilinopyrimidines were prepared and evaluated for in vitro inhibition of EGFR/Her-2 kinase activity and the growth of tumor cell lines (BT474 and N87). Several of these compounds inhibited the g...
- Ligand based design of novel histamine H-4 receptor antagonists; fragment optimization and analysis of binding kinetics
[作者:Smits, RA; Lim, HD; van der Meer, T; Kuhne, S; Bessembinder, K; Zuiderveld, OP; Wijtmans, M; de Esch, IJP; Leurs, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:461-467 , 文章类型: Article,,卷期:2012年22-1]
- The histamine H-4 receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H4R ligands, a low affinity isoquinoline frag...
- Development of phyllanthin containing microcapsules and their improved biological activity towards skin cells and Staphylococcus aureus
[作者:Lam, PL; Gambari, R; Yip, J; Yuen, MCW; Lam, KH; Wong, RSM; Wang, XW; Tang, JCO; Kok, SHL; Chui, CH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:468-471 , 文章类型: Article,,卷期:2012年22-1]
- Chitosan based microcapsule which encapsulated with phyllanthin was developed by simple coacervation. The composition and surface morphology of phyllanthin containing microcapsules were analyzed by Fourier Transform Infr...
- Fused thiophene derivatives as MEK inhibitors
[作者:Laing, VE; Brookings, DC; Carbery, RJ; Simorte, JG; Hutchings, MC; Langham, BJ; Lowe, MA; Allen, RA; Fetterman, JR; Turner, J; Meier, C; Kennedy, J; Merriman, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:472-475 , 文章类型: Article,,卷期:2012年22-1]
- A number of novel fused thiophene derivatives have been prepared and identified as potent inhibitors of MEK. The SAR data of selected examples and the in vivo profiling of compound 13h demonstrates the functional activit...
- Synthesis and antibacterial activity of a novel series of acylides active against community acquired respiratory pathogens
[作者:Kumar, R; Rathy, S; Hajare, AK; Surase, YB; Dullu, J; Jadhav, JS; Venkataramanan, R; Chakrabarti, A; Pandya, M; Bhateja, P; Ramkumar, G; Das, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:476-481 , 文章类型: Article,,卷期:2012年22-1]
- A novel series of acylides 4 were designed to overcome antibacterial resistance and evaluated for in vitro and in vivo activity. This series of acylides was designed from clarithromycin by changing the substitution on th...
- Synthesis, characterization and activity of new phosphonate dipeptides as potential inhibitors of VanX
[作者:Jia, C; Yang, KW; Liu, CC; Feng, L; Xiao, JM; Zhou, LS; Zhang, YL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:482-484 , 文章类型: Article,,卷期:2012年22-1]
- VanX, a Zn(II)-dependent D-ala-D-ala dipeptidase, is essential for vancomycin resistance in Enterococcus faecium. The enzymatic activity of VanX was previously found to be inhibited competitively by 2-{[(1-aminoethyl) (h...
- Synthesis and evaluation of novel prodrugs of caspase inhibitors
[作者:Charrier, JD; Durrant, SJ; Studley, J; Lawes, L; Weber, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:485-488 , 文章类型: Article,,卷期:2012年22-1]
- A novel type of caspase inhibitor prodrug that improves systemic exposure after oral administration in rats has been designed. Such a prodrug, based on a 6,6a-dihydrofuro[3,2-d]oxazol-5(3aH)-one motif, has the advantage ...
- Physicochemical properties and inhibition effect on iron deficiency anemia of a novel polysaccharide-iron complex (LPPC)
[作者:Zhang, ZS; Wang, XM; Han, ZP; Yin, L; Zhao, MX; Yu, SC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:489-492 , 文章类型: Article,,卷期:2012年22-1]
- Porphyran (P) was extracted from red algae Porphyra by boiling water. A novel polysaccharide-iron complex (LPPC) was prepared under the alkaline condition by adding a ferric chloride solution to the low molecular weight ...
- Developing potent backbone cyclic peptides bearing the shared epitope sequence as rheumatoid arthritis drug-leads
[作者:Naveh, S; Tal-Gan, Y; Ling, S; Hoffman, A; Holoshitz, J; Gilon, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:493-496 , 文章类型: Article,,卷期:2012年22-1]
- Rheumatoid arthritis (RA) is a common human leukocyte antigen-associated disease. Most RA patients have a five-residue sequence motif called the shared epitope (SE) in the DR beta-chain of the HLA-DRB1 protein. The SE wa...
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