- Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17a-hydroxylase-17,20-lyase (CYP17)-Part II: Core rigidification and influence of substituents at the methylene bridge.
[作者:Hu, Qingzhong;Negri, Matthias;Jahn-Hoffmann, Kerstin;Zhuang, Yan;Olgen, Sureyya;Bartels, Marc;Mueller-Vieira, Ursula;Lauterbach, Thomas;Hartmann, Rolf W.;,期刊:Bioorganic & Medicinal Chemistry, 页码:7715-7727 , 文章类型: 研究论文,,卷期:2008年16-16]
- Thirty-five novel substituted imidazolyl methylene biphenyls have been synthesized as CYP17 inhibitors for the potential treatment of prostate cancer. Their activities have been tested with recombinant human CYP17 expre...
- Array-based fluorescence assay for serine/threonine kinases using specific chemical reaction.
[作者:Akita, Shoji;Umezawa, Naoki;Kato, Nobuki;Higuchi, Tsunehiko;,期刊:Bioorganic & Medicinal Chemistry, 页码:7788-7794 , 文章类型: 研究论文,,卷期:2008年16-16]
- serine/threonine kinases using a peptide array. Our approach is based on chem. reactions specific to phosphoserine and phosphothreonine residues, i.e., base-mediated b-elimination of the phosphate group and subsequent M...
- New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties.
[作者:Leon, Rafael;de los Rios, Cristobal;Marco-Contelles, Jose;Huertas, Oscar;Barril, Xavier;Luque, F. Javier;Lopez, Manuela G.;Garcia, Antonio G.;Villarroya, Mercedes;,期刊:Bioorganic & Medicinal Chemistry, 页码:7759-7769 , 文章类型: 研究论文,,卷期:2008年16-16]
- tacripyrimedones 1-5, a series of new tacrine-1,4-dihydropyridine hybrids bearing the general structure of 11-amino-12-aryl-3,3-dimethyl-3,4,5,7,8,9,10,12-octahydrodibenzo[b,g] [1,8]naphthyridine-1(2H)-one. These multif...
- Synthesis, DNA-binding ability and evaluation of antitumour activity of triazolo[1,2,4]benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates.
[作者:Kamal, Ahmed;Khan, M. Naseer A.;Srikanth, Y. V. V.;Reddy, K. Srinivasa;Juvekar, Aarti;Sen, Subrata;Kurian, Nisha;Zingde, Surekha;,期刊:Bioorganic & Medicinal Chemistry, 页码:7804-7810 , 文章类型: 研究论文,,卷期:2008年16-16]
- A series of triazolobenzothiadiazine-pyrrolobenzodiazepine conjugates linked through different alkane spacers have been prepd. These compds. have exhibited significant cytotoxicity against most of the cell lines examd. ...
- Design, synthesis and preliminary biological evaluation of acridine compounds as potential agents for a combined targeted chemo-radionuclide therapy approach to melanoma.
[作者:Desbois, Nicolas;Gardette, Maryline;Papon, Janine;Labarre, Pierre;Maisonial, Aurelie;Auzeloux, Philippe;Lartigue, Claire;Bouchon, Bernadette;Debiton, Eric;Blache, Yves;Chavignon, Olivier;Teulade, Jean-Claude;Maublant, Jean;Madelmont, Jean-Claude;Moins, Ni,期刊:Bioorganic & Medicinal Chemistry, 页码:7671-7690 , 文章类型: 研究论文,,卷期:2008年16-16]
- Various iodo-acridone and acridine carboxamides have been prepd. and evaluated as agents for targeted radionuclide and/or chemotherapy for melanoma, due to their structural similarity to benzamides which are known to pos...
- 9-N-Substituted berberine derivatives: Stabilization of G-quadruplex DNA and down-regulation of oncogene c-myc.
[作者:Ma, Yan;Ou, Tian-Miao;Hou, Jin-Qiang;Lu, Yu-Jing;Tan, Jia-Heng;Gu, Lian-Quan;Huang, Zhi-Shu;,期刊:Bioorganic & Medicinal Chemistry, 页码:7582-7591 , 文章类型: 研究论文,,卷期:2008年16-16]
- A series of 9-N-substituted berberine derivs. (2a-j) were synthesized and evaluated as a new class of G-quadruplex binding ligands. G-quadruplex of DNA had been proven to be the transcription controller of human c-myc ge...
- Nakijiquinones G-I, new sesquiterpenoid quinones from marine sponge.
[作者:Takahashi, Yohei;Kubota, Takaaki;Ito, Junji;Mikami, Yuzuru;Fromont, Jane;Kobayashi, Jun'ichi;,期刊:Bioorganic & Medicinal Chemistry, 页码:7561-7564 , 文章类型: 研究论文,,卷期:2008年16-16]
- Three new sesquiterpenoid quinones, nakijiquinones G-I (1-3), contg. a different amino group derived from amino acids have been isolated from Okinawan marine sponges of the family Spongiidae, and the structures and relat...
- Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines.
[作者:Ansari, Farzana Latif;Iftikhar, Fatima;Ihsan-ul-Haq;Mirza, Bushra;Baseer, Mohammad;Rashid, Umer;,期刊:Bioorganic & Medicinal Chemistry, 页码:7691-7697 , 文章类型: 研究论文,,卷期:2008年16-16]
- Solid-phase synthesis of a parallel library of 3'-hydroxy-2,3-dihydrobenzothiazepines has been carried out through [4+3] annulation of a,b-unsatd. ketones with aminothiophenol, using Wang resin as solid support. The syn...
- 2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: A study on the importance of modifications at the side chain on the activity.
[作者:Shen, Yanhong;Sheng, Rong;Zhang, Jing;He, Qiaojun;Yang, Bo;Hu, Yongzhou;,期刊:Bioorganic & Medicinal Chemistry, 页码:7646-7653 , 文章类型: 研究论文,,卷期:2008年16-16]
- As a part of our project aimed at developing new agents of potential application in AD, a new series of 2-phenoxy-indan-1-one derivs. which possess alkylamine side chain were designed, synthesized, and evaluated for thei...
- Synthesis and antiproliferative evaluation of amide-containing flavone and isoflavone derivatives.
[作者:Chen, I.-Li;Chen, Jhy-Yih;Shieh, Po-Chuen;Chen, Jih-Jung;Lee, Choa-Hsun;Juang, Shin-Hun;Wang, Tai-Chi;,期刊:Bioorganic & Medicinal Chemistry, 页码:7639-7645 , 文章类型: 研究论文,,卷期:2008年16-16]
- and evaluated for their antiproliferative activities. These compds. were synthesized via alkylation of hydroxyl precursors followed by the reaction with H2SO4 and NaN3 (Schmidt reaction). The preliminary assays indicat...
- In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.
[作者:Antunes, Joao E.;Freitas, Matheus P.;da Cunha, Elaine F. F.;Ramalho, Teodorico C.;Rittner, Roberto;,期刊:Bioorganic & Medicinal Chemistry, 页码:7599-7606 , 文章类型: 研究论文,,卷期:2008年16-16]
- A series of drug-like compds. derived from Sildenafil, Vardenafil and Tadalafil analogs were modeled through the MIA-QSAR (multivariate ligand-based approach. A highly predictive model was achieved and novel compds., wi...
- Synthesis and silencing properties of siRNAs possessing lipophilic groups at their 3'-termini.
[作者:Ueno, Yoshihito;Kawada, Koshi;Naito, Tomoharu;Shibata, Aya;Yoshikawa, Kayo;Kim, Hye-Sook;Wataya, Yusuke;Kitade, Yukio;,期刊:Bioorganic & Medicinal Chemistry, 页码:7698-7704 , 文章类型: 研究论文,,卷期:2008年16-16]
- Short-interfering RNAs (siRNAs) conjugated with lipophilic groups at their 3'-termini were synthesized. The properties of the synthesized siRNAs were examd. in detail, and it was found that at low concns., their silenci...
- Microwave-assisted solid phase synthesis, PEGylation, and biological activity studies of glucagon-like peptide-1(7-36) amide.
[作者:Chi, Yushi;Zhang, Huibin;Huang, Wenlong;Zhou, Jinpei;Zhou, Yinghong;Qian, Hai;Ni, Shuaijian;,期刊:Bioorganic & Medicinal Chemistry, 页码:7607-7614 , 文章类型: 研究论文,,卷期:2008年16-16]
- The insulinotropic hormone glucagon-like peptide-1 (GLP-1) is rapidly inactivated in the body. In order to improve its stability, we replaced the enzymic hydrolyzation position Ala8 with Gly and replaced Ala30 with Cys....
- Studies on the antifungal properties of N-thiolated b-lactams.
[作者:O'Driscoll, Marci;Greenhalgh, Kerriann;Young, Ashley;Turos, Edward;Dickey, Sonja;Lim, Daniel V.;,期刊:Bioorganic & Medicinal Chemistry, 页码:7832-7837 , 文章类型: 研究论文,,卷期:2008年16-16]
- N-Thiolated b-lactams had previously been shown to have antibacterial activity against a narrow selection of pathogenic bacteria including Staphylococcus aureus and Bacillus anthracis, as well as apoptotic-inducing activ...
- Synthesis and cellular effects of cycloterpenals: Cyclohexadienal-based activators of neurite outgrowth.
[作者:Bench, Bennie J.;Tichy, Shane E.;Perez, Lisa M.;Benson, Jenna;Watanabe, Coran M. H.;,期刊:Bioorganic & Medicinal Chemistry, 页码:7573-7581 , 文章类型: 研究论文,,卷期:2008年16-16]
- An unusual class of diterpenoid natural products, cycloterpenals' (with a central cyclohexadienal core), that arise in nature by condensation of retinoids and other isoprenes, have been isolated from a variety of organis...
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