- Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives
[作者:Lee, CC; Huang, KF; Lin, PY; Huang, FC; Chen, CL; Chen, TC; Guh, JH; Lin, JJ; Huang, HS,期刊:European Journal of Medicinal Chemistry, 页码:323-336 , 文章类型: Article,,卷期:2012年47-1]
- A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, telomerase inhibitory activity by TRAP assay, and ...
- 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site
[作者:Ghizzoni, M; Wu, J; Gao, TL; Haisma, HJ; Dekker, FJ; Zheng, YG,期刊:European Journal of Medicinal Chemistry, 页码:337-344 , 文章类型: Article,,卷期:2012年47-1]
- Histone acetyltransferases are important enzymes that regulate various cellular functions, such as epigenetic control of DNA transcription. Development of HAT inhibitors with high selectivity and potency will provide pow...
- CK2 alpha and CK2 alpha ' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives
[作者:Janeczko, M; Orzeszko, A; Kazimierczuk, Z; Szyszka, R; Baier, A,期刊:European Journal of Medicinal Chemistry, 页码:345-350 , 文章类型: Article,,卷期:2012年47-1]
- The goal of this study was to test the inhibitory activity of a series of tetrahalogenobenzimidazoles, including a number of novel derivatives, on individual catalytic subunits of human CK2. 4,5,6,7-tetrabromo- and 4,5,6...
- Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors
[作者:Reddy, NP; Reddy, TC; Aparoy, P; Achari, C; Sridhar, PR; Reddannaa, P,期刊:European Journal of Medicinal Chemistry, 页码:351-359 , 文章类型: Article,,卷期:2012年47-1]
- A group of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives were designed using Site point connection method, synthesized and evaluated for their 5-Lipoxygenase (5-LOX) inhibitory activity. Hydrophobic site points in 5-LO...
- Design and synthesis of novel stiripentol analogues as potential anticonvulsants
[作者:Aboul-Enein, MN; El-Azzouny, AA; Attia, MI; Maklad, YA; Amin, KM; Abdel-Rehim, M; El-Behairy, MF,期刊:European Journal of Medicinal Chemistry, 页码:360-369 , 文章类型: Article,,卷期:2012年47-1]
- A series of stiripentol (SIP) analogues namely, 2-1(1E)-1-(1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ylidene]-N-(aryl/H)hydrazinecarboxamides 7a-h, (+/-)-(5RS)-N-(aryl/H)-(1,3-benzodioxol-5-yl)-3-tert-butyl-4,5-dihyd...
- Synthesis of novel benzofurocoumarin analogues and their anti-proliferative effect on human cancer cell lines
[作者:Francisco, CS; Rodrigues, LR; Cerqueira, NMFSA; Oliveira-Campos, AMF; Rodrigues, LM,期刊:European Journal of Medicinal Chemistry, 页码:370-376 , 文章类型: Article,,卷期:2012年47-1]
- The synthesis of five new tetracyclic benzofurocoumarin (benzopsoralen) analogues is described. Their inhibitory effects on the growth of three human tumor cell lines (MDA MB 231 (breast adenocarcinoma), HeLa (cervix ade...
- Synthesis, molecular docking study and antitumor activity of novel 2-phenylindole derivatives
[作者:El-Nakkady, SS; Hanna, MM; Roaiah, HM; Ghannam, IAY,期刊:European Journal of Medicinal Chemistry, 页码:387-398 , 文章类型: Article,,卷期:2012年47-1]
- The starting material, 4-(1-indol-2-yl)phenol 1 was obtained via Fischer synthesis. Vilsmeir Haack's formylation of 1 gave the carboxaldehyde derivative 2 which was subjected to different reactions affording the 3-substi...
- Novel palladium(II) and platinum(II) complexes with 1H-benzimidazol-2-ylmethyl-N-(4-bromo-phenyl)-amine: Structural studies and anticancer activity
[作者:Ghani, NTA; Mansour, AM,期刊:European Journal of Medicinal Chemistry, 页码:399-411 , 文章类型: Article,,卷期:2012年47-1]
- [MLCl(2)] (L = (1H-benzimidazol-2-ylmethyl)-N-(4-bromo-phenyl)-amine; M = Pd & Pt) and [PdL(OH(2))(2)]center dot 2X center dot zH(2)O (X = Br, I, z = 2; X = SCN, z = 1; X = NO(3), z = 0) complexes have been synthesized a...
- Design, synthesis and biological evaluation of novel glycosylated diphyllin derivatives as topoisomerase II inhibitors
[作者:Shi, DK; Zhang, W; Ding, N; Li, M; Li, YX,期刊:European Journal of Medicinal Chemistry, 页码:424-431 , 文章类型: Article,,卷期:2012年47-1]
- Recently, a novel glycosylated diphyllin derivative 11 which exhibiting potent anticancer activity by targeting topoisomerase II alpha was reported by our group. In order to provide more molecules for structure-activity ...
- From COX-2 inhibitor nimesulide to potent anti-cancer agent: Synthesis, in vitro, in vivo and pharmacokinetic evaluation
[作者:Zhong, B; Cai, XH; Chennamaneni, S; Yi, X; Liu, LL; Pink, JJ; Dowlati, A; Xu, Y; Zhou, AM; Su, B,期刊:European Journal of Medicinal Chemistry, 页码:432-444 , 文章类型: Article,,卷期:2012年47-1]
- Cyclooxygenase-2 (COX-2) inhibitor nimesulide inhibits the proliferation of various types of cancer cells mainly via COX-2 independent mechanisms, which makes it a good lead compound for anti-cancer drug development. In ...
- Novel 1,3,4-heterodiazole analogues: Synthesis and in-vitro antitumor activity
[作者:Taher, AT; Georgey, HH; EI-Subbagh, HI,期刊:European Journal of Medicinal Chemistry, 页码:445-451 , 文章类型: Article,,卷期:2012年47-1]
- The synthesis of some new heterodiazole and their annulated imidazo[2,1-b]1,3,4-oxa/thiadiazolone 6a-d, 7a-d; 1,3,4-oxa or thiadiazole[3,2-a]pyrimidine diamine 8a-d and 1,3,4-oxa or thiadiazole-3-piperidino-1-propamide 1...
- Electrochemical and spectroscopic investigations of isoniazide and its analogs with ds.DNA at physiological pH: Evaluation of biological activities
[作者:Arshad, N; Yunus, U; Razzque, S; Khan, M; Saleem, S; Mirza, B; Rashid, N,期刊:European Journal of Medicinal Chemistry, 页码:452-461 , 文章类型: Article,,卷期:2012年47-1]
- Interaction and binding of isonicotinic acid hydrazide (INH) and its two analogs; pyrazine carboxylic acid hydrazide (PCH) and 2,4-dihydroxy benzoic acid hydrazide (2,4-DHBAH) with DNA has been investigated by UV-spectro...
- Physicochemical profile of macrolides and their comparison with small molecules
[作者:Stepanic, V; Ziher, D; Gabelica-Markovic, V; Jelic, D; Nunhuck, S; Valko, K; Kostrun, S,期刊:European Journal of Medicinal Chemistry, 页码:462-472 , 文章类型: Article,,卷期:2012年47-1]
- Macrolides are stereospecific macrolactones of high molecular weights. Herein, 600 mostly semisynthetic macrolides are compared with 50,000 small non-macrolide synthetic molecules in terms of measured physicochemical pro...
- Synthesis, molecular modeling and biological evaluation of 2-(benzylthio)-5-aryloxadiazole derivatives as anti-tumor agents
[作者:Liu, K; Lu, X; Zhang, HJ; Sun, J; Zhu, HL,期刊:European Journal of Medicinal Chemistry, 页码:473-478 , 文章类型: Article,,卷期:2012年47-1]
- A series of 2-(benzylthio)-5-aryloxadiazole derivatives have been designed and synthesized, and their biological activities are also evaluated for EGFR inhibitory activity. Fourteen compounds among the twenty compounds a...
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