- Histone deacetylase inhibitor prodrugs in nanoparticle vector enhanced gene expression in human cancer cells
[作者:Ishii, Y; Hattori, Y; Yamada, T; Uesato, S; Maitani, Y; Nagaoka, Y,期刊:European Journal of Medicinal Chemistry, 页码:4603-4610 , 文章类型: Article,,卷期:2009年44-11]
- We developed histone deacetylase inhibitor (HDACI) prodrugs to enhance the expression of the external genes transfected into human cells with cationic nanoparticles (NPs). We synthesized five kinds of lipid-linked HDACI ...
- Antitumor and antimycobacterial activities of cyclopalladated complexes: X-ray structure of [Pd(C-2,N-dmba)(Br)(tu)] (dmba = N,N-dimethylbenzylamine, tu = thiourea)
[作者:Moro, AC; Mauro, AE; Netto, AVG; Ananias, SR; Quilles, MB; Carlos, IZ; Pavan, FR; Leite, CQF; Horner, M,期刊:European Journal of Medicinal Chemistry, 页码:4611-4615 , 文章类型: Article,,卷期:2009年44-11]
- The reactions between [Pd(C-2,N-dmba)(mu-X)](2) (dmba = N,N-dimethylbenzylamine: X = Cl, Br) and thiourea (tu) in the 1:2 molar ratio at room temperature resulted in the mononuclear compounds [Pd(C-2,N-dmba)(Cl)(tu)] (1)...
- Structure-activity relationship of dopaminergic halogenated 1-benzyl-tetrahydroisoquinoline derivatives
[作者:El Aouad, N; Berenguer, I; Romero, V; Marin, P; Serrano, A; Andujar, S; Suvire, F; Bermejo, A; Ivorra, MD; Enriz, RD; Cabedo, N; Cortes, D,期刊:European Journal of Medicinal Chemistry, 页码:4616-4621 , 文章类型: Article,,卷期:2009年44-11]
- Two series of halogenated 1-benzyl-7-chloro-6-hydroxy-tetrahydroisoquinolines were prepared to explore the influence of each series on the affinity for dopamine receptors. All the compounds displayed a high affinity for ...
- Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs
[作者:Bhandari, SV; Dangre, SC; Bothara, KG; Patil, AA; Sarkate, AP; Lokwani, DK; Gore, ST; Deshmane, BJ; Raparti, VT; Khachane, CV,期刊:European Journal of Medicinal Chemistry, 页码:4622-4636 , 文章类型: Article,,卷期:2009年44-11]
- Various substituted 1,5-diarylpyrazol-3-one derivatives were synthesized and screened for analgesic, anti-inflammatory activities, ulcerogenic potential and for their ability to release nitric oxide. Most compounds exhib...
- Design and one-pot synthesis of alpha-aminophosphonates and bis (alpha-aminophosphonates) by iron(III) chloride and cytotoxic activity
[作者:Rezaei, Z; Firouzabadi, H; Iranpoor, N; Ghaderi, A; Jafari, MR; Jafari, AA; Zare, HR,期刊:European Journal of Medicinal Chemistry, 页码:4266-4275 , 文章类型: Article,,卷期:2009年44-11]
- In this study, we used a solution of FeCl3 in THF to facilitate the Mannich-type reaction of aldehyde, amine and phosphite compounds to form corresponding alpha-aminophosphonates in a one-pot, three-component reaction. S...
- Docking-based 3D-QSAR study of HIV-1 integrase inhibitors
[作者:Gupta, P; Roy, N; Garg, P,期刊:European Journal of Medicinal Chemistry, 页码:4276-4287 , 文章类型: Article,,卷期:2009年44-11]
- In this study, 3-aroyl-1,1-dioxo-1,4,2-benzodithiazine and 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives (HIV-1 integrase inhibitors) were used for CoMFA and CoMSIA to determine the substructu...
- Synthesis and antimicrobial activities of novel quinoline derivatives carrying 1,2,4-triazole moiety
[作者:Eswaran, S; Adhikari, AV; Shetty, NS,期刊:European Journal of Medicinal Chemistry, 页码:4637-4647 , 文章类型: Article,,卷期:2009年44-11]
- A new class of quirroline derivatives containing 1,2,4-triazole moiety were synthesized from derivatives of 4-hydroxy-8-(trifluoromethyl)quinoline-3-carbohydrazide 4 through multi-step reactions. The compound 4, on treat...
- Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
[作者:Zhan, P; Liu, XY; Fang, ZJ; Li, ZY; Pannecouque, C; De Clercq, E,期刊:European Journal of Medicinal Chemistry, 页码:4648-4653 , 文章类型: Article,,卷期:2009年44-11]
- A series of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)acetamide (TTA) derivatives were synthesized and evaluated as potent inhibitors of HIV-1. Among the newly disclosed TTAs, compounds 7f, 7g and 7c were the most...
- Anti-oxidant, anti-fungal and anti-leishmanial activities of novel 3-[4-(1H-imidazol-1-yl) phenyl]prop-2-en-1-ones
[作者:Hussain, T; Siddiqui, HL; Zia-ur-Rehman, M; Yasinzai, MM; Parvez, M,期刊:European Journal of Medicinal Chemistry, 页码:4654-4660 , 文章类型: Article,,卷期:2009年44-11]
- A series of new 3-[4-(1H-imidazol-1-yl) phenyl]prop-2-en-1-ones were synthesized by the condensation of various acetophenones with 4-(1H-imidazol-1-yl) benzaldehyde which was itself prepared by the N-arylation of imidazo...
- Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives
[作者:Zagorska, A; Jurczyk, S; Pawlowski, M; Dybala, M; Nowak, G; Tatarczynska, E; Nikiforuk, A; Chojnacka-Wojcik, E,期刊:European Journal of Medicinal Chemistry, 页码:4288-4296 , 文章类型: Article,,卷期:2009年44-11]
- A series of N-8-arylpiperazinylpropyl derivatives of 1,3-dimethyl-(1H,8H)-imidazo[2,1-f]purine-2,4-dione (2-10) and amide derivatives of 1,3-dimethyl-6,7-dihydroimidazo[2,1-f]purine-2,4-(1H,3H)-dione-7-carboxylic acid (1...
- Pentacyclo-undecane derived cyclic tetra-amines: Synthesis and evaluation as potent anti-tuberculosis agents
[作者:Onajole, OK; Govender, K; Govender, P; van Helden, PD; Kruger, HG; Maguire, GEM; Muthusamy, K; Pillay, M; Wiid, I; Govender, T,期刊:European Journal of Medicinal Chemistry, 页码:4297-4305 , 文章类型: Article,,卷期:2009年44-11]
- As part of an ongoing effort to develop highly potent anti-tuberculosis agents, fourteen pentacycloundecane (PCU) tetra-amine compounds were synthesized and screened for their in vitro anti-mycobacterial activity against...
- Synthesis, photochemical E (trans) -> Z (cis) isomerization and antimicrobial activity of 2-chloro-5-methylpyridine-3-olefin derivatives
[作者:Gangadasu, B; Reddy, MJR; Ravinder, M; Kumar, SB; Raju, BC; Kumar, KP; Murthy, USN; Rao, VJ,期刊:European Journal of Medicinal Chemistry, 页码:4661-4667 , 文章类型: Article,,卷期:2009年44-11]
- 2-Chloro-5-methylpyridine-3-olefin derivatives (3a-e) have been synthesized from 2-chloro-5-methyl nicotinaldehyde (1) and studied their photochemical E (trans) -> Z (cis) isomerization upon direct irradiation and triple...
- Stimulatory effect of apigenin-6-C-beta-L-fucopyranoside on insulin secretion and glycogen synthesis
[作者:Cazarolli, LH; Folador, P; Moresco, HH; Brighente, IMC; Pizzolatti, MG; Silva, FRMB,期刊:European Journal of Medicinal Chemistry, 页码:4668-4673 , 文章类型: Article,,卷期:2009年44-11]
- In vivo and in vitro treatments were carried out to investigate the effects of apigenin-6-C-beta-L-fucopyranoside (1), isolated from Averrhoa carambola L. (Oxalidaceae), on serum glucose and insulin levels in hyperglycem...
- Novel naphthalimide derivatives as potential apoptosis-inducing agents: Design, synthesis and biological evaluation
[作者:Wu, AB; Xu, YF; Qian, XH; Wang, J; Liu, JW,期刊:European Journal of Medicinal Chemistry, 页码:4674-4680 , 文章类型: Article,,卷期:2009年44-11]
- A series of novel naphthalimide derivatives with flexible alkyl/aryl moieties were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell li...
- Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety
[作者:Jasper, A; Schepmann, D; Lehmkuhl, K; Vela, JM; Buschmann, H; Holenz, J; Wunsch, B,期刊:European Journal of Medicinal Chemistry, 页码:4306-4314 , 文章类型: Article,,卷期:2009年44-11]
- The symmetrically connected spiro[[2]benzopyran-1,4'-piperidines] 1 are highly potent and selective sigma(1) receptor ligands. Changing the position of the spirocyclic nitrogen atom led to the unsymmetrically connected s...
- Synthesis, characterization and derivatization of some novel types of mono- and bis-imidazolidineiminothiones and imidazolidineiminodithiones with antitumor, antiviral, antibacterial and antifungal activities - part I
[作者:El-Sharief, AMS; Moussa, Z,期刊:European Journal of Medicinal Chemistry, 页码:4315-4334 , 文章类型: Article,,卷期:2009年44-11]
- Halogenated and alkylated N-arylcyanothioformanilides were reacted with the nucleophilic reagents triethylamine, hydrazine and diphenyldiazomethane to produce N-arylcyanothioformanilide ammonium salts, a thiosemicarbazid...
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