- Design, synthesis, in vitro antimicrobial and anticancer activity of novel methylenebis-isoxazolo[4,5-b]azepines derivatives
[作者:Rajanarendar, E; Reddy, MN; Krishna, SR; Reddy, KG; Reddy, YN; Rajam, MV,期刊:European Journal of Medicinal Chemistry, 页码:344-349 , 文章类型: Article,,卷期:2012年50-1]
- A series of novel methylene bis-isoxazolo[4,5-b]azepines have been synthesized by reaction of 3,5-dimethyl-4-nitroisoxazole 6 with an appropriate methylene bis-chalcones 7 to obtain various Michael adducts 8a-i, which on...
- (99m)Tc(I)/Re(I) tricarbonyl complexes for in vivo targeting of melanotic melanoma: Synthesis and biological evaluation
[作者:Moura, C; Gano, L; Mendes, F; Raposinho, PD; Abrantes, AM; Botelho, MF; Santos, I; Paulo, A,期刊:European Journal of Medicinal Chemistry, 页码:350-360 , 文章类型: Article,,卷期:2012年50-1]
- The (99m)Tc (I) tricarbonyl complexes fac-[(99m)Tc(kappa(3)-L)(CO)(3)] (Tc1-Tc6) containing N-ethylpyrrolidine and N,N-diethylethylamine groups for melanin binding, were evaluated in vitro and in vivo as radioactive prob...
- Hydroxyl may not be indispensable for raltegravir: Design, synthesis and SAR Studies of raltegravir derivatives as HIV-1 inhibitors
[作者:Wang, ZW; Wang, MX; Yao, X; Li, Y; Qiao, WT; Geng, YQ; Liu, YX; Wang, QM,期刊:European Journal of Medicinal Chemistry, 页码:361-369 , 文章类型: Article,,卷期:2012年50-1]
- A series of raltegravir derivatives 20-42 were prepared and systematically evaluated for their anti-HIV activity. The bioassay results showed that most of the compounds possess good to excellent anti-HIV activity. Especi...
- Design, synthesis and molecular docking studies of some novel spiro[indoline-3, 4 '-piperidine]-2-ones as potential c-Met inhibitors
[作者:Ye, LB; Tian, YX; Li, ZH; Jin, H; Zhu, ZG; Wan, SH; Zhang, JY; Yu, PJ; Zhang, JJ; Wu, SG,期刊:European Journal of Medicinal Chemistry, 页码:370-375 , 文章类型: Article,,卷期:2012年50-1]
- Deregulation of receptor tyrosine kinase c-Met has been reported in human cancers and is considered as an attractive target for small molecule drug discovery. In this study, a series of spiro[indoline-3, 4'-piperidine]-2...
- The selective cytotoxic activity in breast cancer cells by an anthranilic alcohol-derived acyclic 5-fluorouracil O,N-acetal is mediated by endoplasmic reticulum stress-induced apoptosis
[作者:Caba, O; Rodriguez-Serrano, F; Diaz-Gavilan, M; Conejo-Garcia, A; Ortiz, R; Martinez-Amat, A; Alvarez, P; Gallo, MA; Campos, JM; Marchal, JA; Aranega, A,期刊:European Journal of Medicinal Chemistry, 页码:376-382 , 文章类型: Article,,卷期:2012年50-1]
- Advance in the knowledge of molecular biology has thrown light on many aspects of apoptosis regulation mechanisms. This has allowed a change in anti-cancer therapy trends, from classic cytotoxic strategies to the develop...
- Novel molecular combination deriving from natural aminoacids and polyphenols: Design, synthesis and free-radical scavenging activities
[作者:Silvia, V; Baldisserotto, A; Scalambra, E; Malisardi, G; Durini, E; Manfredini, S,期刊:European Journal of Medicinal Chemistry, 页码:383-392 , 文章类型: Article,,卷期:2012年50-1]
- Following the recent output of scientific publications in the matter of synergic activity between different antioxidants, we have undertaken the present study with the aim to synthesize new molecules with radical-scaveng...
- Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNF alpha-induced nuclear factor-kappa B activation inhibition
[作者:Zuo, YL; Yu, Y; Wang, SN; Shao, WY; Zhou, BH; Lin, L; Luo, ZY; Huang, RG; Du, J; Bu, XZ,期刊:European Journal of Medicinal Chemistry, 页码:393-404 , 文章类型: Article,,卷期:2012年50-1]
- A series of biaryl-based chalcones were designed as a combination of the natural chalcone and biphenyl moieties, and synthesized by two step chemistry involving Knoevenagel reaction and microwave assistant Suzuki couplin...
- Evaluation of DNA binding, antioxidant and cytotoxic activity of mononuclear Co(III) complexes of 2-oxo-1,2-dihydrobenzo[h]quinoline-3-carbaldehyde thiosemicarbazones
[作者:Ramachandran, E; Thomas, SP; Poornima, P; Kalaivani, P; Prabhakaran, R; Padma, VV; Natarajan, K,期刊:European Journal of Medicinal Chemistry, 页码:405-415 , 文章类型: Article,,卷期:2012年50-1]
- Four new 2-oxo-1,2-dihydrobenzo[h]quinoline-3-carbaldehyde N-substituted thiosemicarbazone ligands (H(2)-LR, where R = H, Me, Et or Ph) and their corresponding new cobalt(III) complexes have been synthesized and characte...
- Computer-assisted rational design, synthesis, and bioassay of non-steroidal anti-inflammatory agents
[作者:Girgis, AS; Tala, SR; Oliferenko, PV; Oliferenko, AA; Katritzky, AR,期刊:European Journal of Medicinal Chemistry, 页码:1-8 , 文章类型: Article,,卷期:2012年50-1]
- A focused dataset of previously synthesized and tested [1,2,4]-triazolo[1,5-a]pyridines and pyridine-3-carboxylates was studied by Molecular Field Topology Analysis (MFTA) to identify steric and electronic determinants o...
- Synthesis of terphenyl benzimidazoles as tubulin polymerization inhibitors
[作者:Kamal, A; Reddy, MK; Shaik, TB; Rajender; Srikanth, YVV; Reddy, VS; Kumar, GB; Kalivendi, SV,期刊:European Journal of Medicinal Chemistry, 页码:9-17 , 文章类型: Article,,卷期:2012年50-1]
- A series of new terphenyl benzimidazoles (3a-z and 3aa-ad) were synthesized and evaluated for their anticancer activity. All the 30 compounds have shown moderate to good anticancer potency, however some of the compounds ...
- Assessment of antiplatelet activity of 2-aminopyrimidines
[作者:Giridhar, R; Tamboli, RS; Ramajayam, R; Prajapati, DG; Yadav, MR,期刊:European Journal of Medicinal Chemistry, 页码:428-432 , 文章类型: Article,,卷期:2012年50-1]
- A series of 4,6-diaryl-2-aminopyrimidines was developed as antiplatelet agents and their potency was evaluated by in vitro assay. Compound 14k was found to be two times more potent than aspirin. These encouraging results...
- Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold
[作者:Kratky, M; Vinsova, J; Volkova, M; Buchta, V; Trejtnar, F; Stolarikova, J,期刊:European Journal of Medicinal Chemistry, 页码:433-440 , 文章类型: Article,,卷期:2012年50-1]
- A series of novel sulfonamides containing 5-chloro-2-hydroxybenzaldehyde or 5-chloro-2-hydroxybenzoic acid scaffolds were designed, synthesized and characterized by IR, (1)H NMR and (13)C NMR. All ten target synthesized ...
- Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives
[作者:Piccionello, AP; Musumeci, R; Cocuzza, C; Fortuna, CG; Guarcello, A; Pierro, P; Pace, A,期刊:European Journal of Medicinal Chemistry, 页码:441-448 , 文章类型: Article,,卷期:2012年50-1]
- In the present study the synthesis of new Linezolid-like molecules has been achieved by substitution of the oxazolidinone central heterocyclic moiety with a 1,2,4-oxadiazole ring. Two series of 1,2,4-oxadiazoles, bearing...
- Synthesis and biological evaluation of some 6-substituted purines (vol 42, pg 530, 2007)
[作者:Braga, FG; Coimbra, ES; Matos, MD; Carmo, AML; Cancio, MD; da Silva, AD,期刊:European Journal of Medicinal Chemistry, 页码:449-449 , 文章类型: Correction,,卷期:2012年50-1]
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- Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents
[作者:Pan, L; Jiang, Y; Liu, Z; Liu, XH; Liu, Z; Wang, G; Li, ZM; Wang, D,期刊:European Journal of Medicinal Chemistry, 页码:18-26 , 文章类型: Article,,卷期:2012年50-1]
- A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by (1)H NMR, (13)C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The r...
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