- Synthesis and in vitro anti-tumor activity of new oxadiazole thioglycosides
[作者:Abu-Zaied, MA; El-Telbani, EM; Elgemeie, GH; Nawwar, GAM,期刊:European Journal of Medicinal Chemistry, 页码:229-235 , 文章类型: Article,,卷期:2011年46-1]
- A facile, convenient and high yielding synthesis of novel thioglycosides incorporating 1,3,4-oxadiazole, triazole and or triazine moieties from readily available starting materials has been described. The key step of thi...
- Synthesis and evaluation of tumor cell growth inhibition of methyl 3-amino-6-[(hetero)arylethynyl]thieno[3,2-b]pyridine-2-carboxylates. Structure-activity relationships, effects on the cell cycle and apoptosis
[作者:Queiroz, MJRP; Calhelha, RC; Vale-Silva, LA; Pinto, E; Almeida, GM; Vasconcelos, MH,期刊:European Journal of Medicinal Chemistry, 页码:236-240 , 文章类型: Article,,卷期:2011年46-1]
- The methyl 3-amino-6-bromothieno[3,2-b]pyridine-2-carboxylate, recently reported by some of us, was reacted in Sonogashira couplings with several (hetero)arylacetylenes. The growth inhibitory activity of the novel methyl...
- Synthesis and antimicrobial activity of thiosemicarbazides, s-triazoles and their Mannich bases bearing 3-chlorophenyl moiety
[作者:Plech, T; Wujec, M; Siwek, A; Kosikowska, U; Malm, A,期刊:European Journal of Medicinal Chemistry, 页码:241-248 , 文章类型: Article,,卷期:2011年46-1]
- A fast and efficient synthesis of some 1,4-disubstituted thiosemicarbazide derivatives is described. The reaction of 3-chlorobenzoic acid hydrazide with various aryl isothiocyanates gave thiosemicarbazide derivatives (1-...
- New (RS)-benzoxazepin-purines with antitumour activity: The chiral switch from (RS)-2,6-dichloro-9-[1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]-9H-purine
[作者:Lopez-Cara, LC; Conejo-Garcia, A; Marchal, JA; Macchione, G; Cruz-Lopez, O; Boulaiz, H; Garcia, MA; Rodriguez-Serrano, F; Ramirez, A; Cativiela, C; Jimenez, AI; Garcia-Ruiz, JM; Choquesillo-Lazarte, D; Aranega, A; Campos, JM,期刊:European Journal of Medicinal Chemistry, 页码:249-258 , 文章类型: Article,,卷期:2011年46-1]
- Completing an SAR study, a series of (RS)-6-substituted-7- or 9-(1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl)-7H or 9H-purines has been prepared under microwave-assisted conditions. Their antiproliferative activities on MC...
- Imidazo[2,1-b]thiazole carbohydrate derivatives: Synthesis and antiviral activity against Junin virus, agent of Argentine hemorrhagic fever
[作者:Barradas, JS; Errea, MI; D'Accorso, NB; Sepulveda, CS; Damonte, EB,期刊:European Journal of Medicinal Chemistry, 页码:259-264 , 文章类型: Article,,卷期:2011年46-1]
- Herein, we describe the syntheses of 3,5-disubstituted imidazo[2,1-b]thiazole. The cyclization step was performed in two different conditions by using either thermal or microwave heating. Comparing the results of both me...
- Synthesis and antiproliferative activity of novel symmetrical alkylthio- and alkylseleno-imidocarbamates
[作者:Ibanez, E; Plano, D; Font, M; Calvo, A; Prior, C; Palop, JA; Sanmartin, C,期刊:European Journal of Medicinal Chemistry, 页码:265-274 , 文章类型: Article,,卷期:2011年46-1]
- study described here concerns the synthesis of a series of thirty new symmetrically substituted imidothiocarbamate and imidoselenocarbamate derivatives and their evaluation for antitumoral activity in vitro against a pan...
- Synthesis and biophysical evaluation of arylhydrazono-1H-2-indolinones as beta-amyloid aggregation inhibitors
[作者:Campagna, F; Catto, M; Purgatorio, R; Altomare, CD; Carotti, A; De Stradis, A; Palazzo, G,期刊:European Journal of Medicinal Chemistry, 页码:275-284 , 文章类型: Article,,卷期:2011年46-1]
- A series of isatin-3-arylhydrazones were synthesized and evaluated in vitro as inhibitors of A beta(1-40) aggregation using a thioflavin T fluorescence method. An exploration of the effects on A beta(1-40) aggregation of...
- Synthesis and biological evaluation of new 4 beta-anilino-4 '-O-demethyl-4-desoxypodophyllotoxin derivatives as potential antitumor agents
[作者:Wang, L; Yang, FY; Yang, XC; Guan, XH; Hu, CQ; Liu, T; He, QJ; Yang, B; Hu, YZ,期刊:European Journal of Medicinal Chemistry, 页码:285-296 , 文章类型: Article,,卷期:2011年46-1]
- A series of new 4 beta-anilino-4'-O-demethyl-4-desoxypodophyllotoxin derivatives were prepared and evaluated for their cytotoxicities against four human cancer cell lines including KB, KB/VCR, A549 and 95D. Most compound...
- One-pot microwave assisted synthesis under green chemistry conditions, antioxidant screening, and cytotoxicity assessments of benzimidazole Schiff bases and pyrimido[1,2-a]benzimidazol-3(4H)-ones
[作者:Neochoritis, CG; Zarganes-Tzitzikas, T; Tsoleridis, CA; Stephanidou-Stephanatou, J; Kontogiorgis, CA; Hadjipavlou-Litina, DJ; Choli-Papadopoulou, T,期刊:European Journal of Medicinal Chemistry, 页码:297-306 , 文章类型: Article,,卷期:2011年46-1]
- The synthesis of a number of benzimidazole Schiff bases 3 and 3-oxo-pyrimido[2-a]benzimidazoles 4 in excellent yields by a one-step sequence from the reaction of 2-aminobenzimidazole under green chemistry conditions is d...
- Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents
[作者:Guo, RH; Zhang, QA; Ma, YB; Luo, J; Geng, CA; Wang, LJ; Zhang, XM; Zhou, J; Jiang, ZY; Chen, JJ,期刊:European Journal of Medicinal Chemistry, 页码:307-319 , 文章类型: Article,,卷期:2011年46-1]
- A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity...
- Synthesis and anti-mycobacterial activities of triazoloquinolones
[作者:Carta, A; Palomba, M; Briguglio, I; Corona, P; Piras, S; Jabes, D; Guglierame, P; Molicotti, P; Zanetti, S,期刊:European Journal of Medicinal Chemistry, 页码:320-326 , 文章类型: Article,,卷期:2011年46-1]
- A number of quinolone derivatives have been reported to possess anti-mycobacterial activity. Generally. Mycobacterium tuberculosis isolates expressing resistance to both isoniazid and rifampin are susceptible to fluoroqu...
- Part I: Synthesis, cancer chemopreventive activity and molecular docking study of novel quinoxaline derivatives
[作者:Galal, SA; Abdelsamie, AS; Tokuda, H; Suzuki, N; Lida, A; ElHefnawi, MM; Ramadan, RA; Atta, MHE; El Diwani, HI,期刊:European Journal of Medicinal Chemistry, 页码:327-340 , 文章类型: Article,,卷期:2011年46-1]
- The reaction of o-phenylene diamine and ethyl oxamate is reinvestigated and led to 3-aminoquinoxalin-2-(1H)-one rather than benzimidazole-2-carboxamide as was previously reported. The structure of the obtained quinoxalin...
- Synthesis and in vitro antimycobacterial activity of 8-OCH3 ciprofloxacin methylene and ethylene isatin derivatives
[作者:Feng, LS; Liu, ML; Zhang, S; Chai, Y; Wang, B; Zhang, YB; Lv, K; Guan, Y; Guo, HY; Xiao, CL,期刊:European Journal of Medicinal Chemistry, 页码:341-348 , 文章类型: Article,,卷期:2011年46-1]
- A series of novel 8-OCH3 ciprofloxacin methylene and ethylene isatin derivatives with remarkable improvement in lipophilicity were synthesized in this study. These derivatives were evaluated for their in vitro activity a...
- CYP1A2-mediated biotransformation of cardioactive 2-thienylidene-3,4-methylenedioxybenzoylhydrazine (LASSBio-294) by rat liver microsomes and human recombinant CYP enzymes
[作者:Fraga, AGM; da Silva, LL; Fraga, CAM; Barreiro, EJ,期刊:European Journal of Medicinal Chemistry, 页码:349-355 , 文章类型: Article,,卷期:2011年46-1]
- We describe herein the metabolic fate of cardioactive 1,3-benzodioxolyl N-acylhydrazone prototype LASSBio-294 (4) and the structural identification of its major phase I metabolite from rat liver microsomal assays. Our re...
- Synthesis and cytotoxicity of cis-dichloroplatinum (II) complexes of (1S,3S)-1,2,3,4-tetrahydroisoquinolines
[作者:Xu, G; Yan, Z; Wang, N; Liu, ZZ,期刊:European Journal of Medicinal Chemistry, 页码:356-363 , 文章类型: Article,,卷期:2011年46-1]
- A series of novel cisplatin-type platinum complexes with (1S,3S)-1,2,3,4-tetrahydroisoquinolines as the ligands were synthesized as potential anticancer agents in several steps starting from commercially available L-DOPA...
- Antifungal agents. Part 4: Synthesis and antifungal activities of novel indole[1,2-c]-1,2,4-benzotriazine derivatives against phytopathogenic fungi in vitro
[作者:Xu, H; Fan, LL,期刊:European Journal of Medicinal Chemistry, 页码:364-369 , 文章类型: Article,,卷期:2011年46-1]
- A series of novel indole[1,2-c]-1,2,4-benzotriazine derivatives were obtained by a modified Sandmeyer reaction in the presence of tert-butylnitrite (t-BuONO). As compared with hymexazol, a commercially available agricult...
|