- Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1 '-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-3,4-dihydrospiro[chromene-2,4 '-piperidine] analogs
[作者:Uto, Y; Ueno, Y; Kiyotsuka, Y; Miyazawa, Y; Kurata, H; Ogata, T; Yamada, M; Deguchi, T; Konishi, M; Takagi, T; Wakimoto, S; Ohsumi, J,期刊:European Journal of Medicinal Chemistry, 页码:4788-4796 , 文章类型: Article,,卷期:2010年45-11]
- In continuation of our investigation on novel stearoyl-CoA desaturase (SCD) 1 inhibitors, we have already reported on the structural modification of the benzoylpiperidines that led to a series of novel and highly potent ...
- Synthesis of carbohydrate-conjugate heterobimetallic Cu-II-Sn-2(IV) and Zn-II-Sn-2(IV) complexes; their interactions with CT DNA and nucleotides; DNA cleavage, in-vitro cytotoxicity
[作者:Tabassum, S; Khan, RA; Arjmand, F; Juvekar, AS; Zingde, SM,期刊:European Journal of Medicinal Chemistry, 页码:4797-4806 , 文章类型: Article,,卷期:2010年45-11]
- The new heterobimetallic Ni-II-Sn-2(IV) (1), Cu-II-Sn-2(IV) (2) and Zn-II-Sn-2(IV) (3) complexes, containing D-glucosamine, 1,8-diamino-3,6-diazaoctane and imidazole were isolated and characterized by spectral and analyt...
- Synthesis and anti-inflammatory activity evaluation of some novel 6-alkoxy (phenoxy)-[1,2,4]triazolo[3,4-a]phthalazine-3-amine derivatives
[作者:Sun, XY; Hu, CA; Deng, XQ; Wei, CX; Sun, ZG; Quan, ZS,期刊:European Journal of Medicinal Chemistry, 页码:4807-4812 , 文章类型: Article,,卷期:2010年45-11]
- Starting from phthalic anhydride, several new 6-alkoxy(phenoxy)-[1,2,4]triazolo[3,4-a]phthalazine-3-amine derivatives were synthesized as potent anti-inflammatory agent. The study showed that the compounds 6h (6-(2-chlor...
- Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans
[作者:Puri, N; Prakash, O; Manoharlal, R; Sharma, M; Ghosh, I; Prasad, R,期刊:European Journal of Medicinal Chemistry, 页码:4813-4826 , 文章类型: Article,,卷期:2010年45-11]
- In this study, we have explored the structure activity relationships of substrates of two major, promiscuous, multidrug transporters of an opportunistic human pathogen Candida albicans namely, CaCdr1p and CaMdr1p. To dif...
- Synthesis, structural elucidation and DNA-dependant protein kinase and antiplatelet studies of 2-amino-[5, 6, 7, 8-mono and 7, 8-di-substituted]-1, 3-benzoxazines
[作者:Ihmaid, S; Al-Rawi, J; Bradley, C,期刊:European Journal of Medicinal Chemistry, 页码:4934-4946 , 文章类型: Article,,卷期:2010年45-11]
- A number of new 2-amino-[5, 6, 7 and 8]-O-substituted 1,3-benzoxazines, and 2-amino 8-methyl-7-O-substituted-1,3-benzoxazines were synthesized. Thirty one new compounds were tested for their effect on collagen induced pl...
- Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives
[作者:Alafeefy, AM; Kadi, AA; Al-Deeb, OA; El-Tahir, KEH; Al-Jaber, NA,期刊:European Journal of Medicinal Chemistry, 页码:4947-4952 , 文章类型: Article,,卷期:2010年45-11]
- Two series of some new 2,4,6-trisubstituted-quinazoline derivatives were prepared and screened for their analgesic, anti-inflammatory activity and acute toxicity. Four compounds were more potent analgesic agents than the...
- Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors
[作者:Zhu, YY; Xia, SA; Zhu, MG; Yi, WY; Cheng, JG; Song, GH; Li, Z; Lu, P,期刊:European Journal of Medicinal Chemistry, 页码:4953-4962 , 文章类型: Article,,卷期:2010年45-11]
- A series of novel imidazopyrazinone derivatives were synthesized and evaluated with regard to their ability to inhibit dipeptidyl peptidase IV (DPP-IV) in vitro. Of these compounds (2R)-4-oxo-4-[2-(3-carbamoylbenzyl)-hex...
- Synthesis, characterization and cytotoxicity of mixed-ligand complexes of palladium(II) with aromatic diimine and 4-toluenesulfonyl-L-amino acid dianion
[作者:Zhang, JC; Li, LW; Wang, LW; Zhang, FF; Li, XL,期刊:European Journal of Medicinal Chemistry, 页码:5337-5344 , 文章类型: Article,,卷期:2010年45-11]
- Eight new palladium(II) complexes (1a-2d) with 4-toluenesulfonyl-L-amino acid dianion and diimine (bipy and phen) have been synthesized and characterized by elemental analysis, IR, UV, H-1 NMR, C-13 NMR and mass spectra ...
- Crystal structures, DNA-binding and cytotoxic activities studies of Cu(II) complexes with 2-oxo-quinoline-3-carbaldehyde Schiff-bases
[作者:Liu, ZC; Wang, BD; Li, B; Wang, Q; Yang, ZY; Li, TR; Li, Y,期刊:European Journal of Medicinal Chemistry, 页码:5353-5361 , 文章类型: Article,,卷期:2010年45-11]
- Three novel 2-oxo-quinoline-3-carbaldehyde Schiff-bases and their Cu(II) complexes were synthesized. The molecular structures of Cu(II) complexes were determined by X-ray crystal diffraction. The DNA-binding modes of the...
- Synthesis of the steroidal glycoside (25R)-3 beta,16 beta-diacetoxy-12,22-dioxo-5 alpha-cholestan-26-yl beta-D-glucopyranoside and its anti-cancer properties on cervicouterine HeLa, CaSki, and ViBo cells
[作者:Fernandez-Herrera, MA; Mohan, S; Lopez-Munoz, H; Hernandez-Vazquez, JMV; Perez-Cervantes, E; Escobar-Sanchez, ML; Sanchez-Sanchez, L; Regla, I; Pinto, BM; Sandoval-Ramirez, J,期刊:European Journal of Medicinal Chemistry, 页码:4827-4837 , 文章类型: Article,,卷期:2010年45-11]
- The synthesis of the new glycoside (25R)-3 beta,16 beta-diacetoxy-12,22-dioxo-5 alpha-cholestan-26-yl beta-D-glucopyranoside starting from hecogenin is described. This compound showed anti-cancer activity against cervico...
- Synthesis of bioactive polyheterocyclic ring systems as 5 alpha-reductase inhibitors
[作者:Hafez, NAA; Farghaly, TA; Al-Omar, MA; Abdalla, MM,期刊:European Journal of Medicinal Chemistry, 页码:4838-4844 , 文章类型: Article,,卷期:2010年45-11]
- Simple synthetic strategies for the hitherto unreported [1,2,4]triazolo[4,3-a]pyrido[4,3-d]pyrimidines 8 and [1,2,4]triazolo[4',3':1,2]pyrimido[4,5-b][1,6]naphthyridine-5-one 15 are described based on reaction of thione ...
- Design, synthesis and biological evaluation of 1,3,4-oxadiazole derivatives
[作者:Jha, KK; Samad, A; Kumar, Y; Shaharyar, M; Khosa, RL; Jain, J; Kumar, V; Singh, P,期刊:European Journal of Medicinal Chemistry, 页码:4963-4967 , 文章类型: Article,,卷期:2010年45-11]
- 3D QSAR analysis for the 21 molecules of 1,3,4-oxadiazoles was carried out by using k-Nearest Neighbor Molecular Field Analysis (kNN-MFA) combined with various selection procedures. 30 3D QSAR models were generated; one ...
- Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities - Development of highly efficacious cytotoxic agents
[作者:Singh, P; Kaur, M; Holzer, W,期刊:European Journal of Medicinal Chemistry, 页码:4968-4982 , 文章类型: Article,,卷期:2010年45-11]
- Based upon the lead compounds 10 and 11, a number of conjugates were synthesized by the combination of chromone-pyrimidine, chromone-indolinone, chromone-pyrazole, indole-pyrimidine, indole-indolinone and indole-pyrazole...
- Synthesis and antimicrobial activity of 2-substituted [4-(1,3,4-oxadiazol-2-yl methyl)] phthalazin-1(2H)-one derivatives
[作者:Sridhara, AM; Reddy, KRV; Keshavayya, J; Goud, PSK; Somashekar, BC; Bose, P; Peethambar, SK; Gaddam, SK,期刊:European Journal of Medicinal Chemistry, 页码:4983-4989 , 文章类型: Article,,卷期:2010年45-11]
- A series of new 2-substituted [4-(1,3,4-oxadiazol-2-yl)methyl]phthalazin-1(2H)-one derivatives 7a-h to 9a-h were designed and synthesized from methyl (4-oxo-3,4-dihydrophthalazin-1-yl)acetate (4), which in was turn prepa...
- Structural modifications on the phenazine N,N '-dioxide-scaffold looking for new selective hypoxic cytotoxins
[作者:Lavaggi, ML; Nieves, M; Cabrera, M; Olea-Azar, C; de Cerain, AL; Monge, A; Cerecetto, H; Gonzalez, M,期刊:European Journal of Medicinal Chemistry, 页码:5362-5369 , 文章类型: Article,,卷期:2010年45-11]
- We have identified phenazine 5,10-dioxides as prodrugs for antitumour therapy that undergo hypoxic-selective bioreduction to form cytotoxic species. Here, we investigated some structural modifications in order to find ne...
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