- Synthesis and structure-activity relationship of 3-O-acylated (-)-epigallocatechins as 5 alpha-reductase inhibitors
[作者:Lin, SF; Lin, YH; Lin, MJ; Kao, YF; Wang, RW; Teng, LW; Chuang, SH; Chang, JM; Yuan, TT; Fu, KC; Huang, KP; Lee, YS; Chiang, CC; Yang, SC; Lai, CL; Liao, CB; Chen, PN; Lin, YS; Lai, KT; Huang, HJ; Yang, JY; Liu, CW; Wei, WY; Chen, CK; Hiipakka, RA; Liao, SS; Huang, JJ,期刊:European Journal of Medicinal Chemistry, 页码:6068-6076 , 文章类型: Article,,卷期:2010年45-12]
- A series of 3-O-acylated (-)-epigallocatechins were synthesized and their inhibition of steroid 5 alpha-reductase was studied. They were prepared from the reaction of EGCG with tert-butyldimethylsilyl chloride followed b...
- Effect of the chloro-substitution on lowering diabetic hyperglycemia of vanadium complexes with their permeability and cytotoxicity
[作者:Xie, MJ; Niu, YF; Yang, XD; Liu, WP; Li, L; Gao, LH; Yan, SP; Meng, ZH,期刊:European Journal of Medicinal Chemistry, 页码:6077-6084 , 文章类型: Article,,卷期:2010年45-12]
- The effect of the chloro-substitution of dinuclear vanadium (V) complexes on lowering diabetic hyperglycemia was evaluated. The in vivo tests for hypoglycemic activity show that complex 2 at the dose of 10.0 and 20.0 mg ...
- Synthesis of novel chiral Delta(2)-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes
[作者:Dallanoce, C; Magrone, P; Matera, C; Lo Presti, L; De Amici, M; Riganti, L; Clementi, F; Gotti, C; De Micheli, C,期刊:European Journal of Medicinal Chemistry, 页码:5594-5601 , 文章类型: Article,,卷期:2010年45-12]
- The enantiopure diastereomeric Delta(2)-isoxazoline derivatives (2S,5'R)-5a-10a and (2S,5'S)-5b, (2S,5'S)-9b, (2S,5'S)-11b, which are structural analogues of both ABT-418 2 and oxyimino ethers (S)-3 and (Z)-(S)-4, were s...
- Molecular docking and QSAR study on steroidal compounds as aromatase inhibitors
[作者:Dai, YJ; Wang, QA; Zhang, XL; Jia, SR; Zheng, H; Feng, DC; Yu, P,期刊:European Journal of Medicinal Chemistry, 页码:5612-5620 , 文章类型: Article,,卷期:2010年45-12]
- In order to develop more potent, selective and less toxic steroidal aromatase (AR) inhibitors, molecular docking, 2D and 3D hybrid quantitative structure activity relationship (QSAR) study have been conducted using topol...
- Synthesis and biological evaluation of aminoketones
[作者:Rai, US; Isloor, AM; Shetty, P; Isloor, N; Malladi, S; Fun, HK,期刊:European Journal of Medicinal Chemistry, 页码:6090-6094 , 文章类型: Article,,卷期:2010年45-12]
- A three-component Mannich reaction of different ketones with aromatic aldehydes and different amines in microwave irradiation under solvent free condition afforded corresponding beta-amino carbonyl compounds in excellent...
- Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives
[作者:Goncalves, RSB; Kaiser, CR; Lourenco, MCS; de Souza, MVN; Wardell, JL; Wardell, SMSV; da Silva, AD,期刊:European Journal of Medicinal Chemistry, 页码:6095-6100 , 文章类型: Article,,卷期:2010年45-12]
- In this work, we report the synthesis and the antitubercular evaluation of 16 new mefloquine derivatives, formed from reactions between mefloquine and benzaldehydes, with the activity expressed as the minimum inhibitory ...
- Synthesis and in vitro antimicrobial evaluation of novel fluoroquinolone derivatives
[作者:Srinivasan, S; Shafreen, RMB; Nithyanand, P; Manisankar, P; Pandian, SK,期刊:European Journal of Medicinal Chemistry, 页码:6101-6105 , 文章类型: Article,,卷期:2010年45-12]
- A series of 1-ethyl-6,8-difluoro-4-oxo-7(4-aryl piperazin-1-yl) 1,4-dihydro-quinoline-3-carboxylic acid derivatives (6a-f) and 1-ethyl-6,8-difluoro-4-oxo-7(4-piperidin-1-yl) 1,4-dihydro-quinoline-3-carboxylic acid deriva...
- TETA analogue containing one methylenephosphonate pendant arm: Lanthanide complexes and biological evaluation of its Sm-153 and Ho-166 complexes
[作者:Lima, LMP; Delgado, R; Marques, F; Gano, L; Santos, I,期刊:European Journal of Medicinal Chemistry, 页码:5621-5627 , 文章类型: Article,,卷期:2010年45-12]
- The thermodynamic stability constants of complexes of 1,4,8,11-tetraazacyclotetradecane-1,4,8-triacetic-11-methylphosphonic acid (H(5)te3a1p) with La3+, Sm3+, Gd3+, Ho3+ and Lu3+ metal ions were determined by potentiomet...
- Efficient synthesis of 6-(hetero)arylthieno[3,2-b]pyridines by Suzuki-Miyaura coupling. Evaluation of growth inhibition on human tumor cell lines, SARs and effects on the cell cycle
[作者:Queiroz, MJRP; Calhelha, RC; Vale-Silva, LA; Pinto, E; Lima, RT; Vasconcelos, MH,期刊:European Journal of Medicinal Chemistry, 页码:5628-5634 , 文章类型: Article,,卷期:2010年45-12]
- A wide variety of new bi(hetero)aryl derivatives of the thieno[3,2-b]pyridine skeleton was obtained in high to excellent yields (65-91%) by Suzuki-Miyaura cross-coupling of the methyl 3-amino-6-bromothieno[3,2-b]pyridine...
- Convenient synthesis and biological profile of 5-amino-substituted 1,2,4-oxadiazole derivatives
[作者:Ispikoudi, M; Amvrazis, M; Kontogiorgis, C; Koumbis, AE; Litinas, KE; Hadjipavlou-Litina, D; Fylaktakidou, KC,期刊:European Journal of Medicinal Chemistry, 页码:5635-5645 , 文章类型: Article,,卷期:2010年45-12]
- We describe herein a convenient straightforward synthesis of 5-amino-substituted 1,2,4-oxadiazoles, upon the reactions of amidoximes with carbodiimides, as well as their further derivatization to acetamides, in good yiel...
- New amino acid esters of salicylanilides active against MDR-TB and other microbes
[作者:Kratky, M; Vinsova, J; Buchta, V; Horvati, K; Bosze, S; Stolarikova, J,期刊:European Journal of Medicinal Chemistry, 页码:6106-6113 , 文章类型: Article,,卷期:2010年45-12]
- Eleven halogenated (S)-2-(phenylcarbamoyl)phenyl 2-acetamido-3-phenylpropanoates (3a-3k) were designed and synthesized as potential antimicrobial agents. They were evaluated in vitro against some mycobacterial, bacterial...
- Synthesis and cytostatic activity of purine nucleosides derivatives of allofuranose
[作者:Besada, P; Costas, T; Teijeira, M; Teran, C,期刊:European Journal of Medicinal Chemistry, 页码:6114-6119 , 文章类型: Article,,卷期:2010年45-12]
- Several new purine nucleosides derivatives of allofuranose were prepared according to Vorbruggen method, starting from 1,2,5,6-di-O-isopropylidene-alpha-D-allofuranose and using 1,2,3,5,6-pentaacetoxy-beta-D-allofuranose...
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