- Anticancer activity and cDNA microarray studies of a (RS)-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl]-6-chloro-9H-purine, and an acyclic (RS)-O,N-acetalic 6-chloro-7H-purine
[作者:Caba, O; Diaz-Gavilan, M; Rodriguez-Serrano, F; Boulaiz, H; Aranega, A; Gallo, MA; Marchal, JA; Campos, JM,期刊:European Journal of Medicinal Chemistry, 页码:3802-3809 , 文章类型: Article,,卷期:2011年46-9]
- Completing a 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 was previously prepared. The most potent antiproliferative agent against the MCF-7 adenocarcinom...
- Isomalyngamide A, A-1 and their analogs suppress cancer cell migration in vitro
[作者:Chang, TT; More, SV; Lu, IH; Hsu, JC; Chen, TJ; Jen, YC; Lu, CK; Li, WS,期刊:European Journal of Medicinal Chemistry, 页码:3810-3819 , 文章类型: Article,,卷期:2011年46-9]
- Isomalyngamide A (1) and A-1 (2) were isolated from the Taiwanese Lyngbya majuscule and the latter structure was elucidated by a combination of NMR spectroscopic analysis and HRESIMS measurement. We report the isolation ...
- Synthesis and anticancer activity of chalcone-pyrrolobenzodiazepine conjugates linked via 1,2,3-triazole ring side-armed with alkane spacers
[作者:Kamal, A; Prabhakar, S; Ramaiah, MJ; Reddy, PV; Reddy, CR; Mallareddy, A; Shankaraiah, N; Reddy, TLN; Pushpavalli, SNCVL; Pal-Bhadra, M,期刊:European Journal of Medicinal Chemistry, 页码:3820-3831 , 文章类型: Article,,卷期:2011年46-9]
- Aiming to develop multitarget drugs for the anticancer treatment, a new class of chalcone-pyrrolo[2,1-c] [1,4]benzodiazepine (PBD) conjugates linked through a 1,2,3-triazole moiety containing alkane spacers has been desi...
- Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of L-3 '-azido-2 ',3 '-dideoxypurine nucleosides
[作者:Zhang, HW; Detorio, M; Herman, BD; Solomon, S; Bassit, L; Nettles, JH; Obikhod, A; Tao, SJ; Mellors, JW; Sluis-Cremer, N; Coats, SJ; Schinazi, RF,期刊:European Journal of Medicinal Chemistry, 页码:3832-3844 , 文章类型: Article,,卷期:2011年46-9]
- Microwave-assisted optimized transglycosylation reactions were used to prepare eleven modified L-3'-azido-2',3'-dideoxypurine nucleosides. These L-nucleoside analogs were evaluated against HIV and hepatitis B virus. The ...
- Synthesis and anti-inflammatory effects of a series of novel 7-hydroxycoumarin derivatives
[作者:Timonen, JM; Nieminen, RM; Sareila, O; Goulas, A; Moilanen, LJ; Haukka, M; Vainiotalo, P; Moilanen, E; Aulaskari, PH,期刊:European Journal of Medicinal Chemistry, 页码:3845-3850 , 文章类型: Article,,卷期:2011年46-9]
- A number of 7-hydroxycoumarins have been synthesised by Pechmann cyclisation using differently substituted resorcinols employing perchloric acid as the condensing agent. All the compounds have been characterised by analy...
- Synthesis and structure of new bicopper(II) complexes bridged by N-(2-aminopropyl)-N '-(2-oxidophenyl)oxamide: The effects of terminal ligands on structures, anticancer activities and DNA-binding properties
[作者:Li, XW; Zheng, YJ; Li, YT; Wu, ZY; Yan, CW,期刊:European Journal of Medicinal Chemistry, 页码:3851-3857 , 文章类型: Article,,卷期:2011年46-9]
- A novel dissymmetrical N,N'-bis(substituted)oxamide ligand, N-(2-aminopropyl)-N'-(2-oxido- phenyl) oxamide (H(3)apopoxd) (L), and its three bicopper(II) complexes, [Cu(2)(apopoxd)(bpy)]- (ClO(4))center dot H(2)O (1), [Cu...
- Design, synthesis and bioevaluation of novel candidate selective estrogen receptor modulators
[作者:Yadav, Y; MacLean, ED; Bhattacharyya, A; Parmar, VS; Balzarini, J; Barden, CJ; Too, CKL; Jha, A,期刊:European Journal of Medicinal Chemistry, 页码:3858-3866 , 文章类型: Article,,卷期:2011年46-9]
- In an systematic attempt to develop novel Selective Estrogen Receptor Modulators (SERMs), chiral 1-((4-(2-(dialkylamino)ethoxy)phenyl)(2-hydroxynaphthalen-1-yl)methyl)piperidin-4-ols were designed based on an accepted ph...
- Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation
[作者:Deprez-Poulain, R; Cousaert, N; Toto, P; Willand, N; Deprez, B,期刊:European Journal of Medicinal Chemistry, 页码:3867-3876 , 文章类型: Article,,卷期:2011年46-9]
- Ullmann-type reactions are becoming a major tool in medicinal chemistry. In this article, we describe the use of these Copper-catalyzed reactions with various precursors, acyl-heteroarylamines or pyrazoles of interest fo...
- Synthesis and biological evaluation of the glycoside (25R)-3 beta,16 beta-diacetoxy-22-oxocholest-5-en-26-yl beta-D-glucopyranoside: A selective anticancer agent in cervicouterine cell lines
[作者:Fernandez-Herrera, MA; Lopez-Munoz, H; Hernandez-Vazquez, JMV; Lopez-Davila, M; Mohan, S; Escobar-Sanchez, ML; Sanchez-Sanchez, L; Pinto, BM; Sandoval-Ramirez, J,期刊:European Journal of Medicinal Chemistry, 页码:3877-3886 , 文章类型: Article,,卷期:2011年46-9]
- The synthesis and biological evaluation of the new cholestane glycoside (25R)-3 beta,16 beta-diacetoxy-22oxocholest-5-en-26-yl beta-D-glucopyranoside starting from diosgenin is described. This compound showed selective a...
- New insights into the structural requirements for pro-apoptotic agents based on 2,4-diaminoquinazoline, 2,4-diaminopyrido[2,3-d]pyrimidine and 2,4-diaminopyrimidine derivatives
[作者:Font, M; Gonzalez, A; Palop, JA; Sanmartin, C,期刊:European Journal of Medicinal Chemistry, 页码:3887-3899 , 文章类型: Article,,卷期:2011年46-9]
- As a continuation of our work on new anti-tumoral derivatives with selective pro-apoptotic activity in cancer cells, we describe the synthesis and the preliminary evaluation of the cytotoxic and pro-apoptotic activities ...
- Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives
[作者:Rhee, HK; Yoo, JH; Lee, E; Kwon, YJ; Seo, HR; Lee, YS; Choo, HYP,期刊:European Journal of Medicinal Chemistry, 页码:3900-3908 , 文章类型: Article,,卷期:2011年46-9]
- Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (5e, 5k, 5t, 6c and 6f) showed relatively high cytotoxic activity. E...
- Probing the difference between BH3 groove of Mcl-1 and Bcl-2 protein: Implications for dual inhibitors design
[作者:Zhang, ZC; Yang, HN; Wu, GY; Li, ZQ; Song, T; Li, XQ,期刊:European Journal of Medicinal Chemistry, 页码:3909-3916 , 文章类型: Article,,卷期:2011年46-9]
- Based on our previous discovery of a dual inhibitor of Mcl-1 and Bcl-2, 3-thiomorpholin-8-oxo-8H-acenaphthol[,2-b]pyrrole-9-carbonitrile (1, S1), and guided by structure insight of 1 complex with Mcl-1 and Bcl-2, we expl...
- Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors
[作者:Jin, CH; Sreenu, D; Krishnaiah, M; Subrahmanyam, VB; Rao, KS; Mohan, AVN; Park, CY; Son, JY; Son, DH; Park, HJ; Sheen, YY; Kim, DK,期刊:European Journal of Medicinal Chemistry, 页码:3917-3925 , 文章类型: Article,,卷期:2011年46-9]
- A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles 14a-d, 15a-d, 17a, 17b, 18a-d, 19a, and 19b has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and ...
- Combination of pharmacophore model development and binding mode analyses: Identification of ligand features essential for I kappa B kinase-beta (IKK beta) inhibitors and virtual screening based on it
[作者:Sun, HP; Zhu, J; Chen, FH; Zhang, SL; Zhang, Y; You, QD,期刊:European Journal of Medicinal Chemistry, 页码:3942-3952 , 文章类型: Article,,卷期:2011年46-9]
- I kappa B kinase beta (IKK beta) is an important anti-cancer target that plays crucial role in activating the transcription factor NF-kappa B in response to various inflammatory stimuli. In order to discover novel IKK be...
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