- Ligand-based discovery of novel trypanosomicidal drug-like compounds: In silico identification and experimental support
[作者:Castillo-Garit, JA; Vega, MC; Rolon, M; Marrero-Ponce, Y; Gomez-Barrio, A; Escario, JA; Bello, AA; Montero, A; Torrens, F; Perez-Gimenez, F; Aran, VJ; Abad, C,期刊:European Journal of Medicinal Chemistry, 页码:3324-3330 , 文章类型: Article,,卷期:2011年46-8]
- Two-dimensional bond-based linear indices and linear discriminant analysis are used in this report to perform a quantitative structure activity relationship study to identify new trypanosomicidal compounds. A database wi...
- Development of novel naphthalimide derivatives and their evaluation as potential melanoma therapeutics
[作者:Sk, UH; Gowda, ASP; Crampsie, MA; Yun, JK; Spratt, TE; Amin, S; Sharma, AK,期刊:European Journal of Medicinal Chemistry, 页码:3331-3338 , 文章类型: Article,,卷期:2011年46-8]
- Synthesis and anti-melanoma activity of various naphthalimide analogs, rationally modified by introducing isothiocyanate (ITC) and thiourea (TU) functionalities, found in well-known anti-cancer agents, is described. The ...
- Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors
[作者:Wu, WB; Ou, JB; Huang, ZH; Chen, SB; Ou, TM; Tan, JH; Li, D; Shen, LL; Huang, SL; Gu, LQ; Huang, ZS,期刊:European Journal of Medicinal Chemistry, 页码:3339-3347 , 文章类型: Article,,卷期:2011年46-8]
- A series of mansonone F (MF) derivatives were designed and synthesized. These compounds were found to be strong inhibitors for topoisomerases, with much more significant inhibition for topoisomerase II rather than topois...
- Synthesis and structural investigation of some pyrimido[5,4-c]quinolin-4(3H)-one derivatives with a long-chain arylpiperazine moiety as potent 5-HT(1A/2A) and 5-HT(7) receptor ligands
[作者:Lewgowd, W; Bojarski, AJ; Szczesio, M; Olczak, A; Glowka, ML; Mordalski, S; Stanczak, A,期刊:European Journal of Medicinal Chemistry, 页码:3348-3361 , 文章类型: Article,,卷期:2011年46-8]
- A series of new pyrimido[5,4-c]quinolin-4(3H)-ones with variable length of the spacer between amide and 4-arylpiperazine moiety were prepared to further explore the role of a terminal portion in the serotonergic activity...
- Synthesis, characterization and cytotoxicity of some novel 1,3-disubstituted-2,3-dihydro-2-iminobenzimidazoles
[作者:Mavrova, AT; Wesselinova, D; Vassilev, N; Tsenov, JA,期刊:European Journal of Medicinal Chemistry, 页码:3362-3367 , 文章类型: Article,,卷期:2011年46-8]
- Some new 1,3-disubstituted-2,3-dihydro-2-iminobenzimidazoles were synthesized using 1-(un) substituted-2-aminobenzimidazoles as precursors in order to determine their cytotoxicity. The structures of the compounds were co...
- Conjugates of 3 alpha-methoxyserrat-14-en-21 beta-ol (PJ-1) and 3 beta-methoxyserrat-14-en-21 beta-ol (PJ-2) as cancer chemopreventive agents
[作者:Tanaka, R; Tsujii, H; Yamada, T; Kajimoto, T; Tokuda, H; Arai, T; Suzuki, N; Hasegawa, J; Hamashima, Y; Node, M,期刊:European Journal of Medicinal Chemistry, 页码:3368-3375 , 文章类型: Article,,卷期:2011年46-8]
- 3 alpha-Methoxyserrat-14-en-21 beta-ol (PJ-1) and 3 beta-methoxyserrat-14-en-21 beta-ol (PJ-2) were conjugated with well-known phenolic compounds, narigenin, hesperetin, genistein, and daidzein (1-8). Other conjugates of...
- Evaluation of DNA binding, DNA cleavage, protein binding and in vitro cytotoxic activities of bivalent transition metal hydrazone complexes
[作者:Krishnamoorthy, P; Sathyadevi, P; Cowley, AH; Butorac, RR; Dharmaraj, N,期刊:European Journal of Medicinal Chemistry, 页码:3376-3387 , 文章类型: Article,,卷期:2011年46-8]
- Divalent Co, Ni and Cu hydrazone complexes containing [N'-(phenyl(pyridine-2-yl)methylidene) benzohydrazide] ligand were synthesised and characterised. Interactions of these complexes with DNA revealed an intercalative m...
- Synthesis, activity and pharmacokinetics of novel antibacterial 15-membered ring macrolones
[作者:Fajdetic, A; Vinter, A; Paljetak, HC; Padovan, J; Jakopovic, IP; Kapic, S; Alihodzic, S; Filic, D; Modric, M; Kosutic-Hulita, N; Antolovic, R; Schoenfeld, ZI; Mutak, S; Haber, VE; Spaventi, R,期刊:European Journal of Medicinal Chemistry, 页码:3388-3397 , 文章类型: Article,,卷期:2011年46-8]
- Synthesis, antibacterial activity and pharmacokinetic properties of a novel class of macrolide antibiotics-macrolones-derived from azithromycin, comprising oxygen atom(s) in the linker and either free or esterified quino...
- Studies on quinones. Part 47. Synthesis of novel phenylaminophenanthridinequinones as potential antitumor agents
[作者:Valderrama, JA; Ibacache, A; Rodriguez, JA; Theoduloz, C; Benites, J,期刊:European Journal of Medicinal Chemistry, 页码:3398-3409 , 文章类型: Article,,卷期:2011年46-8]
- In our search for potential anticancer agents, a series of 8- and 9-phenylamino-3,4-tetrahydro-phenanthridine-1,7,10(2H)-triones with substituent variations at 6-, 8- and 9-positions were prepared using a highly efficien...
- A class of Trp-Trp-AA-OBzl: Synthesis, in vitro anti-proliferation/in vivo anti-tumor evaluation, intercalation-mechanism investigation and 3D QSAR analysis
[作者:Zhang, XY; Yang, YF; Zhao, M; Liu, L; Zheng, MQ; Wang, YJ; Wu, JH; Peng, SQ,期刊:European Journal of Medicinal Chemistry, 页码:3410-3419 , 文章类型: Article,,卷期:2011年46-8]
- From the anti-tumor active N-tryptophanyl-beta-carboline-3-carboxylic acid benzyl ester and beta-carboline-3-carbonyltryptophan benzyl ester, a pharmacophore, Trp-Trp-OBzl, was drawn. Based on the DOCK scores amino acid ...
- Semi-synthesis and antitumor activity of 6-isomers of 5, 8-O-dimethyl acylshikonin derivatives
[作者:Zhou, W; Zhang, X; Xiao, L; Ding, J; Liu, QH; Li, SS,期刊:European Journal of Medicinal Chemistry, 页码:3420-3427 , 文章类型: Article,,卷期:2011年46-8]
- We recently discovered that 5, 8-O-dimethyl acylshikonin derivatives displayed the selectivity towards MCF-7 and no toxicity to normal cells. Herein, a series of the corresponding 6-isomers of 5, 8-O-dimethyl acylshikoni...
- Angiotensin-I-converting enzyme inhibitory peptides: Chemical feature based pharmacophore generation
[作者:Wang, ZL; Zhang, SS; Jin, HW; Wang, W; Huo, JX; Zhou, LS; Wang, YF; Feng, FQ; Zhang, LR,期刊:European Journal of Medicinal Chemistry, 页码:3428-3433 , 文章类型: Article,,卷期:2011年46-8]
- A validated 3D pharmacophore model was generated for a series of ACE inhibitory peptides, which consisted of five features (two hydrophobic functions, two hydrogen bond acceptors, and a negative ionizable function). The ...
- Synthesis, structure and cytotoxicity of 3-C, N, S, Se substituted benzo[b] selenophene derivatives
[作者:Arsenyan, P; Paegle, E; Belyakov, S; Shestakova, I; Jaschenko, E; Domracheva, I; Popelis, J,期刊:European Journal of Medicinal Chemistry, 页码:3434-3443 , 文章类型: Article,,卷期:2011年46-8]
- Synthesis, molecular structure and cytotoxic activity of a series of 3-C, N, S, Se substituted benzo[6] selenophene derivatives on human fibrosarcoma HT-1080, mouse hepatoma MG-22A, and mouse fibroblasts 3T3 cell lines a...
- Could LogP be a principal determinant of biological activity in 18-crown-6 ethers? Synthesis of biologically active adamantane-substituted diaza-crowns
[作者:Supek, F; Ramljak, TS; Marjanovic, M; Buljubasic, M; Kragol, G; Ilic, N; Smuc, T; Zahradka, D; Mlinaric-Majerski, K; Kralj, M,期刊:European Journal of Medicinal Chemistry, 页码:3444-3454 , 文章类型: Article,,卷期:2011年46-8]
- 18-crown-6 ethers are known to exert their biological activity by transporting K(+) ions across cell membranes. Using non-linear Support Vector Machines regression, we searched for structural features that influence anti...
- Synthesis of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives and their anticancer activity
[作者:Kurumurthy, C; Rao, PS; Swamy, BV; Kumar, GS; Rao, PS; Narsaiah, B; Velatooru, LR; Pamanji, R; Rao, JV,期刊:European Journal of Medicinal Chemistry, 页码:3462-3468 , 文章类型: Article,,卷期:2011年46-8]
- A series of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives 5 and 6 was prepared starting from 2,3-active functional pyridine 1 via cyclization, propargylation followed by reaction with alkyl or perfluoroa...
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