- Structure-based optimization of click-based histone deacetylase inhibitors
[作者:Hou, JL; Feng, CR; Li, ZH; Fang, QH; Wang, HH; Gu, GX; Shi, YK; Liu, P; Xu, F; Yin, Z; Shen, J; Wang, P,期刊:European Journal of Medicinal Chemistry, 页码:3190-3200 , 文章类型: Article,,卷期:2011年46-8]
- Previously, we reported a click-chemistry based approach to the synthesis of a novel class of histone deacetylase (HDAC) inhibitors [1]. The lead compound NSC746457 was found to be as potent as SAHA (Vorinostat). Further...
- Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship
[作者:Thapa, U; Thapa, P; Karki, R; Yun, M; Choi, JH; Jahng, Y; Lee, E; Jeon, KH; Na, Y; Ha, EM; Cho, WJ; Kwon, Y; Lee, ES,期刊:European Journal of Medicinal Chemistry, 页码:3201-3209 , 文章类型: Article,,卷期:2011年46-8]
- Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for topoisomerase I and...
- Design and synthesis of spiro derivatives of parthenin as novel anti-cancer agents
[作者:Reddy, DM; Qazi, NA; Sawant, SD; Bandey, AH; Srinivas, J; Shankar, M; Singh, SK; Verma, M; Chashoo, G; Saxena, A; Mondhe, D; Saxena, AK; Sethi, VK; Taneja, SC; Qazi, GN; Kumar, HMS,期刊:European Journal of Medicinal Chemistry, 页码:3210-3217 , 文章类型: Article,,卷期:2011年46-8]
- Several novel Spiro derivatives of parthenin (1) have been synthesized by the dipolar cycloaddition using various dipoles viz; benzonitrile oxides, nitrones and azides with exocyclic double bond of C ring (alpha-methylen...
- Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines
[作者:El-Gamal, MI; Jung, MH; Lee, WS; Sim, T; Yoo, KH; Oh, CH,期刊:European Journal of Medicinal Chemistry, 页码:3218-3226 , 文章类型: Article,,卷期:2011年46-8]
- Synthesis of a new series of diarylureas and diarylamides having 1H-pyrrolo[3,2-c]pyridine scaffold is described. Their in vitro antiproliferative activity against A375P human melanoma cell line was tested and the effect...
- A class of oral N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carbonyl]- N '-(amino-acid-acyl)hydrazine: Discovery, synthesis, in vitro anti-platelet aggregation/in vivo anti-thrombotic evaluation and 3D QSAR analysis
[作者:Yao, K; Zhao, M; Zhang, XY; Wang, YJ; Li, L; Zheng, MQ; Peng, SQ,期刊:European Journal of Medicinal Chemistry, 页码:3237-3249 , 文章类型: Article,,卷期:2011年46-8]
- The in vivo anti-thrombotic activities of amino acid modified tetrahydro-beta-carbolines depended upon the proximity of the side chain of the amino acid residue to the carboline-cycle. Based on this proximity the compute...
- Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors
[作者:Szymanski, P; Karpinski, A; Mikiciuk-Olasik, E,期刊:European Journal of Medicinal Chemistry, 页码:3250-3257 , 文章类型: Article,,卷期:2011年46-8]
- The synthesis and biochemical evaluation of new hybrids of tacrine (THA) and 4-fluorobenzoic acid (4-FBA) possessing activity towards acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition are presented...
- Structure-activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity
[作者:Subramanian, S; Kim, NS; Thanigaimalai, P; Sharma, VK; Lee, KC; Kang, JS; Kim, HM; Jung, SH,期刊:European Journal of Medicinal Chemistry, 页码:3258-3264 , 文章类型: Article,,卷期:2011年46-8]
- To define the SAR, a series of novel N-arylsulfonylimidazolidinone derivatives were evaluated for their in vitro anticancer activity against five human tumor cell lines, including A549, COLO205, KATO III, K562, SK-OV-3 a...
- Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones
[作者:Kamal, A; Malik, MS; Bajee, S; Azeeza, S; Faazil, S; Ramakrishna, S; Naidu, VGM; Vishnuwardhan, MVPS,期刊:European Journal of Medicinal Chemistry, 页码:3274-3281 , 文章类型: Article,,卷期:2011年46-8]
- A series of conformationally flexible and restricted dimers of monastrol as well as related dihydropyrimidones have been synthesized by employing one-pot Biginelli multicomponent reaction. These dimers have been evaluate...
- Synthesis, cellular uptake, apopotosis, cytotoxicity, cell cycle arrest, interaction with DNA and antioxidant activity of ruthenium(II) complexes
[作者:Huang, HL; Li, ZZ; Liang, ZH; Yao, JH; Liu, YJ,期刊:European Journal of Medicinal Chemistry, 页码:3282-3290 , 文章类型: Article,,卷期:2011年46-8]
- A new ligand and two ruthenium(II) complexes [Ru(bpy)(2)(DNPIP)](ClO(4))(2) 1 and [Ru(bpy)(2)(DAPIP)](ClO(4))(2) 2 were synthesized and characterized. The DNA-binding constants for complexes 1 and 2 were determined to be...
- Aldol derivatives of Thioxoimidazolidinones as potential anti-prostate cancer agents
[作者:Khatik, GL; Kaur, J; Kumar, V; Tikoo, K; Venugopalan, P; Nair, VA,期刊:European Journal of Medicinal Chemistry, 页码:3291-3301 , 文章类型: Article,,卷期:2011年46-8]
- The paper discusses the synthesis and stereochemical aspects of the anti aldol products, 3-(substituted phenyl)-5-[(substituted phenyl) hydroxy methyl]-5-methyl-4-oxo-2-thioxoimidazolidines. The stereochemistry observed ...
- Cytotoxic oxasqualenoids from the red alga Laurencia viridis
[作者:Cen-Pacheco, F; Villa-Pulgarin, JA; Mollinedo, F; Norte, M; Daranas, AH; Fernandez, JJ,期刊:European Journal of Medicinal Chemistry, 页码:3302-3308 , 文章类型: Article,,卷期:2011年46-8]
- Three new polyether squalene derivatives 15-dehydroxythyrsenol A (2), prethyrsenol A (3) and 13-hydroxyprethyrsenol A (4) have been isolated from the red alga Laurencia viridis. Their structures were determined through t...
- Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase
[作者:Recio, E; Musso-Buendia, A; Vidal, AE; Ruda, GF; Kasinathan, G; Nguyen, C; Ruiz-Perez, LM; Gilbert, IH; Gonzalez-Pacanowska, D,期刊:European Journal of Medicinal Chemistry, 页码:3309-3314 , 文章类型: Article,,卷期:2011年46-8]
- We have previously identified a series of triphenylmethane derivatives of deoxyuridine with antimalarial activity in vitro which selectively inhibit Plasmodium falciparum deoxyuridine triphosphate nucleotidohydrolase (Pf...
- Selenocyanates and diselenides: A new class of potent antileishmanial agents
[作者:Plano, D; Baquedano, Y; Moreno-Mateos, D; Font, M; Jimenez-Ruiz, A; Palop, JA; Sanmartin, C,期刊:European Journal of Medicinal Chemistry, 页码:3315-3323 , 文章类型: Article,,卷期:2011年46-8]
- Thirty five selenocyanate and diselenide compounds were subjected to in vitro screening against Leishmania infantum promastigotes and the most active ones were also tested in an axenic amastigote model. In order to estab...
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