- Aconitum and Delphinium alkaloids of curare-like activity. QSAR analysis and molecular docking of alkaloids into AChBP
[作者:Turabekova, MA; Rasulev, BF; Dzhakhangirov, FN; Leszczynska, D; Leszczynski, J,期刊:European Journal of Medicinal Chemistry, 页码:3885-3894 , 文章类型: Article,,卷期:2010年45-9]
- Early studies have shown that some of diterpenoid alkaloids, found in highly toxic plants of the genera Aconitum and Delphinium, act at neuronal nicotinic acetylcholine receptors (nAChRs) and exhibit potent N-cholinolyti...
- Antimony(III) complexes with 2-benzoylpyridine-derived thiosemicarbazones: Cytotoxicity against human leukemia cell lines
[作者:Reis, DC; Pinto, MCX; Souza-Fagundes, EM; Wardell, SMSV; Wardell, JL; Beraldo, H,期刊:European Journal of Medicinal Chemistry, 页码:3904-3910 , 文章类型: Article,,卷期:2010年45-9]
- The antimony(III) complexes [Sb(2Bz4DH)Cl-2) (1), [Sb(H2Bz4M)Cl-3]center dot 2H(2)O (2) and [Sb(2Bz4Ph)Cl-2] (3) were obtained with 2-benzoylpyridine thiosemicarbazone (H2Bz4DH) and its N(4)-methyl (H2Bz4M) and N(4)-phen...
- Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues
[作者:Woo, S; Kang, DH; Nam, JM; Lee, CS; Ha, EM; Lee, ES; Kwon, Y; Na, Y,期刊:European Journal of Medicinal Chemistry, 页码:4221-4228 , 文章类型: Article,,卷期:2010年45-9]
- In order to develop potential anti-cancer agents that act on topoisomerase II and DNA, we have synthesized 12 new xanthone derivatives. In the cytotoxicity test, compounds 17 and 31 exhibited 2- to 7-fold stronger inhibi...
- Regioselective synthesis and molecular modeling study of vasorelaxant active 7,9-dioxa-1,2-diaza-spiro[4.5]dec-2-ene-6,10-diones
[作者:Girgis, AS; Ismail, NSM; Farag, H; El-Eraky, WI; Saleh, DO; Tala, SR; Katritzky, AR,期刊:European Journal of Medicinal Chemistry, 页码:4229-4238 , 文章类型: Article,,卷期:2010年45-9]
- Nitrilimines (PhC-:N+:NR') generated in situ from hydrazonoyl chlorides 2a,b reacted regioselectively with 5-arylidene-2,2-dimethyl[1,3]dioxane-4,6-diones 1a-f to afford 1.3,4-triaryl-8,8-dimethyl-7,9-dioxa-1,2-diaza-spi...
- DNA binding and DNA cleavage studies of a water soluble cobalt(II) complex containing dinitrogen Schiff base ligand: The effect of metal on the mode of binding
[作者:Shahabadi, N; Kashanian, S; Darabi, F,期刊:European Journal of Medicinal Chemistry, 页码:4239-4245 , 文章类型: Article,,卷期:2010年45-9]
- Binding interaction of a water soluble cobalt(II) complex of a Schiff base, SF, (SF = N,N'-bis(5-[(triphenylphosphonium chloride)-methyl] salicylidine)-o-phenylenediamine) with calf thymus DNA (CT-DNA) has been investiga...
- Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles
[作者:Padmavathi, V; Reddy, SN; Reddy, GD; Padmaja, A,期刊:European Journal of Medicinal Chemistry, 页码:4246-4251 , 文章类型: Article,,卷期:2010年45-9]
- A new class of oxadiazoles is prepared by treating aminosulfonylacetic acids with different carboxylic acid hydrazides. Interconversion of oxadiazoles to thiadiazoles is carried out with thiourea. The compounds are scree...
- Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors
[作者:Sheng, CQ; Xu, H; Wang, WY; Cao, YB; Dong, GQ; Wang, SZ; Che, XY; Ji, HT; Miao, ZY; Yao, JZ; Zhang, WN,期刊:European Journal of Medicinal Chemistry, 页码:3531-3540 , 文章类型: Article,,卷期:2010年45-9]
- N-myristoyltransferase (NMT) has been a promising new target for the design of novel antifungal agents with new mode of action. A series of benzoxazole and indole derivatives were designed and synthesized as isosteric an...
- QSAR studies of bioactivities of 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b] pyridines as 5-HT6 receptor ligands using physicochemical descriptors and MLR and ANN-modeling
[作者:Goodarzi, M; Freitas, MP; Ghasemi, N,期刊:European Journal of Medicinal Chemistry, 页码:3911-3915 , 文章类型: Article,,卷期:2010年45-9]
- Four molecular descriptors were selected from a pool of variables using genetic algorithm, and then used to built a QSAR model for a series of 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 receptor ago...
- Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/isoxazole-pyrrolobenzodiazepine conjugates as potential anticancer agents
[作者:Kamal, A; Reddy, JS; Ramaiah, MJ; Dastagiri, D; Bharathi, EV; Azhar, MA; Sultana, F; Pushpavalli, SNCVL; Pal-Bhadra, M; Juvekar, A; Sen, S; Zingde, S,期刊:European Journal of Medicinal Chemistry, 页码:3924-3937 , 文章类型: Article,,卷期:2010年45-9]
- A series of 3,5-diaryl-isoxazoline/isoxazole linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates were prepared. These conjugates showed potent anticancer activity with GI(50) values in the range of <0.1-3.6 mu M. S...
- Hypervalent iodine(III) mediated synthesis of novel unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles as antibacterial and antifungal agents
[作者:Prakash, O; Kumar, M; Kumar, R; Sharma, C; Aneja, KR,期刊:European Journal of Medicinal Chemistry, 页码:4252-4257 , 文章类型: Article,,卷期:2010年45-9]
- A series of novel 2,5-disubstituted 1,3,4-oxadiazoles 4 have been conveniently synthesized by oxidative cyclization of pyrazolylaldehyde N-acylhydrazones 3 promoted by iodobenzene diacetate under mild conditions (11 exam...
- Prenylflavonoids and prenyl/alkyl-phloroacetophenones: Synthesis and antitumour biological evaluation
[作者:Basabe, P; de Roman, M; Marcos, IS; Diez, D; Blanco, A; Bodero, O; Mollinedo, F; Sierra, BG; Urones, JG,期刊:European Journal of Medicinal Chemistry, 页码:4258-4269 , 文章类型: Article,,卷期:2010年45-9]
- Several prenylflavonoids have been synthesised and tested against human tumour cell lines. The prenyl unit has been geranyl or a labdane diterpene. These labdane-flavonoids have been synthesised for the first time. The a...
- Extending pK(a) prediction accuracy: High-throughput pK(a) measurements to understand pK(a) modulation of new chemical series
[作者:Milletti, F; Storchi, L; Goracci, L; Bendels, S; Wagner, B; Kansy, M; Cruciani, G,期刊:European Journal of Medicinal Chemistry, 页码:4270-4279 , 文章类型: Article,,卷期:2010年45-9]
- We have recently developed a tool. MoKa, to predict the pK(a) of organic compounds using a large dataset of over 26,500 literature pK(a) values as a training set. However, predicting accurately pK(a) (<0.5 pH units) rema...
- Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold
[作者:He, GJ; Dou, DF; Wei, LQ; Alliston, KR; Groutas, WC,期刊:European Journal of Medicinal Chemistry, 页码:4280-4287 , 文章类型: Article,,卷期:2010年45-9]
- A series of compounds based on the N-amino-4-imidazolidinone scaffold was synthesized and screened against human neutrophil elastase (HNE). These studies lead to the identification of a selective, low micromolar reversib...
- Chiral preference of L-tryptophan derived metal-based antitumor agent of late 3d-metal ions (Co(II), Cu(II) and Zn(II)) in comparison to D- and DL-tryptophan analogues: Their in vitro reactivity towards CT DNA, 5 '-GMP and 5 '-TMP
[作者:Arjmand, F; Muddassir, M; Khan, RH,期刊:European Journal of Medicinal Chemistry, 页码:3549-3557 , 文章类型: Article,,卷期:2010年45-9]
- To evaluate the biological preference of chiral drugs for molecular target DNA, new potential metal-based chemotherapeutic agents 1-3 (a-c) of late 3d-transition metals derived from I. form, D form, and DL-tryptophan, re...
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