- Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum
[作者:Li, N; Wu, CF; Xu, XY; Liu, ZY; Li, X; Zhao, YQ,期刊:European Journal of Medicinal Chemistry, 页码:173-178 , 文章类型: Article,,卷期:2012年50-1]
- Five novel triterpenes were isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum and identified as gypensapogenin A (1), gypensapogenin B (2), gypensapogenin C (3), 3-O-beta-D-glucopyranosyl-gypensapo...
- Novel acid-type cyclooxygenase-2 inhibitors: Design, synthesis, and structure-activity relationship for anti-inflammatory drug
[作者:Hayashi, S; Ueno, N; Murase, A; Nakagawa, Y; Takada, J,期刊:European Journal of Medicinal Chemistry, 页码:179-195 , 文章类型: Article,,卷期:2012年50-1]
- Cyclooxygenase (COX) is a key rate-limiting enzyme for prostaglandin (PG) production cascades in the human body. The mechanisms of both the anti-inflammation effects and the side-effects of traditional COX inhibitors are...
- Total synthesis and structure-activity relationships of new echinocandin-like antifungal cyclolipohexapeptides
[作者:Yao, JZ; Liu, HM; Zhou, T; Chen, H; Miao, ZY; Sheng, CQ; Zhang, WN,期刊:European Journal of Medicinal Chemistry, 页码:196-208 , 文章类型: Article,,卷期:2012年50-1]
- A series of new echinocandin-like cyclolipohexapeptides were designed and total synthesized via solution phase [3 + 3]-segment coupling strategy with an attempt to improve antifungal activity. The designed compounds show...
- Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach
[作者:Distinto, S; Esposito, F; Kirchmair, J; Cardia, MC; Gaspari, M; Maccioni, E; Alcaro, S; Markt, P; Wolber, G; Zinzula, L; Tramontano, E,期刊:European Journal of Medicinal Chemistry, 页码:216-229 , 文章类型: Article,,卷期:2012年50-1]
- We report the first application of ligand-based virtual screening (VS) methods for discovering new compounds able to inhibit both human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT)-associated function...
- Galactolipids from Bauhinia racemosa as a new class of antifilarial agents against human lymphatic filarial parasite, Brugia malayi
[作者:Sashidhara, KV; Singh, SP; Misra, S; Gupta, J; Misra-Bhattacharya, S,期刊:European Journal of Medicinal Chemistry, 页码:230-235 , 文章类型: Article,,卷期:2012年50-1]
- Bioassay guided fractionation of ethanolic extract of the leaves of Bauhinia racemosa led to the isolation of galactolipid and catechin class of the compounds (1-7) from the most active n-butanol fraction (F4). Among the...
- Structure-activity studies on the anti-proliferation activity of ajoene analogues in WHCO1 oesophageal cancer cells
[作者:Kaschula, CH; Hunter, R; Stellenboom, N; Calm, MR; Winks, S; Ogunleye, T; Richards, P; Cotton, J; Zilbeyaz, K; Wang, YB; Siyo, V; Ngarande, E; Parker, MI,期刊:European Journal of Medicinal Chemistry, 页码:236-254 , 文章类型: Article,,卷期:2012年50-1]
- The organosulfur compound ajoene derived from the rearrangement of allicin found in crushed garlic can inhibit the proliferation of tumour cells by inducing G(2)/M cell cycle arrest and apoptosis. We report on the applic...
- Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold
[作者:Ilic, M; Kikelj, D; Ilas, J,期刊:European Journal of Medicinal Chemistry, 页码:255-263 , 文章类型: Article,,卷期:2012年50-1]
- Fluorinated 3,4-dihydro-2H-1,4-benzoxazine derivatives possessing both thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activities were prepared as potential dual antithrombotic compounds. Fluorine sca...
- Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose) polymerase-1 inhibitors
[作者:Kulkarni, SS; Singh, S; Shah, JR; Low, WK; Talele, TT,期刊:European Journal of Medicinal Chemistry, 页码:264-273 , 文章类型: Article,,卷期:2012年50-1]
- We have demonstrated that quinazolin-4(3H)-one, a nicotinamide (NI) mimic with PARP-1 inhibitory activity in the high micromolar range (IC(50) = 5.75 mu M) could be transformed into highly active derivatives with only ma...
- Multi-component synthesis and in vitro and in vivo anticancer activity of novel arylmethylene bis-isoxazolo[4,5-b]pyridine-N-oxides
[作者:Rajanarendar, E; Raju, S; Reddy, MN; Krishna, SR; Kiran, LH; Reddy, ARN; Reddy, YN,期刊:European Journal of Medicinal Chemistry, 页码:274-279 , 文章类型: Article,,卷期:2012年50-1]
- A three component one-pot protocol has been investigated for the synthesis of arylmethylene bis-isoxazolo[4,5-b]pyridine-N-oxides 1 from the commercially available materials. The title compounds 1 were also synthesized b...
- Design, synthesis and biological evaluation of novel (E)-alpha-benzylsulfonyl chalcone derivatives as potential BRAF inhibitors
[作者:Li, QS; Li, CY; Lu, X; Zhang, H; Zhu, HL,期刊:European Journal of Medicinal Chemistry, 页码:288-295 , 文章类型: Article,,卷期:2012年50-1]
- Activating mutations in the BRAF serine/threonine kinase are found in more than 70% of human melanomas, >90% of which are BRAF(V600E). It provides new therapeutic opportunities in malignant melanoma. In silico and in vit...
- Three novel cyclic hexapeptides from Streptomyces alboflavus 313 and their antibacterial activity
[作者:Ji, ZQ; Wei, SP; Fan, LX; Wu, WJ,期刊:European Journal of Medicinal Chemistry, 页码:296-303 , 文章类型: Article,,卷期:2012年50-1]
- Three novel cyclic hexapeptides, designated NW-G05 (1), NW-G06 (2) and NW-G07 (3), were isolated from the fermentation broth of Streptomyces alboflavus 313. Their structures were elucidated on the basis of extensive spec...
- Use of copper(I) catalyzed azide alkyne cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors
[作者:Letribot, B; Akue-Gedu, R; Santio, NM; El-Ghozzi, M; Avignant, D; Cisnetti, F; Koskinen, PJ; Gautier, A; Anizon, F; Moreau, P,期刊:European Journal of Medicinal Chemistry, 页码:304-310 , 文章类型: Article,,卷期:2012年50-1]
- We have previously demonstrated that pyrrolo[2,3-a]carbazole-3-carbaldehydes are potent Pim kinase inhibitors with in vitro antiproliferative activities. In the present study, we report the synthesis of new pyrrolocarbaz...
- Novel triacsin C analogs as potential antivirals against rotavirus infections
[作者:Kim, Y; George, D; Prior, AM; Prasain, K; Hao, SH; Le, DD; Hua, DH; Chang, KO,期刊:European Journal of Medicinal Chemistry, 页码:311-318 , 文章类型: Article,,卷期:2012年50-1]
- Recently our group has demonstrated that cellular triglyceride (TG) levels play an important role in rotavirus replication. In this study, we further examined the roles of the key enzymes for TG synthesis (lipogenesis) i...
- Photoactivated DNA cleavage and anticancer activity of pyrenyl-terpyridine lanthanide complexes
[作者:Hussain, A; Gadadhar, S; Goswami, TK; Karande, AA; Chakravarty, AR,期刊:European Journal of Medicinal Chemistry, 页码:319-331 , 文章类型: Article,,卷期:2012年50-1]
- Lanthanide(III) complexes [Ln(R-tpy)(acac)(NO(3))(2)] (Ln = La(III) in 1, 2; Gd(III) in 4, 5) and [Ln(py-tpy)(sacac)(NO(3))(2)] (Ln = La(III), Gd(III), 6), where R-tpy is 4'-phenyl-2,2':6',2 ''-terpyridine (ph-tpy in 1, ...
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