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European Journal of Medicinal Chemistry
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#1Ahmed M. Shawky (UQU: Umm al-Qura University)H-Index: 6
#2Mohammed A.S. Abourehab (Minia University)H-Index: 4
Last.Ahmed M. Gouda (Beni-Suef University)H-Index: 7
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Abstract Two new series of pyrrolizine-5-carboxamides were synthesized and evaluated for their anticancer and anti-inflammatory activities. The new compounds exhibited potent cytotoxicity (IC50 = 0.10–22.96 μM) against three cancer (MCF-7, A2780 and HT29) cell lines with selectivity index in the range of 1–258. Moreover, these compounds also exhibited significant anti-inflammatory activity (18.13–44.51% inhibition of inflammation) mediated by inhibition of COX-1/2 with preferential inhibition of...
#1Mahsa Ansari (Mazandaran University of Medical Sciences)H-Index: 1
#2Mohammad Shokrzadeh (Mazandaran University of Medical Sciences)H-Index: 13
Last.Saeed Emami (Mazandaran University of Medical Sciences)H-Index: 33
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Abstract A new series of thiazole-2(3H)-thiones containing 4-(3,4,5-trimethoxyphenyl) moiety were synthesized as diaryl-heterocylic analogs of combretastatin A-4 with anticancer activity. The cytotoxicity evaluation of synthesized compounds against cancer cell lines (A549, MCF-7 and SKOV3) revealed that most of them had potent cytotoxic activity toward all tested cell lines (IC50s
#1Marek Bajda (Jagiellonian University Medical College)H-Index: 15
#2Dorota Łażewska (Jagiellonian University Medical College)H-Index: 10
Last.Barbara Malawska (Jagiellonian University Medical College)
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Abstract Multi-target-directed ligands seem to be an interesting approach to the treatment of complex disorders such as Alzheimer's disease. The aim of the present study was to find novel multifunctional compounds in a non-imidazole histamine H3 receptor ligand library. Docking-based virtual screening was applied for selection of twenty-six hits which were subsequently evaluated in Ellman's assay for the inhibitory potency toward acetyl- (AChE) and butyrylcholinesterase (BuChE). The virtual scre...
#1Samir Mehndiratta (TMU: Taipei Medical University)H-Index: 8
#2Mei-Hsiang Lin (TMU: Taipei Medical University)
Last.Jing-Ping Liou (TMU: Taipei Medical University)H-Index: 5
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Abstract Novel dual inhibitors of histone deacetylase (HDAC) and heat-shock protein 90 (HSP90) are synthesized and evaluated. These compounds are endowed with potent HDAC and HSP90 inhibitory activities with IC50 values in nanomolar range with Compound 20 (HDAC IC50 = 194 nM; HSP90α IC50 = 153 nM) and compound 26 (HDAC IC50 = 360 nM; HSP90α IC50 = 77 nM) displaying most potent HDAC and HSP90α inhibitory activities. Both of these compounds induce HSP70 expression and down regulate HSP90 client pr...
#1Hyeon Jeong Kim (KIST: Korea Institute of Science and Technology)H-Index: 2
#2Bo Ko Jang (KIST: Korea Institute of Science and Technology)H-Index: 2
Last.Ki Duk Park (Kyung Hee University)H-Index: 16
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Abstract Alzheimer's disease is a common neurodegenerative disease characterized by progressive degeneration and neuronal cell death, resulting in neural network dysfunction. As the underlying mechanisms, oxidative damage and neuroinflammation have been reported to contribute to the onset and deterioration of Alzheimer's disease. The nuclear factor E2-related factor 2-antioxidant responsive element (Nrf2-ARE) signaling pathway is a pivotal cellular defense mechanism against oxidative stress. Nrf...
#1Jiaqi Xiao (Qilu University of Technology)H-Index: 1
#2Zhou Sun (Qilu University of Technology)
Last.Feng Gao (Qilu University of Technology)H-Index: 1
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Abstract Hybrid molecules have the potential to enhance the efficacy against both drug-sensitive and drug-resistant organisms, and ferrocene hybrid Ferroquine has demonstrated great potency in clinical trials against both drug-sensitive and drug-resistant malaria. Accordingly, hybridization of ferrocene with other antimalarial pharmacophores represents a promising strategy to develop novel antimalarial candidates. This work attempts to systematically review the recent study of ferrocene hybrids ...
#1Qiong Wu (PKU: Peking University)H-Index: 1
#2Ruiying Wang (Peking Union Medical College)H-Index: 2
Last.Hongzheng Fu (PKU: Peking University)H-Index: 17
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Abstract Panaxatriol (PT) is a natural product derived from ginseng that possesses cardioprotective effects in isolated rat hearts. To develop more potent therapeutic agents against myocardial ischemia/reperfusion (MI/R) injury from natural products, a novel series of heterocycle ring-fused panaxatriol derivatives were designed and synthesized. In vitro results showed that approximately half of them exhibited increased cytoprotective activity compared with PT in a cardiomyocyte model of oxygen-g...
#1Abdullah A. Ghawanmeh (Universiti Malaysia Pahang)H-Index: 1
#2Hussein M. Al-Bajalan (UKM: National University of Malaysia)
Last.Kwok Feng Chong (Universiti Malaysia Pahang)H-Index: 16
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Abstract (−)-Colchicine, an anti-microtubulin polymerization agent, is a valuable medication and the drug of choice for gout, Behcet's disease and familial Mediterranean fever. It has a narrow therapeutic index due to its high toxicity towards normal cells. Nonetheless, numerous (−)-colchicine derivatives have been synthesized and studied for their structure-activity relationship and preferential toxicity. Different functional groups such as amides, thioamides, N-arylurea and 8,12-diene cyclic h...
#1Yachuang Wu (SPU: Shenyang Pharmaceutical University)H-Index: 1
#2Xiudong DingH-Index: 1
Last.Yanfang Zhao (SPU: Shenyang Pharmaceutical University)H-Index: 15
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Abstract We previously discovered a series of novel biaryloxazolidinone analogues bearing a hydrazone moiety with potent antibacterial activity. However, the most potent compound OB-104 exhibited undesirable chemical and metabolic instability. Herein, novel biaryloxazolidinone analogues were designed and synthesized to improve the chemical and metabolic stability. Compounds 6a-1, 6a-3, 14a-1, 14a-3 and 14a-7 showed significant antibacterial activity against the tested Gram-positive bacteria as c...
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