European Journal of Medicinal Chemistry
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Abstract null null Selection of R-groups (substituents, functional groups) is of critical importance for the generation of analogues during hit-to-lead and lead optimization. In the practice of medicinal chemistry, R-group selection is mostly driven by chemical experience and intuition taking synthetic criteria into account. However, systematic analyses of substituents are currently rare. In this work, we have computationally isolated R-groups from more than 17,000 analog series comprising ∼315,...
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#1Dong-Dong Luo (Ocean University of China)H-Index: 3
#2Yuhang Zhang (PKU: Peking University)
Last. Wen-Yu Wang (Capital Medical University)H-Index: 1
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Abstract null null 5-Fluorouracil (5-FU) and its prodrugs are the essential clinical drugs for colorectal cancer (CRC) treatment. However, the drug resistance of 5-FU has caused high mortality of CRC patients. Thus, it is urgent to develop reversal agents of 5-FU resistance. Sphingosine-1-phosphate receptor 2 (S1PR2) was proved to be a potential target for reversing 5-FU resistance, but the activity of known S1PR2 antagonists JTE-013 were weak in 5-FU-resistant cell lines. To develop more potent...
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#1Jiang-Jiang Tang (NWAFU: Northwest A&F University)H-Index: 16
#2Min-Ran Wang (NWAFU: Northwest A&F University)
Last. Jin-Ming Gao (NWAFU: Northwest A&F University)H-Index: 30
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Abstract null null Dysregulation of neuroinflammation is a key pathological factor in the progressive neuronal damage of neurodegenerative diseases. An in-house natural products library of 1407 compounds were screened against neuroinflammation in lipopolysaccharide (LPS)-activated microglia cells to identify a novel hit 1,6-O,O-diacetylbritannilactone (OABL) with anti-neuroinflammatory activity. Furthermore, a 1,10-seco-eudesmane sesquiterpenoid library containing 33 compounds was constructed by...
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#1Marina Marinović (University of Zagreb)H-Index: 1
#2Goran Poje (University of Zagreb)
Last. Zrinka Rajić (University of Zagreb)H-Index: 16
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Abstract null null The rise of the resistance of the malaria parasite to the currently approved therapy urges the discovery and development of new efficient agents. Previously we have demonstrated that harmicines, hybrid compounds composed from β-carboline alkaloid harmine and cinnamic acid derivatives, linked via either triazole or amide bond, exert significant antiplasmodial activity. In this paper, we report synthesis, antiplasmodial activity and cytotoxicity of expanded series of novel triaz...
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#1Qijie Gong (CPU: China Pharmaceutical University)H-Index: 2
#2Fulai Yang (CPU: China Pharmaceutical University)
Last. Xiaojin Zhang (CPU: China Pharmaceutical University)H-Index: 21
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Abstract null null Since NQO1 is overexpressed in many cancer cells, it can be used as a biomarker for cancer diagnosis and targeted therapy. NQO1 substrates show potent anticancer activity through the redox cycle mediated by NQO1, while the NQO1 probes can monitor NQO1 levels in cancers. High sensitivity of probes is needed for diagnostic imaging in clinic. In this study, based on the analysis of NQO1 catalytic pocket, the naphthoquinone trigger group 13 rationally designed by expanding the aro...
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#1Yu Nairong (CPU: China Pharmaceutical University)
#2Na Li (CPU: China Pharmaceutical University)H-Index: 6
Last. Li Chen (CPU: China Pharmaceutical University)H-Index: 12
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Abstract null null In this study, eleven new 3- and 7-positions modified scopoletin derivatives (18a-k) were designed, synthesized, and biologically evaluated against human breast cancer cell lines. Most compounds showed improved antiproliferative activity against MCF-7 and MDA-MB-231 cells and weaker cytotoxicity on human breast epithelial cell line MCF-10A than lead compound 5. Among them, compound 18e exhibited the most potent antiproliferative activity against MCF-7 cells (IC50 = 0.37 ± 0.05...
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#1Marina Petrenko (MLU: Martin Luther University of Halle-Wittenberg)H-Index: 3
#2Antje Güttler (MLU: Martin Luther University of Halle-Wittenberg)H-Index: 9
Last. René Csuk (MLU: Martin Luther University of Halle-Wittenberg)H-Index: 27
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Abstract null null Many pentacyclic triterpenoids show anti-cancer and anti-inflammatory properties. Recently, we detected a pronounced cytotoxicity and radiosensitivity of two betulinyl sulfamates in human breast cancer cells. Besides betulinic acid scaffold (BSBA-S), we synthesized several new sulfamate-coupled scaffolds from oleanolic acid (OSBA-S), ursolic acid (USBA-S), platanic acid (PSBA-S) and maslinic acid (MSBA-S). Highest cytotoxicity was monitored in breast cancer cell lines after MS...
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#1Dyhia Amrane (AMU: Aix-Marseille University)
#2Nicolas Primas (AMU: Aix-Marseille University)H-Index: 7
Last. Dominique Mazier (University of Paris)H-Index: 57
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Abstract null null The identification of a plant-like Achille's Heel relict, i.e. the apicoplast, that is essential for Plasmodium spp., the causative agent of malaria lead to an attractive drug target for new antimalarials with original mechanism of action. Although it is not photosynthetic, the apicoplast retains several anabolic pathways that are indispensable for the parasite. Based on previously identified antiplasmodial hit-molecules belonging to the 2-trichloromethylquinazoline and 3-tric...
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#1Jin Li (Sichuan University)
#2Lu Feng (Sichuan University)H-Index: 1
Last. Guan Wang (Sichuan University)H-Index: 8
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Abstract null null Tyrosinase is a copper-containing metalloenzyme that is responsible for the rate-limiting catalytic step in the melanin biosynthesis and enzymatic browning. As a promising target, tyrosinase inhibitors can be used as skin whitening agents and food preservatives, thus having broad potential in the fields of food, cosmetics, agriculture and medicine. From 2015 to 2020, numerous synthetic inhibitors of tyrosinase have been developed to overcome the challenges of low efficacy and ...
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#1Tian-Tian Lu (CAS: Chinese Academy of Sciences)
#2Yuna Shimadate (University of Toyama)H-Index: 1
Last. Chu-Yi Yu (CAS: Chinese Academy of Sciences)H-Index: 20
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Abstract null null 5-C-Alkyl-DNJ and 5-C-alkyl- l -ido-DNJ derivatives have been designed and synthesized efficiently from an null l -sorbose-derived cyclic nitrone. The DNJ and null l -ido-DNJ derivatives with C-5 alkyl chains ranging from methyl to dodecyl were assayed against various glycosidases to study the effect of chain length on enzyme inhibition. Glycosidase inhibition study of DNJ derivatives showed potent and selective inhibitions of α-glucosidase; DNJ derivatives with methyl, pentyl...
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