全部文献期刊会议图书|学者科研项目
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作者:Azizah M. Malebari , Darren Fayne , Seema M. Nathwani ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.189
摘要:Abstract(#br)A series of novel 1,4-diaryl-2-azetidinone analogues of combretastatin A-4 (CA-4) have been designed, synthesised and evaluated in vitro for antiproliferative activity, antiapoptotic activity and inhibition of tubulin polymerisation. Glucuronidation of CA-4 by u...
作者:Xin Chen , Xinyang Chen , Raphael R. Steimbach ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.187
摘要:Abstract(#br)Histone deacetylase 6 (HDAC6) has gained popular attention for its wide participation in various pathological process recently. In this paper, a series of novel derivatives containing 2, 5-diketopiperazine (DKP) skeleton were developed as potent selective HDAC6 ...
作者:Stephanie Federico , Enrico Margiotta , Stefano Moro ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.186
摘要:Abstract(#br)Compounds able to simultaneously bind a biological target and be conjugated to a second specific moiety are attractive tools for the development of multi-purpose ligands useful as multi-target ligands, receptor probes or drug delivery systems, with both therapeutic a...
作者:Hilal Doğan , Şengül Dilem Doğan , Miyase Gözde Gündüz ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.188
摘要:Abstract(#br)Tuberculosis, caused by Mycobacterium tuberculosis , is a serious infectious disease and remains a global health problem. There is an increasing need for the discovery of novel therapeutic agents for its treatment due to the emerging multi-drug resistance. Herei...
作者:Qi Li , Shuaishuai Xing , Ying Chen ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.185
摘要:Abstract(#br)Neurodegenerative diseases are a variety of debilitating and fatal disorder in central nervous system (CNS). Besides targeting neuronal activity by influencing neurotransmitters or their corresponding receptors, modulating the underlying processes that lead to cell d...
作者:Hao Lei , Shu Fan , Hao Zhang ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.186
摘要:Abstract(#br)Targeting L858R/T790M/C797S mutant EGFR is a major challenge in the new-generation EGFR tyrosine kinase inhibitors development for conquering drug resistant NSCLC. In this study, a series of novel 9-heterocyclyl substituted 9 H -purine derivatives were designed ...
作者:Omneya M. Khalil , Aliaa M. Kamal , Silvia Bua ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.188
摘要:Abstract(#br)A series of novel sulfonamide derivatives bearing pyrrole and pyrrolopyrimidine scaffolds were synthesized and screened as carbonic anhydrase inhibitors. The inhibition activity of the synthesized compounds was evaluated against the cytosolic human carbonic anhydrase...
作者:Katarzyna Malarz , Dawid Zych , Michał Kuczak ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.189
摘要:Abstract(#br)Terpyridine complexes are known for their broad biological activities, of which their anticancer potency is the most extensively studied. Strikingly, free ligand activity has rarely been described in the literature. In this study, a lipophilic derivative of terp...
作者:Wenting Zhao , Bin Wang , Yuke Liu ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2020, Vol.189
摘要:Abstract(#br)A series of 4 H -chromen-4-one derivatives obtained by scaffold morphing of the benzofuran compound, TAM16, were tested for antitubercular activity. Compound 8d was active against drug-sensitive and multidrug-resistant tuberculosis. A preliminary druggability evaluat...

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