Full Text Journal Articles in
Journal Eur J Med Chem

Advertisement

Find full text journal articles






In silico screening-based discovery of novel covalent inhibitors of the SARS-CoV-2 3CL protease

Muya Xiong, Tianqing Nie, Qiang Shao, Minjun Li, Haixia Su, Yechun Xu,

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL protease (3CLpro) has been regarded as an extremely promising antiviral target for the treatment of coronavirus disease 2019 (COVID-19). Here, we carried out a virtual screening based on commercial compounds database to find novel covalent non-peptidomimetic inhibitors of this protease. It ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, :]

Cited: 0 times

View full text PDF listing >>



Unraveling the anti-virulence potential and antifungal efficacy of 5-aminotetrazoles using the zebrafish model of disseminated candidiasis.

Natasa Radakovic, Andrea Nikolić, Nataša Terzić Jovanović, Pavle Stojković, Nada Stankovic, Bogdan Šolaja, Igor Opsenica, Aleksandar Pavic,

Candida albicans remains the main causal agent of candidiasis, the most common fungal infection with disturbingly high mortality rates worldwide. The limited diversity and efficacy of clinical antifungal drugs, exacerbated by emerging drug resistance, have resulted in the failure of current antifungal therapies. This imposes an urgent demand for the ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114137]

Cited: 0 times

View full text PDF listing >>



Advertisement

Corrigendum to <'Design, synthesis and biological evaluation of novel peptides with anti-cancer and drug resistance-reversing activities'><[European Journal of Medicinal Chemistry, 89 (2015) 540-548]>.

Xin Deng, Qianqian Qiu, Baowei Yang, Xuekun Wang, Wenlong Huang, Hai Qian,

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114107]

Cited: 0 times

View full text PDF listing >>



Discovery of small-molecule fluorescent probes for C-Met.

Dong Liang, Chen Yu, Xiaojun Qin, Xingye Yang, Xuhui Dong, Mingzhao Hu, Lupei Du, Minyong Li,

C-mesenchymal-epithelia transition factor (c-Met) is highly expressed in various solid tumors such as gastric cancer, liver cancer, and lung cancer, playing a pivotal role in the growth, maintenance, and development of different tumor cells. In this study, three small-molecule fluorescent probes (5, 11, 16) targeting c-Met were developed, and their ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114114]

Cited: 0 times

View full text PDF listing >>



Synthesis of tropane-based σ1 receptor antagonists with antiallodynic activity.

Elena Bechthold, Julian A Schreiber, Nadine Ritter, Lucie Grey, Dirk Schepmann, Constantin Daniliuc, Rafael González-Cano, Francisco Rafael Nieto, Guiscard Seebohm, Bernhard Wünsch,

Following the concept of conformational restriction to obtain high affinity σ<sub>1</sub> ligands, the piperidine ring of eliprodil was replaced by the bicyclic tropane system and an exocyclic double bond was introduced. The envisaged benzylidenetropanes 9 were prepared by conversion of tropanone 10 into the racemic mixture of (Z)-14 and (E)-14. ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114113]

Cited: 0 times

View full text PDF listing >>



Tetrazole derivatives bearing benzodiazepine moiety-synthesis and action mode against virulence of Candida albicans.

M Staniszewska, T Zdrojewski, M Gizińska, M Rogalska, Ł Kuryk, A Kowalkowska, E Łukowska-Chojnacka,

Tetrazole and benzodiazepine derivatives attract widespread attention due to their remarkable pharmaceutical potential. 5-(2-bromophenyl)-7-fluoro-1-[3-(5-(4-chlorophenyl)-2H-tetrazol-2-yl)propyl]-1,3-dihydro-2H-1,4-benzodiazepin-2-one (6c) and 5-(2-bromophenyl)-7-fluoro-1-[3-(5-(2-chlorophenyl)-2H-tetrazol-2-yl)propyl]-1,3-dihydro-2H-1,4-benzodiazepin-2-one (6d) were selected using the microdilution approach and because of their preferential fungicidal activity toward C. albicans. 6c or 6d altered the hyphal morphology, chitin deposition and membrane permeation in planktonic and sessile cells. ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114060]

Cited: 0 times

View full text PDF listing >>



Niemann-Pick C1-Like 1 inhibitors for reducing cholesterol absorption.

Renshuai Zhang, Wenjing Liu, Jun Zeng, Jingsen Meng, Hongfei Jiang, Jie Wang, Dongming Xing,

Cholesterol is an important component of cell membrane. However, elevated level of serum cholesterol is a key risk factor for heart disease. Niemann-Pick C1-Like 1 (NPC1L1) is the crucial target involving in cholesterol cellar uptake. Ezetimibe is the first, and only, NPC1L1 inhibitor approved for the treatment of hypercholesterolemia through ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114111]

Cited: 0 times

View full text PDF listing >>



Discovery of small molecules interacting at lactate dehydrogenases tetrameric interface using a biophysical screening cascade.

Léopold Thabault, Chiara Brustenga, Perrine Savoyen, Mégane Van Gysel, Johan Wouters, Pierre Sonveaux, Raphaël Frédérick, Maxime Liberelle,

Lactate dehydrogenases (LDHs) are tetrameric enzymes of therapeutic relevance for cancer therapy due to their important implications in cancer cell metabolism. LDH active site inhibition suffers from different drawbacks due to several features such as high cellular concentration and a shared active site among the dehydrogenase family. Conversely, targeting the ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114102]

Cited: 0 times

View full text PDF listing >>



Roles and drug development of METTL3 (methyltransferase-like 3) in anti-tumor therapy.

Pengfei Xu, Raoling Ge,

Methyltransferase complex, such as METTL3/METTL14/WTP, catalyze N<sup>6</sup>-methyladenosine (m<sup>6</sup>A), which is the most abundant mRNA modification in mammals. Besides acting as a m<sup>6</sup>A methyltransferase, METTL3 also regulates mRNA translation and other biological processes. Studies have identified numerous roles and molecular mechanisms associated with METTL3 in multiple biological processes especially in tumors ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114118]

Cited: 0 times

View full text PDF listing >>



Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).

Youquan Xie, Yucheng Tian, Yuming Zhang, Zhisheng Zhang, Rui Chen, Mian Li, Jiawei Tang, Jinlei Bian, Zhiyu Li, Xi Xu,

Osteoporosis is a common disease in which the risk of fracture increases due to decreased bone mass and qualitative skeletal changes. Selective androgen receptor modulators (SARMs) are agonists with tissue selectivity, which act as partial or weak androgen receptor (AR) agonists in androgenic tissues, but mainly as complete AR agonists ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114119]

Cited: 0 times

View full text PDF listing >>



Natural products from mangrove sediments-derived microbes: Structural diversity, bioactivities, biosynthesis, and total synthesis.

Kunlong Li, Siqiang Chen, Xiaoyan Pang, Jian Cai, Xinya Zhang, Yonghong Liu, Yiguang Zhu, Xuefeng Zhou,

The mangrove forests are a complex ecosystem, and the microbial communities in mangrove sediments play a critical role in the biogeochemical cycles of mangrove ecosystems. Mangrove sediments-derived microbes (MSM), as a rich reservoir of natural product diversity, could be utilized in the exploration of new antibiotics or drugs. To understand ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114117]

Cited: 0 times

View full text PDF listing >>



Tumor-microenvironmental-response Bi-functional molecules for efficient imaging and anti-tumor activity therapy.

Jin Wang, Ru Si, Qingqing Zhang, Xiaoyan Pan, Jie Zhang,

To improve the visualization and potency of anticancer agents, the diagnosis and treatment integration bi-functional molecules were constructed based on active candidate BD7, approved drug Linifanib, and monoclonal antibody Bevacizumab. Commercial available Rhodamine B was inducted to realize imaging-aided diagnosis and target efficiency monitoring for cancer cells. In order to ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114120]

Cited: 0 times

View full text PDF listing >>



Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors.

Kai Tang, Min Zhao, Ya-Hong Wu, Qiong Wu, Shu Wang, Yu Dong, Bin Yu, Yihui Song, Hong-Min Liu,

Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) encoded by the proto-oncogene PTPN11 is the first identified non-receptor protein tyrosine phosphatase. SHP2 dysregulation contributes to the pathogenesis of different cancers, making SHP2 a promising therapeutic target for cancer therapy. In this article, we report the structure-guided design based on the well-characterized ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114106]

Cited: 0 times

View full text PDF listing >>



Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.

Binbin Cheng, Wei Pan, Yi Xing, Yao Xiao, Jianjun Chen, Zheng Xu,

DDR (DNA damage response) defects in cells drive tumor formation by promoting DNA mutations, which also provides cancer-specific vulnerabilities that can be targeted by synthetic lethality-based therapies. Until now, PARP inhibitors like olaparib are the first successful case of utilizing synthetic lethality-based therapy to treat cancers with DNA-repairing deficiency (e.g. ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114109]

Cited: 0 times

View full text PDF listing >>



A new strategy for hit generation: Novel in cellulo active inhibitors of CYP121A1 from Mycobacterium tuberculosis via a combined X-ray crystallographic and phenotypic screening approach (XP screen).

Martyn Frederickson, Irwin R Selvam, Dimitrios Evangelopoulos, Kirsty J McLean, Mona M Katariya, Richard B Tunnicliffe, Bethany Campbell, Madeline E Kavanagh, Sitthivut Charoensutthivarakul, Richard T Blankley, Colin W Levy, Luiz Pedro S de Carvalho, David Leys, Andrew W Munro, Anthony G Coyne, Chris Abell,

There is a pressing need for new drugs against tuberculosis (TB) to combat the growing resistance to current antituberculars. Herein a novel strategy is described for hit generation against promising TB targets involving X-ray crystallographic screening in combination with phenotypic screening. This combined approach (XP Screen) affords both a validation ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114105]

Cited: 0 times

View full text PDF listing >>



Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.

Huiqiang Wei, Wenfeng Gou, Jun Gao, Hongxin Ning, Yang Song, Deguan Li, Yong Qin, Wenbin Hou, Yiliang Li,

Acute kidney injury (AKI) is associated with high morbidity and mortality. Cisplatin is a common chemotherapeutic, but its nephrotoxicity-driven AKI limits its clinical application. Currently, there are no specific and satisfactory therapies in the clinic for AKI. Inhibitors of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2) or histone deacetylase (HDACs) had ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114115]

Cited: 0 times

View full text PDF listing >>



Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents.

Xin Huang, Yu-Shuang Wang, Duo Ma, Yuan-Yuan Wang, Shi-Da Bian, Bo Zhang, Yu Qiao, Zi-Ran He, Meng Lv, Guo-Long Cai, Zi-Xuan Wang, Xue-Song Liu, Jing-Bo Shi, Ming-Ming Liu,

Hybridization of nitric oxide (NO) donors with known anti-cancer agents have been emerged as a strategy to achieve improved therapeutic effect and to overcome chemo-resistance in cancer therapy. In this study, furoxan moiety as an efficient NO donor was introduced to phenstatin, a microtubule-interfering agent (MIA), leading to the design ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114112]

Cited: 0 times

View full text PDF listing >>



Synthesis and biological application of glyco- and peptide derivatives of fullerene C60.

Lisa Tanzi, Marco Terreni, Yongmin Zhang,

Fullerenes have attracted considerable attention for their possible use in human therapy. Pure C<sub>60</sub> is soluble only in some organic solvents, but this could be overcome by chemical modifications. This review investigates the derivatization strategies and biological applications of fullerene C<sub>60</sub> by using polar "active" molecules as sugars and amino ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114104]

Cited: 0 times

View full text PDF listing >>



Identification of novel xanthine oxidase inhibitors via virtual screening with enhanced characterization of molybdopterin binding groups.

Lu Zhang, Jinying Tian, Hanzeng Cheng, Yajun Yang, Ying Yang, Fei Ye, Zhiyan Xiao,

Xanthine oxidase (XO) is an important therapeutic target for the treatment of hyperuricemia and gout. A virtual screening strategy with enhanced characterization of the molybdopterin binding group (MBG) was applied for the identification of novel XO inhibitors. Briefly, a 3D QSAR pharmacophore with fragment recognition capability was constructed by setting ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114101]

Cited: 0 times

View full text PDF listing >>



Synthesis of 8-aminomorphans with high KOR affinity.

Hendrik Jonas, Daniele Aiello, Dirk Schepmann, Patrizia Diana, Bernhard Wünsch,

2-Azabicyclo[3.3.1]nonanes (morphans) with a (3,4-dichlorophenyl)acetyl group at 2-position and a pyrrolidino moiety at 8-position were designed as conformationally restricted analogs of piperidine-based KOR agonists. The synthesis started with 4-oxopiperidine-2-carboxylic acid comprising 13 reaction steps. At first the ketone 10 was transformed into diester 7 bearing a propionate side chain. Dieckmann ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114079]

Cited: 0 times

View full text PDF listing >>



Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease.

Yichun Shi, Heng Zhang, Qing Song, Guangjun Yu, Zhuoling Liu, Feng Zhong, Zhenghuai Tan, Xiuxiu Liu, Yong Deng,

Based on multitarget-directed ligands approach, through two rounds of screening, a series of 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives were designed, synthesized and evaluated as innovative multifunctional agents against Alzheimer's disease. In vitro biological assays indicated that most of the hybrids were endowed with great AChE inhibitory activity, excellent antioxidant activity and moderate Aβ<sub>1-42</sub> aggregation ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114098]

Cited: 0 times

View full text PDF listing >>



Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC.

Fang Yang, Yalei Wen, Chaofan Wang, Yuee Zhou, Yang Zhou, Zhi-Min Zhang, Tongzheng Liu, Xiaoyun Lu,

KRAS is the most frequently mutated oncogene and plays a predominant role in driving initiation and progression of multiple cancers. Attempts to degrade the oncogene KRAS<sup>G12C</sup> with PROTAC strategy have been considered as an alternative strategy to combate cancers. However, the irreversible PROTACs may compromise the substoichiometric activity to decrease ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114088]

Cited: 0 times

View full text PDF listing >>



Potential applications of clickable probes in EGFR activity visualization and prediction of EGFR-TKI therapy response for NSCLC patients.

Hui Deng, Qian Lei, Weidong Shang, Ying Li, Liyun Bi, Na Yang, Zhiyi Yu, Weimin Li,

The epithelial growth factor receptor (EGFR) is abnormally overexpressed on the cell surface of cancer cells and is strongly associated with cancer cell proliferation, migration, differentiation, apoptosis, and angiogenesis. Tools enabling the visualization of EGFR in a structure-function approach are highly desirable to predict EGFR mutations and guide EGFR tyrosine ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114100]

Cited: 0 times

View full text PDF listing >>



Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.

Maria Dichiara, Antonia Artacho-Cordón, Rita Turnaturi, Miriam Santos-Caballero, Rafael González-Cano, Lorella Pasquinucci, Carla Barbaraci, Isabel Rodríguez-Gómez, Manuel Gómez-Guzmán, Agostino Marrazzo, Enrique J Cobos, Emanuele Amata,

The development of σ<sub>1</sub> receptor antagonists hybridized with a H<sub>2</sub>S-donor is here reported. We aimed to obtain improved analgesic effects when compared to σ<sub>1</sub> receptor antagonists or H<sub>2</sub>S-donors alone. In an in vivo model of sensory hypersensitivity, thioamide 1a induced analgesia which was synergistically enhanced when associated with the σ<sub>1</sub> receptor ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114091]

Cited: 0 times

View full text PDF listing >>



Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.

Tianxiao Wu, Qiaohua Qin, Nian Liu, Chu Zhang, Ruicheng Lv, Wenbo Yin, Yin Sun, Yixiang Sun, Ruifeng Wang, Dongmei Zhao, Maosheng Cheng,

Tropomyosin receptor kinase (TRK) is an ideal target for treating cancers caused by the NTRK gene fusion. In this study, more than 60 2,4-diaminopyrimidine derivatives were prepared to understand the structure-activity relationship and confirm the rationality of the pharmacophore model reported previously. Among them, compound 19k was found to be ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2022, 230:114096]

Cited: 0 times

View full text PDF listing >>



Advertisement


Disclaimer

1.884 s