European Journal of Medicinal Chemistry
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Abstract null null Adenosine is an endogenous purine-based nucleoside expressed nearly in all body tissues. It regulates various body functions by activating four G-protein coupled receptors, A1, A2A, A2B, and A3. These receptors are widely acknowledged as drug targets for treating different neurological, metabolic, and inflammatory diseases. Although numerous adenosine receptor inhibitors have been developed worldwide, achieving target selectivity is still a big hurdle in drug development. Howe...
#1Beier Jiang (SMMU: Second Military Medical University)H-Index: 2
#2Jiaxin Hu (ECNU: East China Normal University)
Last. Li-Fang Yu (ECNU: East China Normal University)H-Index: 17
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Abstract null null The equilibrium between histone acetylation and deacetylation plays an important role in cancer initiation and progression. The histone deacetylases (HDACs) are a class of key regulators of gene expression that enzymatically remove an acetyl moiety from acetylated lysine e-amino groups on histone tails. Therefore, HDAC inhibitors have recently emerged as a promising strategy for cancer therapy and several pan-HDAC inhibitors have globally been approved for clinical use. In the...
#1Chao Wang (Qingdao University)H-Index: 3
#2Yujing Zhang (Qingdao University)H-Index: 2
Last. Dongming Xing (THU: Tsinghua University)H-Index: 10
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Abstract null null Proteolysis targeting chimeras (PROTACs), which hijack proteins of interest (POIs) and recruit E3 ligases for target degradation via the ubiquitin-proteasome pathway, are a novel drug discovery paradigm that has been widely used as biological tools and medicinal molecules with the potential of clinical application value. To date, a wide variety of small molecule PROTACs have been developed. Importantly, VHL-based PROTACs have emerged to be a promising approach for proteins, in...
#1Stefan Schiesser (AstraZeneca)H-Index: 10
#2Peter Hajek (AstraZeneca)
Last. Cox Rhona Jane (AstraZeneca)H-Index: 10
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Abstract null null Inhibition of mucosa-associated lymphoid tissue lymphoma translocation protein-1 (MALT1) is a promising strategy to modulate NF-κB signaling, with the potential to treat B-cell lymphoma and autoimmune diseases. We describe the discovery and optimization of (1s,4s)-N,N′-diaryl cyclohexane-1,4-diamines, a novel series of allosteric MALT1 inhibitors, resulting in compound 8 with single digit micromolar cell potency. X-ray analysis confirms that this compound binds to an induced a...
#1Yu Jiang (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)H-Index: 1
#2Lingling Luo (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)
Last. Tiemin Sun (SPU: Shenyang Pharmaceutical University)H-Index: 1
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Abstract null null The poly (ADP-ribose) polymerase (PARP) inhibitors play a crucial role in cancer therapy. However, most approved PARP inhibitors have lower selectivity to PARP-1 than to PARP-2, so they will inevitably have side effects. Based on the different catalytic domains of PARP-1 and PARP-2, we developed a strategy to design and synthesize highly selective PARP-1 inhibitors. Compounds Y17, Y29, Y31 and Y49 showed excellent PARP-1 inhibition, and their IC50 values were 0.61, 0.66, 0.41 ...
#1Xingrui He (Hunan University of Science and Engineering)H-Index: 1
#1Xingrui HeH-Index: 2
Last. Xiang-Yang Ye (Hangzhou Normal University)H-Index: 3
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Abstract null null Epigentic enzymes histone deacetylases (HDACs) catalyze the removal of acetyl groups from the e-N-acetylated lysine residues of various protein substrates including both histone and non-histone proteins. Different HDACs have distinct biological functions and are recruited to specific regions of the genome. Due to their important biological functions, HDACs have been validated in clinics for anticancer therapy, and are being explored for potential treatment of several other dis...
#1Xue Bai (Inner Mongolia University)H-Index: 1
#2Amjad Ali (ECNU: East China Normal University)H-Index: 16
Last. Faiz-Ur Rahman (Inner Mongolia University)H-Index: 1
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Abstract null null Cancer is one of the most aggressive diseases with poor prognosis and survival rates. Lipids biogenesis play key role in cancer progression, metastasis and tumor development. Suppression of SREBP-mediated lipid biogenesis pathway has been linked with cancer inhibition. Platinum complexes bearing good anticancer effect and multiple genes activation properties are considered important and increase the chances for development of new platinum-based drugs. In this study, we synthes...
#1Bing Zhang (SPU: Shenyang Pharmaceutical University)H-Index: 4
#2Yulin Duan (SPU: Shenyang Pharmaceutical University)H-Index: 2
Last. Jinxin Li (SPU: Shenyang Pharmaceutical University)
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Abstract null null Xanthine oxidase (XO) has been an important target for the treatment of hyperuricemia and gout. The analysis of potential interactions of pyrimidinone and 3-cyano indole pharmacophores present in the corresponding reported XO inhibitors with parts of the XO active pocket indicated that they both can be used as effective fragments for the fragment-based design of nonpurine XO inhibitors. In this paper, we adopted the fragment-based drug design strategy to link the two fragments...
#1Ling Wang (HUST: Huazhong University of Science and Technology)
#2Danya Zhang (HUST: Huazhong University of Science and Technology)
Last. Ling Xi (HUST: Huazhong University of Science and Technology)H-Index: 22
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Abstract null null TMTP1 is a polypeptide independently screened in our laboratory, which can target tumors in situ and metastases. In previous work, we have successfully developed a near-infrared (NIR) probe TMTP1-PEG4-ICG for tumor imaging. However, the limited ability to target tumor micrometastases hinders its further clinical application. Multimerization of peptides has been extensively demonstrated as an effective strategy to increase receptor binding affinity due to “multivalent effect” o...
#1Arya C G (NITC: National Institute of Technology Calicut)
#2Ramesh Gondru (ICMR: Indian Council of Medical Research)H-Index: 6
Last. Janardhan Banothu (NITC: National Institute of Technology Calicut)H-Index: 11
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Abstract null null Coumarin and benzimidazole are privileged structures in medicinal chemistry and are widely used in drug discovery and development due to their vast biological properties. The pharmacokinetic and pharmacodynamic properties of the individual scaffolds can be improved by developing coumarin–benzimidazole chimeric molecules via molecular hybridization approach. The three major classes of coumarin–benzimidazole hybrids are merged, fused and spacer-linked hybrids. Depending on the s...
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