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European Journal of Medicinal Chemistry

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https://www.readbyqxmd.com/read/28814374/from-bench-laboratory-to-bed-hospital-home-how-to-explore-effective-natural-and-synthetic-pak1-blockers-longevity-promoters-for-cancer-therapy
#1
REVIEW
Hiroshi Maruta, Mok-Ryeon Ahn
PAK family kinases are RAC/CDC42-activated kinases that were first found in a soil amoeba 4 decades ago, and 2 decades later, were discovered in mammals as well. Since then at least 6 members of this family have been identified in mammals. One of them called PAK1 has been best studied so far, mainly because it is essential not only for malignant cell growth and metastasis, but also for many other diseases/disorders such as diabetes (type 2), AD (Alzheimer's disease), hypertension, and a variety of inflammatory or infectious diseases, which definitely shorten our lifespan...
August 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28810191/structure-function-studies-of-bpp-brachynh2-and-synthetic-analogues-thereof-with-angiotensin-i-converting-enzyme
#2
Daniel D R Arcanjo, Andreanne G Vasconcelos, Lucas A Nascimento, Ana Carolina Mafud, Alexandra Plácido, Michel M M Alves, Cristina Delerue-Matos, Marcelo P Bemquerer, Nuno Vale, Paula Gomes, Eduardo B Oliveira, Francisco C A Lima, Yvonne P Mascarenhas, Fernando Aécio A Carvalho, Ulf Simonsen, Ricardo M Ramos, José Roberto S A Leite
The vasoactive proline-rich oligopeptide termed BPP-BrachyNH2 (H-WPPPKVSP-NH2) induces in vitro inhibitory activity of angiotensin I-converting enzyme (ACE) in rat blood serum. In the present study, the removal of N-terminal tryptophan or C-terminal proline from BPP-BrachyNH2 was investigated in order to predict which structural components are important or required for interaction with ACE. Furthermore, the toxicological profile was assessed by in silico prediction and in vitro MTT assay. Two BPP-BrachyNH2 analogues (des-Trp(1)-BPP-BrachyNH2 and des-Pro(8)-BPP-BrachyNH2) were synthesized, and in vitro and in silico ACE inhibitory activity and toxicological profile were assessed...
August 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28810190/design-synthesis-and-biological-evaluation-of-novel-2-methoxyestradiol-analogs-as-dual-selective-estrogen-receptor-modulators-serms-and-antiangiogenic-agents
#3
Kejing Lao, Yejun Wang, Mingqi Chen, Jingjing Zhang, Qidong You, Hua Xiang
2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-proliferative activities against 5 different cell lines. The results indicated that most compounds exhibited good activities, in which compound 24c and 30c showed the best activity with low micromolar IC50 (2.73 μM -7...
August 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802123/clathrodin-hymenidin-and-oroidin-and-their-synthetic-analogues-as-inhibitors-of-the-voltage-gated-potassium-channels
#4
Nace Zidar, Aleš Žula, Tihomir Tomašič, Marc Rogers, Robert W Kirby, Jan Tytgat, Steve Peigneur, Danijel Kikelj, Janez Ilaš, Lucija Peterlin Mašič
We have prepared three alkaloids from the Agelas sponges, clathrodin, hymenidin and oroidin, and a series of their synthetic analogues, and evaluated their inhibitory effect against six isoforms of the Kv1 subfamily of voltage-gated potassium channels, Kv1.1-Kv1.6, expressed in Chinese Hamster ovary (CHO) cells using automated patch clamp electrophysiology assay. The most potent inhibitor was the (E)-N-(3-(2-amino-1H-imidazol-4-yl)allyl)-4,5-dichloro-1H-pyrrole-2-carboxamide (6g) with IC50 values between 1...
August 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28810188/novel-tacrine-derivatives-exhibiting-improved-acetylcholinesterase-inhibition-design-synthesis-and-biological-evaluation
#5
Eeda Koti Reddy, Chandran Remya, Kumar Mantosh, Ayyiliath M Sajith, R V Omkumar, C Sadasivan, Shaik Anwar
A novel series of twenty four tacrine derivatives were designed and synthesised. Among these, thirteen were taken for the acetylcholinesterase (AChE) inhibition studies. Three compounds such as 4c, 6c and 6f were found to possess significant AChE inhibitory properties with IC50 values 12.97 ± 0.47 nM, 5.17 ± 0.24 nM and 7.14 ± 0.78 nM respectively. In silico docking studies revealed that these compounds can bind strongly in the active site of the enzyme and prevent enzyme-substrate interactions...
August 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28803677/indole-fused-azepines-and-analogues-as-anticancer-lead-molecules-privileged-findings-and-future-directions
#6
REVIEW
Ashok K Singh, Vinit Raj, Sudipta Saha
The search for new lead compounds of simple structure, displaying highest quality anti-tumor potency with new mechanisms of action and least adverse effects is the major intention of cancer drug discovery now a days. For the time being, indole-fused azepines emerged as a simple class of compounds prolifically designed with strong pharmacological significances in particular of cancer protecting ability. In the recent years from the efforts of our research group, indole-fused heteroazepines, a simple structural class achieved by fusion of indole with oxygen, sulphur and nitrogen containing heteroazepine rings, have known for its superior outcomes in cancer treatment...
August 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802482/recent-advances-on-cdk-inhibitors-an-insight-by-means-of-in-silico-methods
#7
REVIEW
Marco Tutone, Anna Maria Almerico
The cyclin dependent kinases (CDKs) are a small family of serine/threonine protein kinases that can act as a potential therapeutic target in several proliferative diseases, including cancer. This short review is a survey on the more recent research progresses in the field achieved by using in silico methods. All the "armamentarium" available to the medicinal chemists (docking protocols and molecular dynamics, fragment-based, de novo design, virtual screening, and QSAR) has been employed to the discovery of new, potent, and selective inhibitors of cyclin dependent kinases...
August 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802120/discovery-of-pentacyclic-triterpene-3%C3%AE-ester-derivatives-as-a-new-class-of-cholesterol-ester-transfer-protein-inhibitors
#8
Dongyin Chen, Xin Huang, Hongwen Zhou, Hanqiong Luo, Pengfei Wang, Yongzhi Chang, Xinyi He, Suiying Ni, Qingqing Shen, Guoshen Cao, Hongbin Sun, Xiaoan Wen, Jun Liu
A series of pentacyclic triterpene 3β-ester derivatives were designed, synthesized and evaluated as a new class of cholesteryl ester transfer protein (CETP) inhibitors for the treatment of dyslipidemia. In vitro screening assay showed that 5 out of 30 compounds displayed moderate inhibiting human CETP activity with IC50s less than 10 μM. Among them, compound 20 (IC50 = 2.3 μM) had the most potent biological activity, and effectively ameliorated plasma lipid levels of human adipose tissue specific CETP transgenic (ap2-CETPTg) mice and guinea pigs...
August 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800460/synthesis-and-biological-evaluation-of-4-biphenylamino-5-halo-2-5h-furanones-as-potential-anticancer-agents
#9
Yan-Cheng Wu, Shi-He Luo, Wen-Jie Mei, Liang Cao, Han-Qing Wu, Zhao-Yang Wang
An efficient route without metal catalyst has been developed for synthesis of 4-biphenylamino-5-halo-2(5H)-furanones. The antitumor activities against various tumor cells of all the compounds have been evaluated by MTT assay. Among them, the compound 3j exhibits significant inhibitory activity against MCF-7 human breast cancer cells with an IC50 value of 11.8 μM and low toxicity toward HaCaT human normal cells. The mechanism studies confirm that 3j can induce cell cycle arrest at G2/M phase in MCF-7 cells...
August 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28803048/novel-unsaturated-glycyrrhetic-acids-derivatives-design-synthesis-and-anti-inflammatory-activity
#10
Bo Li, Shi Cai, Yong-An Yang, Shi-Chao Chen, Rui Chen, Jing-Bo Shi, Xin-Hua Liu, Wen-Jian Tang
To develop novel anti-inflammatory agents, a series of unsaturated glycyrrhetic acids were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. The structure-activity relationship (SAR) of NO inhibitory activity was analyzed. α,β-Unsaturated glycyrrhetic acids showed better activity, among them, compounds 6k and 6l with piperazine unit exhibited the most potent nitric oxide (NO) and interleukin-6 (IL-6) inhibitory activity (IC50 = 13.3 and 15.5 μM respectively). Furthermore, compound 6k could also significantly suppress LPS-induced iNOS and COX-2 expression and IL-6 production through MAPKs and NF-kB signaling pathway...
August 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802121/identification-of-highly-potent-n-acylethanolamine-acid-amidase-naaa-inhibitors-optimization-of-the-terminal-phenyl-moiety-of-oxazolidone-derivatives
#11
Yuhang Li, Qi Chen, Longhe Yang, Yanting Li, Yang Zhang, Yan Qiu, Jie Ren, Canzhong Lu
N-acylethanolamine acid amidase (NAAA) is a cysteine hydrolase that participates in the deactivation of fatty acid ethanolamides, such as palmitoylethanolamide (PEA). NAAA inhibition may provide a potential therapeutic strategy for the treatment of diseases in which higher PEA level is desired. In the present study, we reported the structure-activity relationship (SAR) studies for oxazolidone derivatives as NAAA inhibitors. A series of substituents or alkyl replacements for the terminal phenyl ring of oxazolidone derivatives were examined...
August 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28797675/from-the-hive-honey-a-novel-weapon-against-cancer
#12
REVIEW
Mariateresa Badolato, Gabriele Carullo, Erika Cione, Francesca Aiello, Maria Cristina Caroleo
Nowadays there is a folk medicine branch called apitherapy that aims to treat diseases with bee products, including honey. Honey has long been known for its medicinal and health promoting properties. It encloses numerous types of phytochemicals with high phenolic and flavonoid content, which contribute to its antioxidant and anti-inflammatory activities. Varieties and variants of polyphenols in honey showed antiproliferative property against several types of cancer. This review focuses on the latest discoveries about the key role of honey in different stages of carcinogenesis, initiation, proliferation and progression, both in vitro and in vivo, as well as on its adjuvant effect in cancer therapy...
August 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802122/piperlongumine-b-and-analogs-are-promising-and-selective-inhibitors-for-acetylcholinesterase
#13
Jana Wiemann, Julia Karasch, Anne Loesche, Lucie Heller, Wolfgang Brandt, René Csuk
Piperlongumine B (19), an alkaloid previously isolated from long pepper (Piper longum) has been synthesized for the first time in a short sequence and in good yield together with 19 analogs. Screening of these compounds in Ellman's assays showed several of them to be good inhibitors of acetylcholinesterase while being less active for butyrylcholinesterase. Activity of the compounds increased with the ring size of the heterocycle, and a maximum of activity was observed for an analog holding 12 methylene groups in the aliphatic side chain...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800871/malignant-pleural-mesothelioma-state-of-the-art-and-advanced-cell-therapy
#14
Giorgio Facchetti, Francesco Petrella, Lorenzo Spaggiari, Isabella Rimoldi
Malignant Pleural Mesothelioma (MPM) is an aggressive malignancy highly resistant to chemotherapy, with a response rate of 20% of patients and for this reason an efficient treatment is still a challenge. Platinum-based chemotherapy in association with a third-generation antifolate is the front-line standard of care whereas any second-line treatment was approved for MPM thus making it a pathology that evokes the need for new therapeutic agents. Different platinum-drugs were synthesised and tested as an option for patients who are not candidates to cisplatin-based therapy...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800451/synthesis-antimicrobial-dna-cleavage-and-antioxidant-activities-of-tricyclic-sultams-derived-from-saccharin
#15
Ibrahim Elghamry, Magdy M Youssef, Mohammed A Al-Omair, Hany Elsawy
Two series of fused tricyclic sultams (carboxylates, 3a, b and 5a, f, g and anilides 5b-e) were synthesized from saccharin and their chemical structures were confirmed by spectroscopic tools. Then, their antibacterial activities and MIC were evaluated against two strains of gram positive and gram-negative bacteria. The MIC values of the tested compounds are in the of range 8-33 μg/ml. In addition, their DNA cleavage ability, binding affinity and their anticancer activities against hepatic cancer cell were tested...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28797884/drifting-of-heme-coordinating-group-in-imidazolylmethylxanthones-leading-to-improved-selective-inhibition-of-cyp11b1
#16
Silvia Gobbi, Qingzhong Hu, Christina Zimmer, Federica Belluti, Angela Rampa, Rolf W Hartmann, Alessandra Bisi
An abnormal increase in glucocorticoid levels is responsible for pathological disorders affecting different organs and systems, and the selective inhibition of appropriate steroidogenic enzymes represents a validated strategy to restore their physiological levels. In continuing our studies on CYP11B inhibitors, in this paper a small series of 6-substituted 3-imidazolylmethylxanthones was designed and synthesized, according to the data acquired from previously reported series of derivatives and from a purposely-performed docking study...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802125/novel-4-3-4-oxo-5-2-oxoindolin-3-ylidene-thiazolidin-2-ylidene-amino-benzenesulfonamides-synthesis-carbonic-anhydrase-inhibitory-activity-anticancer-activity-and-molecular-modelling-studies
#17
Wagdy M Eldehna, Mahmoud F Abo-Ashour, Alessio Nocentini, Paola Gratteri, Ibrahim H Eissa, Mohamed Fares, Omnia E Ismael, Hazem A Ghabbour, Mahmoud M Elaasser, Hatem A Abdel-Aziz, Claudiu T Supuran
Herein we report the synthesis of two series of novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino)benzenesulfonamides (4a-m and 7a-g). All the newly prepared sulfonamides were in vitro investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I, II, IV and IX, using a stopped-flow CO2 hydrase assay. In particular, hCA isoforms II and IX (tumor-associated) were more susceptible to inhibition by the synthesized derivatives, with KIs in the range of 2...
August 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800870/recent-advances-in-her2-positive-breast-cancer-epigenetics-susceptibility-and-therapeutic-strategies
#18
REVIEW
Heena Singla, Abhilash Ludhiadch, Raman Preet Kaur, Harish Chander, Vinod Kumar, Anjana Munshi
HER2 amplification/overexpression accounts for aggressive clinical features of HER2 positive breast cancer. Epigenetic changes including DNA methylation, histone modifications and ncRNAs/miRNAs are associated with regulation of DNA chromatin and specifically, gene transcription. Hence, these produce eminent effects upon proto-oncogenes, tumor-suppressors and key cancer-regulatory signaling pathways. Understanding of epigenomic regulation of HER2 overexpression and signaling may help uncover the unmatchable physiology of HER2 gene/protein...
August 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800461/design-synthesis-and-biological-evaluation-of-novel-3-substituted-imidazo-1-2-a-pyridine-and-quinazolin-4-3h-one-derivatives-as-pi3k%C3%AE-inhibitors
#19
Yan-Hua Fan, Wei Li, Dan-Dan Liu, Meng-Xuan Bai, Hong-Rui Song, Yong-Nan Xu, SangKook Lee, Zhi-Peng Zhou, Jian Wang, Huai-Wei Ding
Phosphatidylinositol 3-kinase (PI3K) is a pivotal regulator of intracellular signaling pathways and considered as a promising target in the development of a therapeutic treatment of cancer. Among the different PI3K subtypes, the PIK3CA gene encoding PI3K p110α is frequently mutated and overexpressed in majority of human cancers. Therefore, the inhibition of PI3Kα has been considered to be an efficient approach for the treatment of cancer. In this study, two series compounds containing hydrophilic group in imidazo[1,2-a]pyridine and quinazolin-4(3H)-one were synthesized and their antiproliferative activities against five cancer cell lines, including HCT-116, SK-HEP-1, MDA-MB-231, SNU638 and A549, were evaluated...
August 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800459/novel-cinnamamide-dibenzylamine-hybrids-potent-neurogenic-agents-with-antioxidant-cholinergic-and-neuroprotective-properties-as-innovative-drugs-for-alzheimer-s-disease
#20
Jin Wang, Pei Cai, Xue-Lian Yang, Fan Li, Jia-Jia Wu, Ling-Yi Kong, Xiao-Bing Wang
By using fragments endowed with interesting and complementary properties for the treatment of Alzheimer's disease (AD), a novel series of cinnamamide-dibenzylamine hybrids have been designed, synthesized, and evaluated biologically. In vitro assay indicated that most of the target compounds exhibited a significant ability to inhibit ChEs, strong potency inhibitory of self-induced β-amyloid (Aβ) aggregation and to act as potential antioxidants and biometal chelators. A Lineweaver-Burk plot and molecular modeling study showed that compound 7f targeted both the CAS and PAS of AChE...
August 1, 2017: European Journal of Medicinal Chemistry
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