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Some effects of a chrysin bromide-derivative on GABA-A receptors and on Caenorhabditis elegans.

José Téllez-Arreola, Alejandro Valdez-Calderón, Simplicio González-Montiel, Ataúlfo Martinez-Torres, Adan Hernandez,

MicroPubl Biol (microPublication biology)
[2019, 2019:]

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Identification of histone deacetylase inhibitors with (arylidene)aminoxy scaffold active in uveal melanoma cell lines.

Susanna Nencetti, Doretta Cuffaro, Elisa Nuti, Lidia Ciccone, Armando Rossello, Marina Fabbi, Flavio Ballante, Gabriella Ortore, Grazia Carbotti, Francesco Campelli, Irene Banti, Rosaria Gangemi, Garland R Marshall, Elisabetta Orlandini,

Uveal melanoma (UM) represents an aggressive type of cancer and currently, there is no effective treatment for this metastatic disease. In the last years, histone deacetylase inhibitors (HDACIs) have been studied as a possible therapeutic treatment for UM, alone or in association with other chemotherapeutic agents. Here we synthesised a ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):34-47]

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Synthesis, biological activities and docking studies of pleuromutilin derivatives with piperazinyl urea linkage.

Yuanyuan Zhang, Chuan Xie, Yang Liu, Feng Shang, Rushiya Shao, Jing Yu, Chunxia Wu, Xinghui Yao, Dongfang Liu, Zhouyu Wang,

Antibiotics resistance is becoming increasingly common, involving almost all antibiotics on the market. Diseases caused by drug resistant bacteria, such as MRSA, have high mortality and negatively affect public health. The development of new drugs would be an effective means of solving this problem. Modifications based on bioactive natural products ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):764-775]

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Onopordopicrin from the new genus Shangwua as a novel thioredoxin reductase inhibitor to induce oxidative stress-mediated tumor cell apoptosis.

Junmin Zhang, Zai-Qin Zheng, Qianhe Xu, Ya Li, Kun Gao, Jianguo Fang,

Isolation and identification of natural products from plants is an essential approach for discovering drug candidates. Herein we report the characterization of three sesquiterpene lactones from a new genus <i>Shangwua</i>, e.g. onopordopicrin (ONP), C<b>2</b>, and C<b>3</b>, and evaluation of their pharmacological functions in interfering cellular redox signaling. Compared to C<b>2</b> ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):790-801]

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Synthesis and characterization of silver substituted strontium phosphate silicate apatite using solid-state reaction for osteoregenerative applications.

Dong Chen, Jingxin Zhao, Xin Jiang,

Strontium phosphosilicate is one of the fastest-growing apatite in bone regeneration application due to the presence of strontium and silica components in the parent materials. However, bacterial infections cause setbacks to the bone regeneration process often leading to surgical revisions, and is a big issue that needs to be addressed. ... Read more >>

Bioengineered (Bioengineered)
[2021, 12(1):1111-1125]

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Effect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms.

Samir Mehndiratta, Mei-Chuan Chen, Yuh-Hsuan Chao, Cheng-Hsin Lee, Jing-Ping Liou, Mei-Jung Lai, Hsueh-Yun Lee,

A series of 3-subsituted quinolinehydroxamic acids has been synthesised and evaluated for their effect on human lung cancer cell line (A549), human colorectal cancer cell line (HCT116) and HDAC isoforms 1, 2, 6, and 8. The results indicated that substitution at C3 of quinoline is favoured for HDAC6 selectivity. Two ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):74-84]

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Turning Pore Size of Silica-Based Nano-TiO₂ for Treating Cyanide Wastewater.

Yubo Pan, Yali Zhang, Yaoguo Huang, Yun Jia, Hongyou Cui, Ming Wang,

Cyanide wastewater is a very highly toxic substance. In this study, a kind of silicon-based nano-TiO₂ material by turning pore size accurately is prepared to treat cyanide wastewater. The materials are characterized by XRD, TG analysis, N₂ adsorption/desorption test, UVAS analysis and TEM. Results show that adding NaCl to the ... Read more >>

J Nanosci Nanotechnol (Journal of nanoscience and nanotechnology)
[2021, 21(10):5150-5156]

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Pyridinium-2-carbaldoximes with quinolinium carboxamide moiety are simultaneous reactivators of acetylcholinesterase and butyrylcholinesterase inhibited by nerve agent surrogates.

Hyun Myung Lee, Rudolf Andrys, Jakub Jonczyk, Kyuneun Kim, Avinash G Vishakantegowda, David Malinak, Adam Skarka, Monika Schmidt, Michaela Vaskova, Kamil Latka, Marek Bajda, Young-Sik Jung, Barbara Malawska, Kamil Musilek,

The pyridinium-2-carbaldoximes with quinolinium carboxamide moiety were designed and synthesised as cholinesterase reactivators. The prepared compounds showed intermediate-to-high inhibition of both cholinesterases when compared to standard oximes. Their reactivation ability was evaluated <i>in vitro</i> on human recombinant acetylcholinesterase (<i>hr</i>AChE) and human recombinant butyrylcholinesterase (<i>hr</i>BChE) inhibited by nerve agent surrogates (NIMP, NEMP, ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):437-449]

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Synthesis of some quinazolinones inspired from the natural alkaloid L-norephedrine as EGFR inhibitors and radiosensitizers.

Mostafa M Ghorab, Maged S Abdel-Kader, Ali S Alqahtani, Aiten M Soliman,

A set of quinazolinones synthesized by the aid of L-norephedrine was assembled to generate novel analogues as potential anticancer and radiosensitizing agents. The new compounds were evaluated for their cytotoxic activity against MDA-MB-231, MCF-7, HepG-2, HCT-116 cancer cell lines and EGFR inhibitory activity. The most active compounds <b>5</b> and <b>6</b> ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):218-237]

Cited: 1 time

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Analogues of 2'-hydroxychalcone with modified C4-substituents as the inhibitors against human acetylcholinesterase.

Sri Devi Sukumaran, Shah Bakhtiar Nasir, Jia Ti Tee, Michael J C Buckle, Rozana Othman, Noorsaadah Abd Rahman, Vannajan Sanghiran Lee, Syed Nasir Abbas Bukhari, Chin Fei Chee,

A series of C4-substituted tertiary nitrogen-bearing 2'-hydroxychalcones were designed and synthesised based on a previous mixed type acetylcholinesterase inhibitor. Majority of the 2'-hydroxychalcone analogues displayed a better inhibition against acetylcholinesterase (AChE) than butyrylcholinesterase (BuChE). Among them, compound <b>4c</b> was identified as the most potent AChE inhibitor (IC<sub>50</sub>: 3.3 µM) and showed ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):130-137]

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Fabrication of Self-Healable, Robust Superhydrophobic Surfaces Using UV-Crosslinked Nanocomposite Films.

Yeon-Ah Park, Young-Geun Ha,

Studies on fabricating robust superhydrophobic surfaces by a low-cost method have been rare, despite the recent demand for nature-inspired superhydrophobic surfaces including self-healing ability in various industrial applications. Herein, we propose a fabrication method for self-healable, robust superhydrophobic nanocomposite films by facile solution-processed spray coating and UV curing. The components ... Read more >>

J Nanosci Nanotechnol (Journal of nanoscience and nanotechnology)
[2021, 21(12):6212-6216]

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Recovering Nutrients from Waste Black Water Through Multi-Functional Mesoporous Silica.

Eun-Sik Kim, Wang Geun Shim, Jeongmin Cha, Min-Jin Hwang,

In order to prevent the harmful effects in water phase such as eutrophication, industrial and urban sewages must be treated before discharging into the aquatic environment. In this work, amine grafted magnetic nanoporous silica materials are synthesized and applied as an adsorbent for the recovery of nutrients from waste black ... Read more >>

J Nanosci Nanotechnol (Journal of nanoscience and nanotechnology)
[2021, 21(9):4936-4940]

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Improved hydrolysis yields and silica recovery by design of experiments applied to acid-alkali pretreatment in rice husks

Bruna R Moreira, Marcia C Breitkreitz, Rachael Simister, Simon J McQueen-Mason, Leonardo D Gomez, Camila A Rezende,

In this work, a two-step pretreatment using acid and alkali was optimized for rice rusks (Oryza sativa) using a 2⁵⁻¹ fractional factorial design (FFD), followed by a central composite design (CCD) to further optimization of enzymatic saccharification. The effect of five variables was simultaneously evaluated: H₂SO₄ concentration (from 0–5.4 % ... Read more >>

(Industrial crops and products.)
[2021, 170:Not Available]

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Triterpenoids from strawberry Fragaria × ananassa Duch. cultivar Senga Sengana leaves

Michał Gleńsk, Marta K Dudek, Agata Rybacka, Maciej Włodarczyk, Izabela Fecka,

Senga Sengana is a common strawberry (Fragaria × ananassa Duch.) cultivar growing in southern Poland. From leaves of this popular horticultural plant six triterpenoids were obtained including one glycoside nigaichigoside F1. All compounds were isolated by repeated silica gel column chromatography and preparative HPLC on Reverse phase RP-18. Their structures ... Read more >>

(Industrial crops and products.)
[2021, 169:Not Available]

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Preparation of Mesoporous Silica Nanoparticles Modified by Urushiol and Their Adsorption on Malachite Green.

Xue-Qing Xiao, Zhi-Yu Chen, Jia-Wen Chen, Qin-Hui Chen,

The presence of malachite green dye in wastewater has a great negative impact on the environment. At present, industrial wastewater is treated using adsorption, electrolysis and membrane separation, among which the adsorption method is the most widely used wastewater treatment. In this study mesoporous silica nanoparticles (MSNs) were prepared using ... Read more >>

J Nanosci Nanotechnol (Journal of nanoscience and nanotechnology)
[2021, 21(9):4792-4796]

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Modulation of SETDB1 activity by APQ ameliorates heterochromatin condensation, motor function, and neuropathology in a Huntington's disease mouse model.

Yu Jin Hwang, Seung Jae Hyeon, Younghee Kim, Sungsu Lim, Min Young Lee, Jieun Kim, Ashwini M Londhe, Lizaveta Gotina, Yunha Kim, Ae Nim Pae, Yong Seo Cho, Jihye Seong, Hyemyung Seo, Yun Kyung Kim, Hyunah Choo, Hoon Ryu, Sun-Joon Min,

The present study describes evaluation of epigenetic regulation by a small molecule as the therapeutic potential for treatment of Huntington's disease (HD). We identified 5-allyloxy-2-(pyrrolidin-1-yl)quinoline (APQ) as a novel SETDB1/ESET inhibitor using a combined <i>in silico</i> and <i>in vitro</i> cell based screening system. APQ reduced SETDB1 activity and H3K9me3 levels in ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):856-868]

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Design, synthesis and evaluation of carbazole derivatives as potential antimicrobial agents.

Yi-Jie Xue, Ming-Yue Li, Xue-Jun Jin, Chang-Ji Zheng, Hu-Ri Piao,

Five series of novel carbazole derivatives containing an aminoguanidine, dihydrotriazine, thiosemicarbazide, semicarbazide or isonicotinic moiety were designed, synthesised and evaluated for their antimicrobial activities. Most of the compounds exhibited potent inhibitory activities towards different bacterial strains (including one multidrug-resistant clinical isolate) and one fungal strain with minimum inhibitory concentrations (MICs) ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):295-306]

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The anti-depressant effects of a novel PDE4 inhibitor derived from resveratrol.

Yingcong Yu, Jinhui Wang, Xianfeng Huang,

<h4>Context</h4>Resveratrol has shown anti-stress and anti-depressant-like abilities involved in inhibiting phosphodiesterase-4 (PDE4) enzyme. However, its application is limited due to its low efficacy, bioavailability and selectivity.<h4>Objective</h4>This study synthesized a new resveratrol derivative RES003 and evaluated its PDE4 inhibitory and anti-depressant-like activities <i>in vitro</i> and <i>in vivo</i>, respectively.<h4>Materials and methods</h4>PDEs inhibitory activities were ... Read more >>

Pharm Biol (Pharmaceutical biology)
[2021, 59(1):418-423]

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Drug delivery of amoxicillin molecule as a suggested treatment for covid-19 implementing functionalized mesoporous SBA-15 with aminopropyl groups.

Haneen F Alazzawi, Issam K Salih, Talib M Albayati,

SARS-CoV-2 is a novel coronavirus that was isolated and identified for the first time in Wuhan, China in 2019. Nowadays, it is a worldwide danger and the WHO named it a pandemic. In this investigation, a functionalization post-synthesis method was used to assess the ability of an adapted SBA-15 surface ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):856-864]

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Synthesis, biological evaluation and molecular docking investigation of new sulphonamide derivatives bearing naphthalene moiety as potent tubulin polymerisation inhibitors.

Guangcheng Wang, Meiyan Fan, Wenjing Liu, Min He, Yongjun Li, Zhiyun Peng,

A new series of sulphonamide derivatives bearing naphthalene moiety were synthesised and evaluated for their antiproliferative and tubulin polymerisation inhibitory activities. These new compounds were evaluated for their <i>in vitro</i> antiproliferative activity against MCF-7 and A549 by using CCK-8 method. Among all the tested compounds, compound <b>5c</b> with naphthalen-1-yl moiety exhibited ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):1402-1410]

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Galactosylated Chitosan Modified Magnetic Mesoporous Silica Nanoparticles Loaded with Nedaplatin for the Targeted Chemo-Photothermal Synergistic Therapy of Cancer.

Yihan Kong, Xue Li, Xiaojing Liu, Jingjing Pang, Xinling Mu, Wei Liu,

The use of chemotherapy combined with photothermal therapy (PTT) is getting a focus topic for cancer treatment. Duing this research, the double targeting drug delivery system of nedaplatin (NDP)-carboxyl-functionalized magnetic mesoporous silica (MMSN-COOH)-galactosylated chitosan (GC) nanoparticles (NPs) was constructed. Because MMSNs have special physical properties, it can target to the ... Read more >>

J Nanosci Nanotechnol (Journal of nanoscience and nanotechnology)
[2021, 21(9):4553-4564]

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Encapsulation of sea fennel (Crithmum maritimum) essential oil in nanoemulsion and SiO2 nanoparticles for treatment of the crop pest Spodoptera litura and the dengue vector Aedes aegypti

Udaiyan Suresh, Kadarkarai Murugan, Chellasamy Panneerselvam, Al Thabiani Aziz, Kevin Cianfaglione, Lan Wang, Filippo Maggi,

Crithmum maritimum L. (Apiaceae), also known as sea fennel, is a halophythe plant colonizing cliffs and coastal dunes and pebble of the Mediterranean sea and Atlantic ocean. Based on previous reports, this herb produces an essential oil endowed with insecticidal effects against various pests and insect vectors. In the present ... Read more >>

(Industrial crops and products.)
[2021, 158:Not Available]

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Novel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters.

Elisabetta Barresi, Chiara Giacomelli, Laura Marchetti, Emma Baglini, Silvia Salerno, Giovanni Greco, Federico Da Settimo, Claudia Martini, Maria Letizia Trincavelli, Sabrina Taliani,

Small-molecules acting as positive allosteric modulators (PAMs) of the A<sub>2B</sub> adenosine receptor (A<sub>2B</sub> AR) could potentially represent a novel therapeutic strategy for pathological conditions characterised by altered bone homeostasis, including osteoporosis. We investigated a library of compounds (<b>4</b>-<b>13</b>) exhibiting different degrees of chemical similarity with three indole derivatives (<b>1</b>-<b>3</b>), which ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):286-294]

Cited: 1 time

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Larvicidal activity of Annona mucosa Jacq. extract and main constituents rolliniastatin 1 and rollinicin against Aedes aegypti and Aedes albopictus

Alzeir Machado Rodrigues, Alice Araujo da Silva, José Claudio Carneiro de Freitas, Victor Emanuel Pessoa Martins, Maria Auxiliadora Pantoja Ferreira, Ana Cássia Sarmento Ferreira, Cynthia Letícia Serra Cabeça, Ana Livya Moreira Rodrigues, Daniela Ribeiro Alves, Selene Maia de Morais,

Annona mucosa Jacq. (Annonaceae) is an edible plant whose fruit is appreciated in the Amazon region of Brazil. The seeds of this plant are rich sources of acetogenins, substances that have antimicrobial, anticancer, repellent, insecticide and larvicidal activities. However, studies on larvicidal evaluation of these substances are almost always limited ... Read more >>

(Industrial crops and products.)
[2021, 169:Not Available]

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Design, synthesis, and in vitro evaluation of BP-1-102 analogs with modified hydrophobic fragments for STAT3 inhibition.

Patrik Oleksak, Miroslav Psotka, Marketa Vancurova, Olena Sapega, Jana Bieblova, Milan Reinis, David Rysanek, Romana Mikyskova, Katarina Chalupova, David Malinak, Jana Svobodova, Rudolf Andrys, Helena Rehulkova, Vojtech Skopek, Pham Ngoc Lam, Jiri Bartek, Zdenek Hodny, Kamil Musilek,

Twelve novel analogs of STAT3 inhibitor BP-1-102 were designed and synthesised with the aim to modify hydrophobic fragments of the molecules that are important for interaction with the STAT3 SH2 domain. The cytotoxic activity of the reference and novel compounds was evaluated using several human and two mouse cancer cell ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2021, 36(1):410-424]

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