keyword
https://read.qxmd.com/read/38524479/new-benzimidazole-triazole-derivatives-as-topoisomerase-i-inhibitors-design-synthesis-anticancer-screening-and-molecular-modeling-studies
#1
JOURNAL ARTICLE
Ulviye Acar Çevik, Betül Kaya, Ismail Celik, Mithun Rudrapal, Gourav Rakshit, Arzu Karayel, Serkan Levent, Derya Osmaniye, Begüm Nurpelin Sağlık Özkan, Merve Baysal, Özlem Atlı Ekliog Lu, Yusuf Özkay, Zafer Asım Kaplancıklı
In this study, we designed, synthesized, and evaluated a series of 1,2,4-triazole benzimidazoles for their cytotoxic effects against the A549, C6, and NIH3T3 cell lines. Additionally, these compounds were assessed for their inhibitory activity against DNA topoisomerase I, aiming to develop novel anticancer agents. The synthesized final compounds 4a - h were characterized using 1 H NMR, 13 C NMR, and HRMS. Among them, compounds 4b and 4h emerged as the most potent agents against the A549 cell line, exhibiting an IC50 value of 7...
March 19, 2024: ACS Omega
https://read.qxmd.com/read/38408672/antimicrobials-in-eisenia-fetida-earthworms-a-comprehensive-study-from-method-development-to-the-assessment-of-uptake-and-degradation
#2
JOURNAL ARTICLE
I Vergara-Luis, C F Rutkoski, E Urionabarrenetxea, E A Almeida, E Anakabe, M Olivares, M Soto, A Prieto
In this work, an accurate analytical method was developed for the simultaneous analysis of twenty-seven antimicrobials (AMs) in earthworms using liquid chromatography coupled to a triple quadrupole mass spectrometry detector (UHPLC-MS/MS). Adequate apparent recoveries (80-120 %) and limits of quantification (LOQ) (1 μg·kg-1 - 10 μg·kg-1 ) were obtained, with the exception of norfloxacin (34 μg·kg-1 ). The method was applied to evaluate the accumulation of sulfamethazine (SMZ) and tetracycline (TC) in earthworms after performing OECD-207 toxicity test, in which Eisenia fetida (E...
February 24, 2024: Science of the Total Environment
https://read.qxmd.com/read/38312789/validation-of-a-core-patient-reported-outcome-measure-for-life-participation-in-kidney-transplant-recipients-the-song-life-participation-instrument
#3
JOURNAL ARTICLE
Allison Jaure, Rahim T Vastani, Armando Teixeira-Pinto, Angela Ju, Jonathan C Craig, Andrea K Viecelli, Nicole Scholes-Robertson, Michelle A Josephson, Curie Ahn, Zeeshan Butt, Fergus J Caskey, Fabienne Dobbels, Kevin Fowler, Sheila Jowsey-Gregoire, Vivekanand Jha, Jane C Tan, Benedicte Sautenet, Martin Howell
INTRODUCTION: Life participation has been established as a critically important core for trials in kidney transplantation. We aimed to validate a patient-reported outcome measure for life participation in kidney transplant recipients. METHODS: A psychometric evaluation of the Standardized Outcomes in Nephrology life participation (SONG-LP) measure was conducted in adult kidney transplant recipients. The measure includes 4 items of life participation (leisure, family, work, and social) each with a 5-point Likert scale...
January 2024: KI Reports
https://read.qxmd.com/read/38312159/crystal-structures-of-sixteen-phosphane-chalcogenide-complexes-of-gold-i-chloride-bromide-and-iodide
#4
JOURNAL ARTICLE
Daniel Upmann, Peter G Jones, Dirk Bockfeld, Eliza Târcoveanu
The structures of 16 phosphane chalcogenide complexes of gold(I) halides, with the general formula R 1 3- n R 2 n P E Au X ( R 1 = t -butyl; R 2 = isopropyl; n = 0 to 3; E = S or Se; X = Cl, Br or I), are presented. The eight possible chlorido derivatives are: 1a , n = 3, E = S; 2a , n = 2, E = S; 3a , n = 1, E = S; 4a , n = 0, E = S; 5a , n = 3, E = Se; 6a , n = 2, E = Se; 7a , n = 1, E = Se; and 8a , n = 0, E = Se, and the corresponding bromido derivatives are 1b - 8b in the same order. However, 2a and 2b were badly disordered and 8a was not obtained...
January 1, 2024: Acta Crystallographica. Section E, Crystallographic Communications
https://read.qxmd.com/read/38206850/relational-attributions-for-one-s-own-resilience-predict-compassion-for-others
#5
JOURNAL ARTICLE
Rachel L Ruttan, Ting Zhang, Sivahn B Barli, Katherine A DeCelles
Existing work on attribution theory distinguishes between external and internal attributions (i.e., "I overcame adversity due to luck" vs. "my own effort"). We introduce the construct of relational resilience attributions (i.e., "due to help from other people") as a critical, but overlooked form of external attribution that predicts compassion toward others. We first document the presence of internal, relational (social external), and situational (nonsocial external) resilience attributions among people who have overcome unemployment, showing the predominance of internal attributions (Study 1)...
January 11, 2024: Journal of Personality and Social Psychology
https://read.qxmd.com/read/38012128/a-simeprevir-inducible-molecular-switch-for-the-control-of-cell-and-gene-therapies
#6
JOURNAL ARTICLE
Stacey E Chin, Christina Schindler, Lisa Vinall, Roger B Dodd, Lisa Bamber, Sandrine Legg, Anna Sigurdardottir, D Gareth Rees, Tim I M Malcolm, Samantha J Spratley, Cecilia Granéli, Jonathan Sumner, Natalie J Tigue
Chemical inducer of dimerization (CID) modules can be used effectively as molecular switches to control biological processes, and thus there is significant interest within the synthetic biology community in identifying novel CID systems. To date, CID modules have been used primarily in engineering cells for in vitro applications. To broaden their utility to the clinical setting, including the potential to control cell and gene therapies, the identification of novel CID modules should consider factors such as the safety and pharmacokinetic profile of the small molecule inducer, and the orthogonality and immunogenicity of the protein components...
November 27, 2023: Nature Communications
https://read.qxmd.com/read/37867649/synthesis-antifungal-ergosterol-inhibition-antibiofilm-activities-and-molecular-docking-on-%C3%AE-tubulin-and-sterol-14-alpha-demethylase-along-with-dft-based-quantum-mechanical-calculation-of-pyrazole-containing-fused-pyridine-pyrimidine-derivatives
#7
JOURNAL ARTICLE
Nisheeth C Desai, Ashvinkumar G Khasiya, Dharmpalsinh J Jadeja, Jahnvi D Monapara, Aratiba M Jethawa, Bharti P Dave, Sree Kanth Sivan, Vijjulatha Manga, Pravin C Mhaske, Doongar R Chaudhary
Multidrug-resistant fungal infections have become much more common in recent years, especially in immune-compromised patients. Therefore, researchers and pharmaceutical professionals have focused on the development of novel antifungal agents that can tackle the problem of resistance. In continuation to this, a novel series of pyrazole-bearing pyrido[2,3- d ]pyrimidine-2,4(1 H ,3 H )-dione derivatives ( 4a - 4o ) have been developed. These compounds have been screened against Candida albicans , Aspergillus niger , and Aspergillus clavatus ...
October 17, 2023: ACS Omega
https://read.qxmd.com/read/37693668/structures-of-rac-2-4-3-5-di-methyl-ene-xylitol-derivatives
#8
JOURNAL ARTICLE
Michael Satlow, Paul G Williard
The structures of three racemic (tetra-hydro-[1,3]dioxino[5,4- d ][1,3]dioxin-4-yl)methanol derivatives are reported, namely, 4-[(methyl-sulfon-yloxy)meth-yl]-2,4,4a,6,8,8a-hexa-hydro-[1,3]dioxino[5,4- d ][1,3]dioxine, C8 H14 O7 S, 1 , 4-[(benz-yloxy)meth-yl]-2,4,4a,6,8,8a-hexa-hydro-[1,3]dioxino[5,4- d ][1,3]dioxine, C14 H18 O5 , 2 , and 4-[(anilinocarbon-yl)meth-yl]-2,4,4a,6,8,8a-hexa-hydro-[1,3]dioxino[5,4- d ][1,3]dioxine, C14 H17 NO6 , 3 . Mesylate ester 1 at 173 K has triclinic P symmetry and both benzyl ether 2 at 173 K and phenyl urethane 3 have monoclinic P 21 / c symmetry...
September 1, 2023: Acta Crystallographica. Section E, Crystallographic Communications
https://read.qxmd.com/read/37636505/new-supramolecules-of-bis-acylhydrazones-linked-bisphenol-sulfide-for-alzheimer-s-targeting-cholinesterases-by-in-vitro-and-in-silico-approaches
#9
JOURNAL ARTICLE
Muhammad Ibrahim, Mumtaz Ali, Sobia Ahsan Halim, Abdul Latif, Manzoor Ahmad, Sajid Ali, SameeUllah, Ajmal Khan, Alany Ingrido Rebierio, Jalal Uddin, Ahmed Al-Harrasi
In current research, two functional components, i.e. , hydrazone and bisphenol sulfide were combined to get useful supramolecules in medicinal chemistry. Herein 25 new 4,4'-thiodiphenol bis-acylhydrazones were synthesized in good to excellent yields. Initially ethyl-2-chloroacetate was reacted with 4,4'-thiodiphenol, which was further reacted with excess hydrazine hydrate to produce 2,2'-((thiobis(4,1-phenylene))bis(oxy))di(acetohydrazide), which was then combined with various aromatic and aliphatic aldehydes to get the desired products (hydrazones, 4a-4y)...
August 21, 2023: RSC Advances
https://read.qxmd.com/read/37418342/active-surveillance-of-oesophageal-cancer-after-response-to-neoadjuvant-chemoradiotherapy-dysphagia-is-uncommon
#10
JOURNAL ARTICLE
Maria J Valkema, Manon C W Spaander, Jurjen J Boonstra, Jolanda M van Dieren, Wouter L Hazen, G Willemien Erkelens, I Lisanne Holster, Andries van der Linden, Klaas van der Linde, Liekele E Oostenbrug, Rutger Quispel, Erik J Schoon, Peter D Siersema, Michail Doukas, Ben M Eyck, Berend J van der Wilk, Pieter C van der Sluis, Bas P L Wijnhoven, Sjoerd M Lagarde, J Jan B van Lanschot
BACKGROUND: Active surveillance is being investigated as an alternative to standard surgery after neoadjuvant chemoradiotherapy for oesophageal cancer. It is unknown whether dysphagia persists or develops when the oesophagus is preserved after neoadjuvant chemoradiotherapy. The aim of this study was to assess the prevalence and severity of dysphagia during active surveillance in patients with an ongoing response. METHODS: Patients who underwent active surveillance were identified from the Surgery As Needed for Oesophageal cancer ('SANO') trial...
September 6, 2023: British Journal of Surgery
https://read.qxmd.com/read/37210826/design-synthesis-and-evaluation-of-2-aryl-quinoline-derivatives-against-12r-lipoxygenase-12r-lox-discovery-of-first-inhibitor-of-12r-lox
#11
JOURNAL ARTICLE
Harshavardhan Bhuktar, Sharda Shukla, Kumar Reddy Kakularam, Srikanth Battu, Manupati Srikanth, Susmita Srivastava, Raghavender Medishetti, Pooja Ram, P C Jagadish, Mahaboobkhan Rasool, Sandipan Chakraborty, Nooruddin Khan, Pallu Reddanna, Srinivas Oruganti, Manojit Pal
The 12R-lipoxygenase (12R-LOX), a (non-heme) iron-containing metalloenzyme belonging to the lipoxygenase (LOX) family catalyzes the conversion of arachidonic acid (AA) to its key metabolites. Studies suggested that 12R-LOX plays a critical role in immune modulation for the maintenance of skin homeostasis and therefore can be considered as a potential drug target for psoriasis and other skin related inflammatory diseases. However, unlike 12-LOX (or 12S-LOX) the enzyme 12R-LOX did not receive much attention till date...
May 12, 2023: Bioorganic Chemistry
https://read.qxmd.com/read/37189423/phytoceramides-from-the-marine-sponge-monanchora-clathrata-structural-analysis-and-cytoprotective-effects
#12
JOURNAL ARTICLE
Elena A Santalova, Alexandra S Kuzmich, Ekaterina A Chingizova, Ekaterina S Menchinskaya, Evgeny A Pislyagin, Pavel S Dmitrenok
In our research on sphingolipids from marine invertebrates, a mixture of phytoceramides was isolated from the sponge Monanchora clathrata (Western Australia). Total ceramide, ceramide molecular species (obtained by RP-HPLC, high-performance liquid chromatography on reversed-phase column) and their sphingoid/fatty acid components were analyzed by NMR (nuclear magnetic resonance) spectroscopy and mass spectrometry. Sixteen new ( 1b , 3a , 3c , 3d , 3f , 3g , 5c , 5d , 5f , 5g , 6b - g ) and twelve known ( 2b , 2e , 2f , 3b , 3e , 4a - c , 4e , 4f , 5b , 5e ) compounds were shown to contain phytosphingosine-type backbones i -t17:0 ( 1 ), n -t17:0 ( 2 ), i -t18:0 ( 3 ), n -t18:0 ( 4 ), i -t19:0 ( 5 ), or ai -t19:0 ( 6 ), N -acylated with saturated (2 R )-2-hydroxy C21 ( a ), C22 ( b ), C23 ( c ), i- C23 ( d ), C24 ( e ), C25 ( f ), or C26 ( g ) acids...
April 14, 2023: Biomolecules
https://read.qxmd.com/read/37078174/effect-of-hydrophobic-extension-of-aryl-enaminones-and-pyrazole-linked-compounds-combined-with-sulphonamide-sulfaguanidine-or-carboxylic-acid-functionalities-on-carbonic-anhydrase-inhibitory-potency-and-selectivity
#13
JOURNAL ARTICLE
Heba Abdelrasheed Allam, Mohamed E Albakry, Walaa R Mahmoud, Alessandro Bonardi, Shaimaa A Moussa, Samy Mohamady, Hatem A Abdel-Aziz, Claudiu T Supuran, Hany S Ibrahim
Design and synthesis of three novel series of aryl enaminones ( 3a - f and 5a - c ) and pyrazole ( 4a-c ) linked compounds with sulphonamides, sulfaguanidine, or carboxylic acid functionalities were reported as carbonic anhydrase inhibitors (CAIs) using the "tail approach" strategy in their design to achieve the most variable amino acids in the middle/outer rims of the hCAs active site. The synthesised compounds were assessed in vitro for their inhibitory activity against the following human (h) isoforms, hCA I, II, IX, and XII using stopped-flow CO2 hydrase assay...
December 2023: Journal of Enzyme Inhibition and Medicinal Chemistry
https://read.qxmd.com/read/37052518/synthesis-of-thiazole-chalcone-hybrid-molecules-antioxidant-alpha-%C3%AE-amylase-inhibition-and-docking-studies
#14
JOURNAL ARTICLE
Hafsa Iqbal, Tashfeen Akhtar, Muhammad Haroon, Aydın Aktaş, Ehsaan Tahir, Muhammad Ehsan
The molecular hybrid approach is very significant to combat various drug-resistant disorders. A simple, convenient, and cost-effective synthesis of thiazole-based chalcones is accomplished, using a molecular hybrid approach, in two steps. The compound 1-(2-phenylthiazol-4-yl)ethanone (3) was used as the main intermediate for the synthesis of 3-(arylidene)-1-(2-phenylthiazol-4-yl)prop-2-en-1-ones (4a-f). Thin layer chromatography was used to testify the formation and purity of all synthesized compounds. Further structural confirmation of all compounds was achieved via different spectroscopic techniques (UV, FT-IR, 1 H- and 13 C-NMR) and elemental analysis...
April 13, 2023: Chemistry & Biodiversity
https://read.qxmd.com/read/36773918/in-situ-release-and-sequestration-of-co-2-in-cement-composites-using-lta-zeolites
#15
JOURNAL ARTICLE
Wenjie Luo, Bo Li, Mengxia Xu, Chengheng Pang, Edward Lester, Liujie Xu, Kien-Woh Kow
This paper investigates the impact of in-situ release and sequestration of CO2 on the compressive strength, volume of permeable voids, phase change, hydration reaction, and micro-morphology of cement mortars. Two Linde Type A (LTA) zeolites with micro-pore dimensions of 5 Å and 4 Å (i.e., LTA 5A and 4A zeolites) were employed as CO2 carriers herein. The incorporation of 312 wt% plain LTA 5A and 4A zeolites increases the 1-day compressive strength of the mortars. However, the use of plain LTA 5A zeolite shows marginal contributions to the 7 and 28-day compressive strengths of the mortars, whilst using plain LTA 4A zeolite even deteriorates their 7 and 28-day compressive strengths...
February 9, 2023: Science of the Total Environment
https://read.qxmd.com/read/36645086/express-people-prefer-to-predict-middle-most-likely-quantitative-outcomes-not-extreme-ones-but-they-still-over-estimate-their-likelihood
#16
JOURNAL ARTICLE
Marie Juanchich, Miroslav Sirota, Karl Teigen
Past work showed a tendency to associate verbal probabilities (e.g., possible, unlikely) with extreme quantitative outcomes, and to over-estimate the outcomes' probability of occurrence. In the first four experiments (Exp 1, Exps. 2a-c), we tested whether this "extremity effect" reflects a general preference for extreme (vs. central or less extreme) values of a distribution. Participants made predictions based on a frequency distribution in two scenarios. We did not find a preference for extreme outcomes. Instead, most of the participants made a prediction about the middle, most frequent outcome of the distribution (i...
January 16, 2023: Quarterly Journal of Experimental Psychology: QJEP
https://read.qxmd.com/read/36633993/are-there-dominant-response-tendencies-for-social-reactions-trust-trumps-mistrust-evidence-from-a-dominant-behavior-measure-dbm
#17
JOURNAL ARTICLE
Maayan Katzir, Ann-Christin Posten
The question of whether individuals are more prone to trust or to mistrust has increasingly interested economists and psychologists in recent years. To investigate whether people have an initial response tendency to trust versus mistrust, we developed a novel paradigm-the Dominant Behavior Measure (DBM). Capitalizing on decades of meticulous research in basic cognitive psychology (i.e., bilingual studies, Stroop paradigm), we designed a task to measure the dominance of reactions in the social realm. Participants engaged in a series of trust games that involved switching between trusting and mistrusting two trustworthy counterparts and two untrustworthy counterparts, identified by color (while ignoring a distractor name) or by name (when no color was presented)...
January 12, 2023: Journal of Personality and Social Psychology
https://read.qxmd.com/read/36613958/the-synthesis-and-absolute-configuration-of-enantiomeric-pure-r-and-s-3-piperidin-3-yl-1h-indole-derivatives
#18
JOURNAL ARTICLE
Marek Król, Grzegorz Ślifirski, Jerzy Kleps, Piotr Podsadni, Ilona Materek, Anna E Kozioł, Franciszek Herold
This article describes the synthesis of new chiral 3-(piperidin-3-yl)-1H-indole derivatives (R)-10a-c and (S)-11a-c from the corresponding diastereomers: (3R, 2R) and (3S, 2R)-2-[3-(1H-indol-3-yl)-1-piperidyl]-2-phenyl-acetamides (3R, 2R)-4a, (3R, 2R)-6b, (3R, 2R)-8c and (3S, 2R)-5a, (3S, 2R)-7b, (3S, 2R)-9c . Diastereomers were obtained by N-alkylation of derivatives of racemic 3-(piperidin-3-yl)-1H-indoles 1a-c using (S)-2-(4-toluenesulfonyloxy)-phenylacetic amide (S)-II . The same method was applied to obtain (3R, 2S)-methyl-2-[3-(1H-indole-3-yl)-1-piperidyl]-2-phenylacetate (3R, 2S)-2a and (3S, 2S)-methyl-2-[3-(1H-indole-3-yl)-1-piperidyl]-2-phenylacetate (3S, 2S)-3a diastereomers by treating amine 1a with (R)-2-(4-toluenesulfonyloxy)-phenylacetic acid methylester (R)-I ...
December 28, 2022: International Journal of Molecular Sciences
https://read.qxmd.com/read/36557897/design-synthesis-and-biological-evaluation-of-syn-and-anti-like-double-warhead-quinolinones-bearing-dihydroxy-naphthalene-moiety-as-epidermal-growth-factor-receptor-inhibitors-with-potential-apoptotic-antiproliferative-action
#19
JOURNAL ARTICLE
Essmat M El-Sheref, Mohamed A Ameen, Kamal M El-Shaieb, Fathy F Abdel-Latif, Asmaa I Abdel-Naser, Alan B Brown, Stefan Bräse, Hazem M Fathy, Iqrar Ahmad, Harun Patel, Hesham A M Gomaa, Bahaa G M Youssif, Asmaa H Mohamed
Our investigation includes the synthesis of new naphthalene-bis-triazole-bis-quinolin-2(1H)-ones 4a - e and 7a - e  via Cu-catalyzed [3 + 2] cycloadditions of 4-azidoquinolin-2(1 H )-ones 3a - e with 1,5-/or 1,8-bis(prop-2-yn-1-yloxy)naphthalene ( 2 ) or ( 6 ). All structures of the obtained products have been confirmed with different spectroscopic analyses. Additionally, a mild and versatile method based on copper-catalyzed [3 + 2] cycloaddition (Meldal-Sharpless reaction) was developed to tether quinolinones to O-atoms of 1,5- or 1,8-dinaphthols...
December 10, 2022: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/36515681/the-choice-of-%C3%AE-vinyliminium-ligand-substituents-is-key-to-optimize-the-antiproliferative-activity-of-related-diiron-complexes
#20
JOURNAL ARTICLE
Beatrice Campanella, Simona Braccini, Giulio Bresciani, Michele De Franco, Valentina Gandin, Federica Chiellini, Alessandro Pratesi, Guido Pampaloni, Lorenzo Biancalana, Fabio Marchetti
Diiron vinyliminium complexes constitute a large family of organometallics displaying a promising anticancer potential. The complexes [Fe2Cp2(CO)(μ-CO){μ-η1:η3-C(R3)C(R4)CN(R1)(R2)}]CF3SO3 (2a-c, 4a-d) were synthesized, assessed for their behavior in aqueous solutions (D2O solubility, Log Pow, stability in D2O/DMSO-d6 mixture at 37°C over 48 hours) and investigated for their antiproliferative activity against A2780 and A2780cisR ovarian cancer cell lines and the nontumoral one Balb/3T3 clone A31...
December 14, 2022: Metallomics: Integrated Biometal Science
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