RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA07741E
Manyam Subbi Reddy, Killari Satyam and Surisetti Suresh
{"title":"Design and application of intramolecular arylogous nitroaldol condensation to access 2-aryl-benzofuran and -indole derivatives and formal synthesis of saprisartan†","authors":"Manyam Subbi Reddy, Killari Satyam and Surisetti Suresh","doi":"10.1039/D4RA07741E","DOIUrl":"https://doi.org/10.1039/D4RA07741E","url":null,"abstract":"<p >This study presents the design and application of intramolecular arylogous nitroaldol (Henry) condensation. A transition metal-free, base-mediated reaction of <em>ortho</em>-heteroatom-substituted aryl aldehydes/ketones and 2-nitrobenzyl (pseudo)halides has been developed to access a wide range of 2-(2-nitroaryl)benzofuran/2-(2-nitroaryl)indole derivatives in high yields. The reaction appears to proceed through <em>O</em>-/<em>N</em>-benzylation and intramolecular arylogous nitroaldol condensation. The application potential of the presented strategy has been demonstrated in the formal synthesis of anti-hypertensive agent saprisartan through the efficient synthesis of an advanced key intermediate, which has been accomplished in a ten-fold high overall yield by using resourceful, inexpensive and less-toxic reagents compared to the known methods.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 37234-37239"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra07741e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142672305","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA06618A
Pravinkamaraj Ponraj and Saravanakumar Rajendran
{"title":"Design and synthesis of a novel curcumin–combretastatin A4 molecular skeleton: two pharmacophores†","authors":"Pravinkamaraj Ponraj and Saravanakumar Rajendran","doi":"10.1039/D4RA06618A","DOIUrl":"https://doi.org/10.1039/D4RA06618A","url":null,"abstract":"<p >The logical design and synthesis of a novel compound combretastatin A-4-integrated curcumin is presented. Claisen condensation of phenylacetone with ethyl acetates formed 1,5-diphenylpentane-2,4-dione. Condensation of the dione with benzaldehyde <em>via</em> a modified Pabon procedure formed combretastatin A-4-integrated curcumin. The single-crystal X-ray structure of one of the CA-4 integrated CURs was established as a representative example. Curcumin (CUR) and combretastatin A-4 (CA-4) are well-known bioactive natural products; however, their poor pharmacokinetic profiles and <em>cis</em>–<em>trans</em> isomerization under <em>in vivo</em> conditions, respectively, have limited their biological applications. Herein, coupling of an aryl group at the olefinic C2 and/or C6 position of CUR integrates a CA-4-like structure with <em>cis</em>-configuration locked to CUR. At the same time, aryl coupling created steric hindrance around the olefinic bond and could resist the reductive metabolism of CUR and contribute to a better pharmacokinetic profile. Remarkably, this modification did not disturb the functional groups in both the natural products (CUR and CA-4), which is promising for their therapeutic effects. Thus, the synthesized CA-4-integrated CUR molecular architecture offers a new molecular skeleton to be explored for bio-application.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 37227-37233"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra06618a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142679416","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA03904A
Xinyu Feng, Qi Xue, Junlin Zhang, Kaidi Yang, Kunkai Wang, Bozhou Wang and Fuqiang Bi
{"title":"Research on TNTON/DNTF eutectic characteristics: an exploration of low eutectic mixture based melt-cast explosive carriers†","authors":"Xinyu Feng, Qi Xue, Junlin Zhang, Kaidi Yang, Kunkai Wang, Bozhou Wang and Fuqiang Bi","doi":"10.1039/D4RA03904A","DOIUrl":"https://doi.org/10.1039/D4RA03904A","url":null,"abstract":"<p >To modify the sensitivity and melting point of the casting of DNTF, a eutectic system of insensitive explosive 3,5,5-trinitro-1,3-oxazinane (TNTON) and DNTF was prepared through a new method. The melting and liquefaction processes of TNTON/DNTF at different ratios were investigated, and a <em>T–x</em> phase diagram was established. The melting and decomposition processes of TNTON, DNTF, and TNTON/DNTF eutectic at different heating rates were compared, while the sensitivity tests were conducted to study the desensitizing effect of TNTON on DNTF. Using EXPLO-5 software, the detonation performance of the TNTON/DNTF eutectic was calculated. The experimental results show that the stoichiometric composition of the TNTON/DNTF eutectic is 58.26 : 41.74, with an average melting point of 69 °C. With the increase of heating rate, both the melting and decomposition reactions are delayed. According to the activation energy (<em>E</em><small><sub>a</sub></small>) curve, the thermal decomposition is through an autocatalytic process. The impact and friction sensitivity of the TNTON/DNTF eutectic are 38 J and 252 N, respectively. Theoretical density of the TNTON/DNTF eutectic is 1.906 g cm<small><sup>−3</sup></small>, and the calculated detonation velocity is 8921 m s<small><sup>−1</sup></small>. The TNTON/DNTF eutectic exhibits good thermal stability and can significantly reduce the sensitivity of DNTF while maintaining its high energy level. The detonation performance of TNTON/DNTF low eutectic cast explosive is better than that of TNT based cast explosive.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 36980-36988"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra03904a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142679504","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA07184K
Quan V. Vo, Nguyen Thi Hoa and Adam Mechler
{"title":"The radical scavenging activity of 1-methyl-1,4-dihydronicotinamide: theoretical insights into the mechanism, kinetics and solvent effects†","authors":"Quan V. Vo, Nguyen Thi Hoa and Adam Mechler","doi":"10.1039/D4RA07184K","DOIUrl":"https://doi.org/10.1039/D4RA07184K","url":null,"abstract":"<p >1,4-Dihydronicotinamide derivatives, including 1-methyl-1,4-dihydronicotinamide (<strong>MNAH</strong>), are derivatives of the active center of nicotinamide coenzyme (<strong>NADH</strong>) and are therefore potent radical scavengers. <strong>MNAH</strong> serves as a useful model of <strong>NADH</strong> that allows for modeling studies to address the activity of this important biomolecule. In this work, <strong>MNAH</strong> activity was evaluated against typical free radicals using quantum chemical calculations in physiological environments, with a secondary aim of comparing activity against two physiologically relevant radicals of markedly different stability, HO˙, and HOO˙, to establish which of these is a better model for assessing antioxidant capacity in physiological environments. The HO˙ + <strong>MNAH</strong> reaction exhibited diffusion-limited overall rate constants in all media, including the gas phase. The HOO˙ antiradical activity of <strong>MNAH</strong> was also good, with overall rate constants of 2.00 × 10<small><sup>4</sup></small> and 2.44 × 10<small><sup>6</sup></small> M<small><sup>−1</sup></small> s<small><sup>−1</sup></small>, in lipid and aqueous media, respectively. The calculated rate constant in water (<em>k</em><small><sub>overall</sub></small>(<strong>MNAH</strong> + HOO˙) = 3.84 × 10<small><sup>5</sup></small> M<small><sup>−1</sup></small> s<small><sup>−1</sup></small>, pH = 5.6) is in good agreement with the experimental data (<em>k</em><small><sub>exp</sub></small>(<strong>NADH</strong> + HOO˙) = (1.8 ± 0.2)×10<small><sup>5</sup></small> M<small><sup>−1</sup></small> s<small><sup>−1</sup></small>). In terms of mechanism, the H-abstraction of the C4–H bond characterized the HOO˙ radical scavenging activity of <strong>MNAH</strong>, whereas HO˙ could react with <strong>MNAH</strong> at several sites and following either of SET (in polar media), RAF, and FHT reactions, which could be ascribed to the high reactivity of HO˙. For this reason the results suggest that activity against HOO˙ is a better basis for comparison of anti-radical potential. In the broader context, the HOO˙ scavanging activity of <strong>MNAH</strong> is better than that of reference antioxidants such as <em>trans</em>-resveratrol and ascorbic acid in the nonpolar environment, and Trolox in the aqueous physiological environment. Therefore, in the physiological environment, <strong>MNAH</strong> functions as a highly effective radical scavenger.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 37196-37201"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra07184k?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142679415","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA07061E
Quan-Doan Mai, Dang Thi Hanh Trang, Ngo Thi Loan, Hanh Nhung Bui, Nguyen Trung Thanh, Ta Ngoc Bach, Anh-Tuan Pham and Anh-Tuan Le
{"title":"Flexible paper-based Ag dendritic SERS chips for rapid in situ detection of thiram residues on pear skin†","authors":"Quan-Doan Mai, Dang Thi Hanh Trang, Ngo Thi Loan, Hanh Nhung Bui, Nguyen Trung Thanh, Ta Ngoc Bach, Anh-Tuan Pham and Anh-Tuan Le","doi":"10.1039/D4RA07061E","DOIUrl":"https://doi.org/10.1039/D4RA07061E","url":null,"abstract":"<p >Surface-enhanced Raman scattering (SERS) is a powerful, highly efficient analytical technique capable of providing label-free, non-invasive, rapid, and ultrasensitive molecular detection down to the single-molecule level. Despite its advantages, SERS remains largely confined to laboratory settings due to the complexities of substrate fabrication and challenges in analyzing real-world samples. Developing flexible SERS substrates that achieve both high fabrication efficiency and high sensing performance, while being practical for field applications, is critical for advancing SERS toward broader, real-world use. In this study, we present a novel paper-based Ag dendritic SERS chip, fabricated <em>via</em> a simple chemical reduction process that directly forms Ag dendritic nanostructures on cellulose fibers. This chip substrate demonstrates exceptional sensitivity for the detection of thiram pesticide, with a detection limit as low as 7.76 × 10<small><sup>−11</sup></small> M. The chip substrate also exhibits outstanding reliability, with reproducibility and repeatability both less than 5%. Furthermore, the flexible nature of the paper substrate enables it to conform to curved surfaces and be in direct contact with analytes, exemplified by its ability to adhere to and retrieve thiram from pear skin using a novel “paste-and-peel-off” technique. The substrate shows remarkable performance for thiram detection on pear skin, with sharp recovery rates ranging from 90% to 105%. With its facile fabrication, excellent sensitivity, high reliability, and practical applicability in non-invasive sampling, the paper-based Ag dendritic SERS substrate offers significant potential as an advanced substrate to bring SERS out of the laboratory and closer to real-world applications.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 36960-36969"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra07061e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142672332","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA07447E
Edina Rusen, Alexandra Mocanu, Gabriela Toader, Aurel Diacon, Cosmin Romanitan, Ovidiu Iorga, Martino Aldrigo, Catalin Parvulescu, Raul Mitran and Oana Brincoveanu
{"title":"Design of polyurethane composite foam obtained from industrial PET wastes and MXenes for EMI shielding applications†","authors":"Edina Rusen, Alexandra Mocanu, Gabriela Toader, Aurel Diacon, Cosmin Romanitan, Ovidiu Iorga, Martino Aldrigo, Catalin Parvulescu, Raul Mitran and Oana Brincoveanu","doi":"10.1039/D4RA07447E","DOIUrl":"https://doi.org/10.1039/D4RA07447E","url":null,"abstract":"<p >The primary aim of this study was to synthesize and characterize polyurethane (PUR) foams derived from the depolymerization products of poly(ethylene terephthalate) (PET) and MXenes (Nb<small><sub>2</sub></small>AlC). The depolymerized PET products were produced through a zinc acetate-catalyzed glycolysis process using diethylene glycol (DEG) as solvent. These glycolysis products were then reacted with 4,4′-diphenylmethane diisocyanate (MDI), commercial polyols, and MXenes to produce the PUR foams. The resulting materials were characterized using FT-IR, SEM, EDX mapping, mechanical testing, thermal analysis, and electromagnetic interference (EMI) shielding assessments. The analysis revealed that specimens with a higher concentration of the filler (3.55%) exhibited superior mechanical properties, while the thermal behavior remained relatively unchanged. The sample containing 2.56% of MXenes showed significant potential as an effective EMI shielding material in the 8–9 GHz frequency range, while the blank sample provided the best performance between 9–13 GHz, mostly due to a bigger high-frequency absorption in the upper part of the X band. Regarding mechanical performance, the compression force increased slightly from 1013.31 N to 1013.71 N as the Mxenes concentration increased from 2.56% to 3.55%.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 37202-37215"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra07447e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142679413","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA06847E
Rana Saad, Khaled Abdelkarem, Adel M. El Sayed, Mohamed Shaban, Inas A. Ahmed, M. T. Tammam and Hany Hamdy
{"title":"Characterization and enhanced carbon dioxide sensing performance of spin-coated Na- and Li-doped and Co-doped cobalt oxide thin films†","authors":"Rana Saad, Khaled Abdelkarem, Adel M. El Sayed, Mohamed Shaban, Inas A. Ahmed, M. T. Tammam and Hany Hamdy","doi":"10.1039/D4RA06847E","DOIUrl":"https://doi.org/10.1039/D4RA06847E","url":null,"abstract":"<p >Recognizing the substantial effects of carbon dioxide on human health and the environment, monitoring CO<small><sub>2</sub></small> levels has become increasingly vital. Owing to energy constraints and the widespread application of CO<small><sub>2</sub></small> gas sensors, it is important to design cost-effective, more efficient, and faster response CO<small><sub>2</sub></small> gas sensors that operate at room temperature and involve a low-cost technique. This study aims to develop a cost-effective and efficient CO<small><sub>2</sub></small> gas detector that functions at room temperature and uses less power than traditional high-temperature CO<small><sub>2</sub></small> sensors. In this study, we achieved this by employing innovative Co<small><sub>3</sub></small>O<small><sub>4</sub></small> thin films with optimized spinel-structured p-type semiconductors through spin-coating, facilitated by Li and Na doping as well as Li/Na codoping. Doping with 3% Li/Na reduced the crystallite size from 92.4 to 8.03 nm and increased the band gap from 3.31 to 3.69 eV. At room temperature (30 °C), the sensor response improved significantly, increasing from 50% to 345.01% for 3% Li-Co<small><sub>3</sub></small>O<small><sub>4</sub></small> upon the addition of 3% Na at a concentration of 9990 ppm. This performance surpasses that of most metal-oxide-based CO<small><sub>2</sub></small> sensors reported in the literature. Additionally, this optimized sensor demonstrated a very short response time of 18.8 s and a recovery time of 16.4 s at a CO<small><sub>2</sub></small> concentration of 9990 ppm diluted with air. It outperformed other films in terms of sensitivity, stability, response and recovery times, and performance across a wide range of relative humidity levels (43–90%). The sensor exhibited superior selectivity for CO<small><sub>2</sub></small> than for N<small><sub>2</sub></small>, H<small><sub>2</sub></small>, and NH<small><sub>3</sub></small>. Overall, the 3% Li, Na-Co<small><sub>3</sub></small>O<small><sub>4</sub></small> sensor is well-suited for climate change mitigation and industrial applications.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 49","pages":" 36852-36867"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra06847e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142672294","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA07236G
Huan Li and Yanxiao Li
{"title":"Design of an LiF-rich interface layer using high-concentration fluoroethylene carbonate and lithium bis(fluorosulfonyl)imide (LiFSI) to stabilize Li metal batteries","authors":"Huan Li and Yanxiao Li","doi":"10.1039/D4RA07236G","DOIUrl":"https://doi.org/10.1039/D4RA07236G","url":null,"abstract":"<p >The development of high-energy-density Li metal batteries is limited by the uncontrollable growth of Li dendrites and an unstable Li/electrolyte interface during long-term Li plating/stripping. In this work, using high-concentration fluoroethylene carbonate (FEC) electrolyte, an LiF-rich interface layer was generated on the Li metal surface. This LiF-rich interface layer could effectively inactivate the high reactivity of the Li metal surface and suppress lithium dendrite growth, forming a uniform and dense structure at the Li/electrolyte interface to stabilize Li metal batteries. Owing to the enhanced interface stability offered by the high-concentration FEC electrolyte with LiFSI additive, the Li‖LiFePO<small><sub>4</sub></small> cell presented high capacity retention (89.1%) after 200 cycles at 1C (165 mA g<small><sup>−1</sup></small>) and retained over 133.7 mA h g<small><sup>−1</sup></small> at 10C rate, whereas only 115.0 mA h g<small><sup>−1</sup></small> was achieved in the traditional carbonate ester electrolyte. The results show an obvious improvement in the cycle performance and rate capability of Li metal batteries containing a high-concentration FEC electrolyte with LiFSI as an additive.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 37074-37081"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra07236g?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142672298","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA07318E
Adam K. Hedger, Jonathan Findell, Dinesh S. Barak, Celia A. Schiffer, Jonathan K. Watts and Akbar Ali
{"title":"Efficient convergent synthesis of 1,3-diazepinone nucleosides by ring-closing metathesis and direct glycosylation†","authors":"Adam K. Hedger, Jonathan Findell, Dinesh S. Barak, Celia A. Schiffer, Jonathan K. Watts and Akbar Ali","doi":"10.1039/D4RA07318E","DOIUrl":"https://doi.org/10.1039/D4RA07318E","url":null,"abstract":"<p >A new and highly efficient ring-closing metathesis-based strategy was developed for the synthesis of the cyclic urea 1,3-diazepinone, presenting significant improvement upon previous methods. Using a direct glycosylation approach, analogues of the potent cytidine deaminase (CDA) inhibitor diazepinone riboside were then synthesized including 2′-deoxyribo-, 2′-deoxy-2′-fluoroarabino-, and 2′-deoxy-2′,2′-difluoro-diazepinone nucleosides, all with moderate to good yield and excellent anomeric selectivity. Crucially, in contrast to the previous multistep linear synthesis of 2′-deoxyribo- and 2′-deoxy-2′-fluoroarabino-diazepinone nucleosides, this is the first report of direct glycosylation to access these nucleosides. Overall, we report efficient convergent routes to multiple 2′-modified-diazepinone nucleosides for further evaluation as CDA and potential APOBEC3 inhibitors.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 37216-37226"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra07318e?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142679414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2024-11-20DOI: 10.1039/D4RA03571B
Asmaa E. Kassab, Rania M. Gomaa and Ehab M. Gedawy
{"title":"Drug repurposing of fluoroquinolones as anticancer agents in 2023","authors":"Asmaa E. Kassab, Rania M. Gomaa and Ehab M. Gedawy","doi":"10.1039/D4RA03571B","DOIUrl":"https://doi.org/10.1039/D4RA03571B","url":null,"abstract":"<p >Drug developers are currently focusing on investigating alternative strategies, such as “drug repositioning”, to address issues associated with productivity, regulatory obstacles, and the steadily rising cost of pharmaceuticals. Repositioning is the best strategy to stop searching for new drugs because it takes less time and money to investigate new indications for already approved or unsuccessful drugs. Although there are several potent Topo II inhibitors available on the market as important drugs used in the therapy of many types of cancer, more may be required in the future. The current inhibitors have drawbacks including acquired resistance and unfavorable side effects such as cardiotoxicity and subsequent malignancy. A substantial body of research documented the cytotoxic potential of experimental fluoroquinolones (FQs) on tumor cell lines and their remarkable efficacy against eukaryotic Topo II in addition to optimized physical and metabolic characteristics. The FQ scaffold has a unique ability to potentially resolve every major issue associated with traditional Topo II inhibitors while maintaining a highly desirable profile in crucial drug-likeness parameters; therefore, there is a significant chance that FQs will be repositioned as anticancer candidates. This review offers a summary of the most recent research on the anticancer potential of FQs that was published in 2023. Along with discussing structural activity relationship studies and the mechanism underlying their antiproliferative activity, this review aims to provide up-to-date information that will spur the development of more potent FQs as viable cancer treatment candidates.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 50","pages":" 37114-37130"},"PeriodicalIF":3.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2024/ra/d4ra03571b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142679511","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}