ChemistrySelectPub Date : 2024-12-21DOI: 10.1002/slct.202405153
Gaikwad Rajendra, Krithika Ganesh, Dr. Govinda G. Rajulu, Dr. Ganesh Sambasivam, Dr. Nagashree Shivashankarappa
{"title":"Green Synthesis of Repotrectinib: Impact of Aqueous Micellar Media on Chemoenzymatic Transformations","authors":"Gaikwad Rajendra, Krithika Ganesh, Dr. Govinda G. Rajulu, Dr. Ganesh Sambasivam, Dr. Nagashree Shivashankarappa","doi":"10.1002/slct.202405153","DOIUrl":"https://doi.org/10.1002/slct.202405153","url":null,"abstract":"<p>A greener, milder, and scalable route for the synthesis of the anticancer drug repotrectinib has been developed. The effect of aqueous micellar media on the synthesis of the key chiral amine intermediate followed by repotrectinib has been studied. The synthesis of 2-[(1R)-1-aminoethyl]-4-fluorophenol ((<b><i>R</i></b>)<b>-1</b>) from a commercially available ketone was carried out using the enzyme ATA-025 in the surfactant TPGS-750-M, resulting in an 82% yield and an enantiomeric excess (ee) > 99%. This method avoids the use of expensive chiral auxiliaries and hazardous reagents. Furthermore, the chiral amine ((<b><i>R</i></b>)<b>-1</b>) was used in the synthesis of repotrectinib in an aqueous medium, resulting in a high yield and an ee > 99%.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 48","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142861887","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-21DOI: 10.1002/slct.202404117
Subbulakshmi Ganesan, Vijay J. Upadhye, Nutan Sharma, Arpit Arora, Arunachalam Chinnathambi, Sulaiman Ali Alharbi, Samer Hasan Hussein-Al-Ali, Suha Mujahed Abudoleh, Indumathi Thangavelu
{"title":"Construction of Sorafenib Tosylate and Etoposide-loaded Liposomes: A Path to Precision Liver Cancer Therapy and its Apoptosis Induction","authors":"Subbulakshmi Ganesan, Vijay J. Upadhye, Nutan Sharma, Arpit Arora, Arunachalam Chinnathambi, Sulaiman Ali Alharbi, Samer Hasan Hussein-Al-Ali, Suha Mujahed Abudoleh, Indumathi Thangavelu","doi":"10.1002/slct.202404117","DOIUrl":"https://doi.org/10.1002/slct.202404117","url":null,"abstract":"<p>Nanotechnology is an effective tool in fighting against cancer, playing a crucial role in investigating and fabricating novel anticancer drugs. Recognizing the worldwide prevalence of cancer, we combined sorafenib tosylate (ST) and etoposide (ETP) within liposomes. We assessed their ability to kill human umbilical vein endothelial cells (HUVECs) and HepG2 liver cancer cells. The liposomes effectively contained ST and ETP, exhibiting a particle size distribution below 180 nm, a polydisperse index (PDI) below 0.2, a spherical shape, a strong negatively charged zeta potential, and encapsulation efficiencies of 59% for ST, 88% for ETP, and 57% for ST combined with 87% for ETP. The FTIR analysis indicates that the drugs were incorporated within liposomes. Encapsulation of the drugs in liposomes resulted in a more significant cytotoxic impact on HepG2 cells and a reduced cytotoxic impact on HUVECs. The morphological assessment of the HepG2 liver cancer cells was investigated using AO-EB and Hoechst 33258 staining methods. Apoptosis mechanisms of HepG2 cells were examined by Annexin V and PI dual staining. Furthermore, the coadministration of ST and ETP, which were enclosed in liposomes, resulted in a synergistic impact on the drugs, leading to cell death by apoptosis.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 48","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142861911","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-21DOI: 10.1002/slct.202403760
Tutku Tunç, Hulya Ozpinar, Ümit Muhammet Koçyiğit, Sultan ERKAN
{"title":"Exploring the Antioxidant, Antimicrobial, Antidiabetic, and Anticancer Properties of Capsicum annuum L. (Samandağ Pepper): Biochemical and In Silico Insights","authors":"Tutku Tunç, Hulya Ozpinar, Ümit Muhammet Koçyiğit, Sultan ERKAN","doi":"10.1002/slct.202403760","DOIUrl":"https://doi.org/10.1002/slct.202403760","url":null,"abstract":"<p><i>Capsicum annuum</i> L. species from the Samandağ district of Hatay/Turkey was used in our study. Phytochemical analysis of seed and fruit ethanol extracts of this plant was carried out by GC-MS method. Total Antioxidant Status (TAS) and Total Oxidant Status (TOS) levels were determined to calculate the Oxidative Stress Index to determine antioxidant activity. MIC method was used to evaluate antimicrobial properties against pathogenic bacteria and fungi. Anticancer activity was determined by the XTT assay on breast (MCF-7), lung (A549) and brain (C6) cancer cells and healthy fibroblast (WI-38) cell lines. The effects of the extracts on acetylcholinesterase and α-amylase activities were investigated. It was found that <i>C. annuum</i> fruit extract had a lower OSI value than the seed extract. Fruit and seed extracts showed antimicrobial activity on microorganisms at MIC values of 200 µg/mL. Molecular docking studies were conducted to analyze the antibacterial properties of plant active ingredients. These studies are chemical components that are determined to be more abundant in the plant extract. Thus, it aimed to evaluate the effects of active compounds on various bacterial species. The results revealed the potential antibacterial properties of plants and provided important data that these ingredients can be used in future treatment methods. The anticancer activity in all cancer cell lines was very high in both seed and fruit extracts with a selectivity index (SI) well above SI ≥ 3. Furthermore, no deleterious effect on healthy fibroblast (WI-38) cells was observed. The extracts were found to decrease acetylcholinesterase activity but increase α-amylase activity. As a result, these plant extracts were found to have anticholinergic potential.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 48","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142861886","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-17DOI: 10.1002/slct.202403804
S. Raj Mohan, Manoranjan P. Singh, S. Satapathy, S. K. Majumder
{"title":"Dependence of Charge Transport on the Degree of Ordering in Semicrystalline Conjugated Polymers","authors":"S. Raj Mohan, Manoranjan P. Singh, S. Satapathy, S. K. Majumder","doi":"10.1002/slct.202403804","DOIUrl":"https://doi.org/10.1002/slct.202403804","url":null,"abstract":"<p>The influence of ordering inside the crystalline regions of semi-crystalline polymer thin films on charge transport is investigated by analyzing the electric field dependence of mobility calculated using Monte Carlo simulation. The degree of ordering inside the ordered regions is varied by changing the overlap between the hopping transport sites. Negative field dependence of mobility extending to higher electric field strengths along with an increase in the mobility are observed upon increasing the overlap between transport sites inside the ordered region. These observations are attributed to the variation in the charge transport, which affects the transit time that not only decreases but also shows a gradual shift from negative to positive field dependence at lower electric field strengths (∼<3 × 10<sup>5</sup> V/cm). Variations in the transit time are explained using the variation in the field dependence of hops performed by the carrier inside the ordered and disordered regions. Field dependence of mobility is also simulated with ballistic charge transport inside the ordered regions. At low concentrations of ordered regions (COR), higher carrier mobility is attained with hopping transport (∼<70%). Ballistic transport provides higher mobility at higher COR (∼>70%). This suggests that a very high order inside the ordered region may not necessarily provide higher mobility.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 47","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142868507","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-17DOI: 10.1002/slct.202403842
Dr. Joseph Tchamgoue, Prof. Sylvain N. Pechangou, Dr. Abdul R. Issahaku, Dr. Yvan Anderson T. Ngandjui, Prof. Anke Wilhelm, Prof. Eutrophe L-D. Kamto, Prof. Paul F. Moundipa, Prof. Simeon F. Kouam
{"title":"In Vitro and In Silico Anti-Inflammatory Activities of Crude Extract and Phloroglucinol Derivatives from Mallotus oppositifolius (Geisler) Müll. Arg. (Euphorbiaceae)","authors":"Dr. Joseph Tchamgoue, Prof. Sylvain N. Pechangou, Dr. Abdul R. Issahaku, Dr. Yvan Anderson T. Ngandjui, Prof. Anke Wilhelm, Prof. Eutrophe L-D. Kamto, Prof. Paul F. Moundipa, Prof. Simeon F. Kouam","doi":"10.1002/slct.202403842","DOIUrl":"https://doi.org/10.1002/slct.202403842","url":null,"abstract":"<p>Numerous anti-inflammatory agents are used nowadays to relieve daily aches and pain. However, their severe side effects often limit their therapeutic use. In this study, we investigate the anti-inflammatory activity of the crude leaves extract of <i>Mallotus oppositifolius</i> and five of its phloroglucinol derivatives (<b>MO1</b>–<b>MO5</b>). From spectroscopic and spectrometric analysis, the compounds were identified as mallotojaponin B (<b>MO1</b>), mallotojaponin D (<b>MO2</b>), acronyculatin U (<b>MO3</b>), acronyculatin T (<b>MO4</b>), and mallotojaponin C (<b>MO5</b>). A primary macrophage culture activated by <i>Saccharomyces cereviseae</i> (SC) was used to evaluate the anti-inflammatory activity of the crude extract and isolated compounds which were found to be nontoxic to primary macrophages at concentrations ranging from 0.1–50 µg/mL. In addition, the tested samples inhibited the 5-lipoxygenase activity, nitric oxide (NO), and tumor necrosis factor alpha (TNF-α) production by viable primary mouse macrophages in a concentration-dependent manner with <b>MO1</b> and <b>MO3</b> exhibiting the highest in vitro anti-inflammatory activities. Moreover, in silico studies were performed with the isolated compounds to evaluate their binding capacities/scores against the main enzymes involved in inflammation mediation in human cells. The compounds showed good binding affinities to critical anti-inflammation targets particularly mallotojaponin C (<b>MO5</b>) (−44.55 Kcal/mol) and acronyculatin T (<b>MO4</b>) (−41.44 Kcal/mol) which showed the highest affinity for 5-lipoxygenase.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 47","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142868506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-17DOI: 10.1002/slct.202404644
Dr. Suliman A. Alderhami
{"title":"Characterization, Kinetics, Optimization, and Isotherm Studies of Methyl Green Adsorption on Iron Dithiocarbamate Complex","authors":"Dr. Suliman A. Alderhami","doi":"10.1002/slct.202404644","DOIUrl":"https://doi.org/10.1002/slct.202404644","url":null,"abstract":"<p>Iron (III) diethyldithiocarbamate complex (Fe(DTC)) of the general formula [Fe(S<sub>2</sub>CN(Et)<sub>2</sub>)<sub>3</sub>] was synthesized and characterized using chemical, thermogravimetric (TGA/DTG), and (FT-IR) analysis. The vapor adsorption tests verified that the Fe(DTC) was mesoporous and that the pore surface area was 16.73 m<sup>2</sup>/g, according to the N<sub>2</sub> adsorption-desorption isotherm. The main aim of this study is to eliminate methyl green (MG) from water via Fe(DTC) adsorption. The adsorption experiments, that investigated the influence of pH and mass, demonstrated that both of these factors have an impact on adsorption. The optimal conditions for MG adsorption onto the Fe(DTC) metal complex were 0.05 g for a Fe(DTC) mass and a pH value of 7 ± 0.2. At 333 K, the maximum capacity for the Fe(DTC) metal complex adsorbent was 26 mg/g for MG. At 180 min, the elimination efficiency for MG dye was approximately 87%. Based on the kinetic experiments, the pseudo-second-order model was determined to be the most appropriate for assessing the adsorption process. The mechanism of adsorption was studied by appropriating the adsorption data to the Temkin, Freundlich, Langmuir, Temkin, and Radushkevich models. The results can be adequately described by the Langmuir model.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 47","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142868508","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-17DOI: 10.1002/slct.202403341
Wei Dong, Changliang Wang, Ding Shen, Sinan Li, Mingzheng Xue, Shaobin Yang
{"title":"Preparation of Pitch Porous Nitrogen-doped Carbon and Its Low-temperature Lithium Storage Properties","authors":"Wei Dong, Changliang Wang, Ding Shen, Sinan Li, Mingzheng Xue, Shaobin Yang","doi":"10.1002/slct.202403341","DOIUrl":"https://doi.org/10.1002/slct.202403341","url":null,"abstract":"<p>The electrochemical performance of conventional lithium-ion batteries are significantly deteriorates at low temperatures, posing a significant challenge in the development of battery technology. This paper addresses this issue by focusing on the synthesis of a nitrogen-doped porous carbon material with fast lithium-ion diffusion and reaction kinetics at low temperatures. The material was prepared using pitch as a precursor, urea as a nitrogen source and blowing agent, and SiO<sub>2</sub> as a template. The obtained nitrogen-doped porous carbon material (denoted as PN-2) displayed a specific surface area of 167.64 m<sup>2</sup>/g and approximately five microcrystalline layers when the urea addition was 20%. Notably, at low temperatures, PN-2 demonstrated an impressive discharge specific capacity, with average values of 372, 295, 254, and 197 mAh/g at 25 °C, 0 °C, −20 °C, and −40 °C, respectively. The large specific surface area of the porous carbon material effectively increased the active sites for lithium ions, promoting rapid diffusion and improved lithium/delithium kinetics, thus enhancing the multiplicity performance at low temperatures. This research provides the valuable insights for the design of high-performance lithium-ion battery materials suitable for cold climate environments.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 47","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142868505","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-17DOI: 10.1002/slct.202404091
Rui Wang, Jiali Yuan, Huan Zhang, Xiang Liu, Jiani He, Prof. Dr. Lihua Zhu
{"title":"Highly Dispersed Palladium Nanoparticles on Carbon Doping with Nitrogen Derived from MOFs for 4-Nitrophenol Hydrogenation","authors":"Rui Wang, Jiali Yuan, Huan Zhang, Xiang Liu, Jiani He, Prof. Dr. Lihua Zhu","doi":"10.1002/slct.202404091","DOIUrl":"https://doi.org/10.1002/slct.202404091","url":null,"abstract":"<p>A series of the Pd/NC samples with various Pd loadings (0.11%, 0.48%, and 2.52%) are prepared via sodium borohydride (NaBH<sub>4</sub>) reduction method and carbon doping with nitrogen (NC) is acquired by the pyrolysis of ZIF-8. The samples are characterized by XRD, BET, SEM, TEM, HRTEM, STEM-EDX elemental maps and line-scanning, XPS, TG, and so forth. It confirms that the Pd nanoparticles (NPs) are successfully coated on the NC. The catalytic behaviors of the samples are evaluated by the hydrogenation of 4-nitrophenol (4-NP), the 2.52%Pd/NC catalyst shows the best catalytic property among as-obtained catalysts maybe due to the much more Pd(0) species. The 2.52%Pd/NC catalyst exhibits 100% selectivity to 4-aminophenol (4-AP) at high conversion of 4-nitrophenol and 321.8 h<sup>−1</sup> turnover frequency (TOF) under mild reaction conditions (3.0 MPa H<sub>2</sub>, 40 °C, 1 h). Moreover, the catalysts show an excellent stability.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 47","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142868509","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ChemistrySelectPub Date : 2024-12-17DOI: 10.1002/slct.202404444
Rajdeep Dey, Dr. Keerti Vishwakarma, Dr. Bhumika Patel, Dr. Vivek K. Vyas, Dr. Hardik Bhatt
{"title":"Evolution of Telomerase Inhibitors: A Review on Key Patents from 2015 to 2023","authors":"Rajdeep Dey, Dr. Keerti Vishwakarma, Dr. Bhumika Patel, Dr. Vivek K. Vyas, Dr. Hardik Bhatt","doi":"10.1002/slct.202404444","DOIUrl":"https://doi.org/10.1002/slct.202404444","url":null,"abstract":"<p>Telomerase (TERT) is a ribonucleoprotein that regulates telomere length and maintains chromosomal integrity. TERT is a widely expressed protein for replicative immortality in most malignant tumours. TERT is a protein produced by cancer cells that prevents telomere shortening by adding telomere sequences beyond the Hayflick limit, allowing them to divide in an uncontrolled manner. Inhibition of the TERT enzyme is a recognised therapy for treating cancer. The basic objective of the review is to collectively represent the current scenario of treating cancer by inhibiting TERT. With a focus on the recently patented TERT inhibitors and clinical trial data released between 2015 and 2023, this review highlights the work relevant to the development of TERT inhibitors. Furthermore, recent advancements in the clinical development of TERT inhibitors, along with prospective new combinations, are also discussed. The use of TERT inhibitors in cancer therapy has been granted with great interest and significant attention by researchers along with a promising outcome in terms of therapeutic value. Several clinical trial applications and their data gave strong evidence of the use of TERT inhibitors for cancer therapy which provided target therapies, vaccine therapies, nucleoside, non-nucleoside therapies, and so forth with reduced side effects and enhanced potency.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"9 47","pages":""},"PeriodicalIF":1.9,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142868510","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}