The medicinal chemistry of ferrocene has gained its momentum after the discovery of biological activities of ferrocifen and ferroquine. These ferrocenyl drugs have been designed by replacing the aromatic moiety of the organic drugs, tamoxifen and chloroquine respectively, with a ferrocenyl unit. The promising biological activities of these ferrocenyl drugs have paved a path to explore the medicinal applications of several ferrocenyl conjugates. In these conjugates, the ferrocenyl moiety has played a vital role in enhancing or imparting the anticancer activity to the molecule. The ferrocenyl conjugates induce the cytotoxicity by generating reactive oxygen species and thereby damaging the DNA. In medicinal chemistry, the five membered nitrogen heterocycles (azoles) play a significant role due to their rigid ring structure and hydrogen bonding ability with the biomolecules. Several potent drug candidates with azole groups have been in use as chemotherapeutics. Considering the importance of ferrocenyl moiety and azole groups, several ferrocenyl azole conjugates have been synthesized and screened for their biological activities. Hence, in the view of a wide scope in the development of potent drugs based on ferrocenyl azole conjugates, herein we present the details of synthesis and the anticancer activities of ferrocenyl compounds bearing azole groups such as imidazole, triazoles, thiazole and isoxazoles.
二茂铁的药物化学在发现二茂铁昔芬和二茂铁喹的生物活性后获得了发展势头。这些二茂铁药物是通过用二茂铁单元分别取代有机药物他莫昔芬和氯喹的芳香分子而设计出来的。这些二茂铁药物具有良好的生物活性,为探索几种二茂铁共轭物的药物应用铺平了道路。在这些共轭物中,二茂铁在增强或赋予分子抗癌活性方面发挥了重要作用。二茂铁共轭物通过产生活性氧从而破坏 DNA 来诱导细胞毒性。在药物化学中,五元氮杂环(唑类)因其刚性环结构和与生物大分子的氢键能力而发挥着重要作用。一些含有唑基的强效候选药物已被用作化疗药物。考虑到二茂铁基团和唑基团的重要性,人们合成了几种二茂铁基唑共轭物,并对其生物活性进行了筛选。因此,鉴于二茂铁基唑共轭物在开发强效药物方面的广阔前景,我们在此详细介绍了含唑基(如咪唑、三唑、噻唑和异噁唑)的二茂铁化合物的合成和抗癌活性。
{"title":"Ferrocenyl Azoles: Versatile N-Containing Heterocycles and their Anticancer Activities","authors":"Dr. Bhavya Deepthi Sadanala, Dr. Rajiv Trivedi","doi":"10.1002/tcr.202300347","DOIUrl":"10.1002/tcr.202300347","url":null,"abstract":"<p>The medicinal chemistry of ferrocene has gained its momentum after the discovery of biological activities of ferrocifen and ferroquine. These ferrocenyl drugs have been designed by replacing the aromatic moiety of the organic drugs, tamoxifen and chloroquine respectively, with a ferrocenyl unit. The promising biological activities of these ferrocenyl drugs have paved a path to explore the medicinal applications of several ferrocenyl conjugates. In these conjugates, the ferrocenyl moiety has played a vital role in enhancing or imparting the anticancer activity to the molecule. The ferrocenyl conjugates induce the cytotoxicity by generating reactive oxygen species and thereby damaging the DNA. In medicinal chemistry, the five membered nitrogen heterocycles (azoles) play a significant role due to their rigid ring structure and hydrogen bonding ability with the biomolecules. Several potent drug candidates with azole groups have been in use as chemotherapeutics. Considering the importance of ferrocenyl moiety and azole groups, several ferrocenyl azole conjugates have been synthesized and screened for their biological activities. Hence, in the view of a wide scope in the development of potent drugs based on ferrocenyl azole conjugates, herein we present the details of synthesis and the anticancer activities of ferrocenyl compounds bearing azole groups such as imidazole, triazoles, thiazole and isoxazoles.</p>","PeriodicalId":10046,"journal":{"name":"Chemical record","volume":"24 7","pages":""},"PeriodicalIF":7.0,"publicationDate":"2024-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141562743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Roberto do Carmo Pinheiro, Luiza Souza Marques, Juliano Ten Kathen Jung, Cristina Wayne Nogueira, Gilson Zeni
Diorganyl diselenides have emerged as privileged structures because they are easy to prepare, have distinct reactivity, and have broad biological activity. They have also been used in the synthesis of natural products as an electrophile in the organoselenylation of aromatic systems and peptides, reductions of alkenes, and nucleophilic substitution. This review summarizes the advancements in methods for the transformations promoted by diorganyl diselenides in the main functions of organic chemistry. Parallel, it will also describe the main findings on pharmacology and toxicology of diorganyl diselenides, emphasizing anti-inflammatory, hypoglycemic, chemotherapeutic, and antimicrobial activities. Therefore, an examination detailing the reactivity and biological characteristics of diorganyl diselenides provides valuable insights for academic researchers and industrial professionals.
{"title":"Recent Progress in Synthetic and Biological Application of Diorganyl Diselenides","authors":"Roberto do Carmo Pinheiro, Luiza Souza Marques, Juliano Ten Kathen Jung, Cristina Wayne Nogueira, Gilson Zeni","doi":"10.1002/tcr.202400044","DOIUrl":"10.1002/tcr.202400044","url":null,"abstract":"<p>Diorganyl diselenides have emerged as privileged structures because they are easy to prepare, have distinct reactivity, and have broad biological activity. They have also been used in the synthesis of natural products as an electrophile in the organoselenylation of aromatic systems and peptides, reductions of alkenes, and nucleophilic substitution. This review summarizes the advancements in methods for the transformations promoted by diorganyl diselenides in the main functions of organic chemistry. Parallel, it will also describe the main findings on pharmacology and toxicology of diorganyl diselenides, emphasizing anti-inflammatory, hypoglycemic, chemotherapeutic, and antimicrobial activities. Therefore, an examination detailing the reactivity and biological characteristics of diorganyl diselenides provides valuable insights for academic researchers and industrial professionals.</p>","PeriodicalId":10046,"journal":{"name":"Chemical record","volume":"24 7","pages":""},"PeriodicalIF":7.0,"publicationDate":"2024-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141558189","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mahmood Hassan Akhtar, Muhammad Azhar Hayat Nawaz, Manzar Abbas, Ning Liu, Wenzhao Han, Yan Lv, Cong Yu
pH has been considered one of the paramount factors in bodily functions because most cellular tasks exclusively rely on precise pH values. In this context, the current techniques for pH sensing provide us with the futuristic insight to further design therapeutic and diagnostic tools. Thus, pH-sensing (electrochemically and optically) is rapidly evolving toward exciting new applications and expanding researchers’ interests in many chemical contexts, especially in biomedical applications. The adaptation of cutting-edge technology is subsequently producing the modest form of these biosensors as wearable devices, which are providing us the opportunity to target the real-time collection of vital parameters, including pH for improved healthcare systems. The motif of this review is to provide insight into trending tech-based systems employed in real-time or in-vivo pH-responsive monitoring. Herein, we briefly go through the pH regulation in the human body to help the beginners and scientific community with quick background knowledge, recent advances in the field, and pH detection in real-time biological applications. In the end, we summarize our review by providing an outlook; challenges that need to be addressed, and prospective integration of various pH in vivo platforms with modern electronics that can open new avenues of cutting-edge techniques for disease diagnostics and prevention.
{"title":"Advances in pH Sensing: From Traditional Approaches to Next-Generation Sensors in Biological Contexts","authors":"Mahmood Hassan Akhtar, Muhammad Azhar Hayat Nawaz, Manzar Abbas, Ning Liu, Wenzhao Han, Yan Lv, Cong Yu","doi":"10.1002/tcr.202300369","DOIUrl":"10.1002/tcr.202300369","url":null,"abstract":"<p>pH has been considered one of the paramount factors in bodily functions because most cellular tasks exclusively rely on precise pH values. In this context, the current techniques for pH sensing provide us with the futuristic insight to further design therapeutic and diagnostic tools. Thus, pH-sensing (electrochemically and optically) is rapidly evolving toward exciting new applications and expanding researchers’ interests in many chemical contexts, especially in biomedical applications. The adaptation of cutting-edge technology is subsequently producing the modest form of these biosensors as wearable devices, which are providing us the opportunity to target the real-time collection of vital parameters, including pH for improved healthcare systems. The motif of this review is to provide insight into trending tech-based systems employed in real-time or in-vivo pH-responsive monitoring. Herein, we briefly go through the pH regulation in the human body to help the beginners and scientific community with quick background knowledge, recent advances in the field, and pH detection in real-time biological applications. In the end, we summarize our review by providing an outlook; challenges that need to be addressed, and prospective integration of various pH in vivo platforms with modern electronics that can open new avenues of cutting-edge techniques for disease diagnostics and prevention.</p>","PeriodicalId":10046,"journal":{"name":"Chemical record","volume":"24 7","pages":""},"PeriodicalIF":7.0,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141491100","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The cover picture shows the progress in the skeletal editing of the isatin scaffold in the last decade (2013-2023). A series of ring-expansion reactions for the construction of high-value heterocycles (quinolines, quinolones, polycyclic quinazolines, medium-sized compounds), as well as a variety of ring-opening strategies for the generation of the 2-(azoly)anilines by cleavage of the C−C bond and the C−N bond are revealed. More details can be found in article number e202400024 by Tiantian Zhang and Huangdi Feng (DOl: 10.1002/tcr.202400024.