Article
Chemistry, Medicinal
Ling Lv, Mireguli Maimaitiming, Yan Huang, Jichen Yang, Shuxia Chen, Yanfeng Sun, Xuetao Zhang, Xin Li, Changhu Xue, Pingyuan Wang, Chang-Yun Wang, Zhiqing Liu
Summary: A series of quinazolin-4(3H)-one derivatives with cholinesterase inhibition and anti-inflammatory activities were designed and synthesized. The compound MR2938 showed promising inhibitory activity against acetylcholinesterase and suppressed NO production. It also decreased the levels of pro-inflammatory cytokines and suppressed neuroinflammation through blocking certain signaling pathways. These results suggest that MR2938 could be developed as a potential lead compound for anti-AD drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Yu Deng, Hao Mu, Hong-Bo Li, Li-Zhi Fu, Da Tang, Tao Wu, Shu-Heng Huang, Cheng-Hong Li
Summary: The study synthesized a series of anti-toxoplasmosis drugs and investigated the efficacy of two compounds against Toxoplasma gondii in vitro, showing good inhibitory effects. Results indicated that hydrophobic aryl moieties on the side chain could improve activity.
CHEMISTRY & BIODIVERSITY
(2021)
Article
Agronomy
Mei Zhu, Yan Li, Dan-ping Chen, Cheng-peng Li, Gui-ping Ouyang, Zhen-chao Wang
Summary: In this study, a series of compounds with novel structures were designed and synthesized, and their antibacterial activity against Xanthomonas oryzae pv. oryzae was evaluated. Compound 1 exhibited remarkable antibacterial activity and decreased the pathogenicity of the bacteria. These findings suggest that these compounds have the potential to be used as bacteriostats to control rice bacterial leaf blight.
PEST MANAGEMENT SCIENCE
(2023)
Article
Chemistry, Medicinal
Shangde Liu, Duo Yuan, Shanshan Li, Roujie Xie, Yi Kong, Xiong Zhu
Summary: PAR4 antagonists are crucial in reducing the risk of heart attack and thrombotic complications in stroke. Highly selective PAR4 antagonists, such as 13 and 30g, have shown promising activity and selectivity, potentially serving as starting points for further research in this area.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Peng Li, Ying Liu, Hua Yang, Hong-Min Liu
Summary: Recent research has shown that novel quinazolin-4(3H)-one derivatives are potent USP7 inhibitors with promising potential for cancer therapy. Compounds C9 and C19 displayed strong inhibitory activity against USP7 and were particularly effective against gastric cancer cells. Further studies demonstrated their ability to decrease MDM2 protein levels and increase tumor suppressors p53 and p21, making them promising candidates for anti-gastric cancer drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Shen Ge, Yi-Ming Zhu, Xiao-Ping Xu, Shun-Jun Ji
Summary: A palladium-catalyzed three-component reaction was used for the one-pot synthesis of 2-(trifluoromethyl)-quinazolin-4(3H)-imines, using isocyanides, 2,2,2-trifluoro-N-(2-iodophenyl)acetimidoyl chlorides, and amines. The protocol offers a wide substrate scope, high efficiency, and readily available raw materials.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Zheng Jing, Tomohiro Iba, Hisamichi Naito, Pingping Xu, Jun-ichi Morishige, Naoto Nagata, Hironao Okubo, Hitoshi Ando
Summary: Lenvatinib, an oral tyrosine kinase inhibitor, can cause muscle-related adverse reactions. Co-administration of L-carnitine with lenvatinib can prevent the decrease in carnitine content and expression levels of carnitine-related and OXPHOS proteins in the skeletal muscle, without affecting its anticancer activity.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Aram Faraji, Rasoul Motahari, Zaman Hasanvand, Tayebeh Oghabi Bakhshaiesh, Mahsa Toolabi, Setareh Moghimi, Loghman Firoozpour, Mohammad Amin Boshagh, Roya Rahmani, Shima H. M. E. Ketabforoosh, Hamid Reza Bijanzadeh, Rezvan Esmaeili, Alireza Foroumadi
Summary: A series of new compounds containing thiazole-urea were designed, synthesized, and evaluated for their biological activities. Compound 9f showed moderate growth inhibitory effects on cancer cells and induced apoptosis in HUVEC cells. The reduction in cell proliferation may be achieved by inhibiting the phosphorylation of VEGFR-2.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Chrysoula Mikra, Zoi Melissari, Maroula G. Kokotou, Panagiotis Gritzapis, Konstantina C. Fylaktakidou
Summary: A series of quinazolinone derivatives were synthesized using a microwave-assisted one-pot four-component or two-step reaction protocol. The reaction conditions and yield were evaluated, and the molecules were found to have potential applications in organic, medicinal, and material chemistry.
SUSTAINABLE CHEMISTRY AND PHARMACY
(2022)
Article
Biochemistry & Molecular Biology
Anastasios Panagopoulos, Thomas Balalas, Achilleas Mitrakas, Vassilios Vrazas, Katerina R. Katsani, Alexandros E. Koumbis, Michael I. Koukourakis, Konstantinos E. Litinas, Konstantina C. Fylaktakidou
Summary: Photochemo and photodynamic therapies are minimally invasive approaches for cancer treatment and combating bacterial resistance. Quinazolinone compounds, especially when appropriately substituted, show potential as new lead photosensitizers and DNA photocleaving agents under UV and visible light irradiation.
PHOTOCHEMISTRY AND PHOTOBIOLOGY
(2021)
Article
Chemistry, Physical
Weiqiang Chen, Boli Nie, Mei Liu, Hui-Jing Li, Dan-Yang Wang, Weiwei Zhang, Yan-Chao Wu
Summary: In this study, two piperazine-substituted quinazolin-4(3H)-one derivatives, PPQ and MPPQ, were designed and investigated as effective corrosion inhibitors for mild steel in HCl solution. Experimental results showed that both compounds exhibited high corrosion inhibition efficiencies of 96.6% and 96.1% at 0.4 mM concentration. Various analytical techniques confirmed the formation of protective films on the steel surface by PPQ and MPPQ, indicating their potential as corrosion inhibitors in the field of corrosion.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2021)
Article
Biochemistry & Molecular Biology
Abdallah E. Abdallah, Sally Eissa, Maged Mohammed Saleh Al Ward, Reda R. Mabrouk, Ahmed B. M. Mehany, Mohamed Ayman El-Zahabi
Summary: This work aimed to develop new effective anti-cancer agents by designing and synthesizing nineteen new quinazolin4-one derivatives with potential anticancer activity. Compound 36 was identified as the most potent candidate with significant inhibition of VEGFR-2 kinase and good anti-cancer activity against multiple cancer cell lines. Additionally, compound 36 showed good selectivity index and the ability to induce apoptosis in cancer cells.
BIOORGANIC CHEMISTRY
(2021)
Review
Immunology
Parisa Shamshiripour, Fahimeh Hajiahmadi, Shahla Lotfi, Niloofar Robab Esmaeili, Amir Zare, Mahzad Akbarpour, Davoud Ahmadvand
Summary: This review discusses the underlying molecular mechanisms contributing to aberrant angiogenesis in glioblastoma and the clinical applications and limitations of anti-angiogenic immunotherapeutics, as well as the potential advantages and limitations of small interfering RNAs as next-generation therapeutics.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Chemistry, Organic
Natalia B. Kilimciler, Nicolas M. Palavecino, Nadia Gruber, Daniel R. Vega, Liliana R. Orelli, Jimena E. Diaz
Summary: A novel method utilizing trimethylsilyl polyphosphate (PPSE) has been developed to synthesize quinazolin4(3H)-imines (QIs) by reacting 2-aminobenzonitrile with secondary amides. This general reaction allows for the synthesis of N3-aryl and N3-alkyl QIs with varying 2-substituents, resulting in high yields. The procedure can also be applied to derivatives containing additional functional groups. The simplicity of the method, along with readily available starting materials and a mild dehydrating agent, makes it suitable for scalability. Based on literature data and experimental observations, a possible reaction path involving an intermediate nitrilium ion is proposed.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Sumit Kumar, Kishor Padala, Barnali Maiti
Summary: A quinazolin-4(3H)-one ring system is a privileged heterocyclic moiety with distinct biological properties. This study presents an efficient strategy for the synthesis of quinazolin-4(3H)-one using substituted 2-amino benzamide with dimethyl sulfoxide as a carbon source and hydrogen peroxide as an oxidant.
Article
Pharmacology & Pharmacy
Dominik Bakalarz, Marcin Surmiak, Xiaoxiao Yang, Dagmara Wojcik, Edyta Korbut, Zbigniew Sliwowski, Grzegorz Ginter, Grzegorz Buszewicz, Tomasz Brzozowski, Jakub Cieszkowski, Urszula Glowacka, Katarzyna Magierowska, Zhixiang Pan, Binghe Wang, Marcin Magierowski
Summary: Metal-based carbon monoxide (CO)-releasing molecules have shown anti-inflammatory and anti-oxidative properties in maintaining gastric mucosal integrity. This study investigates the protective effects of a metal-free CO-based therapeutic, BW-CO-111, in rat models of gastric damage induced by necrotic ethanol or aspirin. Results suggest that BW-CO-111 could increase gastric mucosal CO content, reduce gastric lesions area, and improve gastric blood flow, with potential different mechanisms based on the specific pathomechanisms in each model.
ACTA PHARMACEUTICA SINICA B
(2021)
Review
Pharmacology & Pharmacy
Xiaoxiao Yang, Wen Lu, Christopher P. Hopper, Bowen Ke, Binghe Wang
Summary: The article highlights the critical roles of gaseous molecules in sustaining life and focuses on carbon monoxide as an endogenously produced signaling molecule with unique pharmacological effects. The review delves into the sophistication of CO-mediated signaling and its potential therapeutic applications.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Chemistry, Analytical
Zhengnan Yuan, Xiaoxiao Yang, Yuqian Ye, Ravi Tripathi, Binghe Wang
Summary: Research shows that ruthenium-based CO-releasing molecules CORM-2 and CORM-3 can induce chemical and spectroscopic changes in various biological reagents under specific conditions, which cannot be replicated with CO-deleted CO-RMs. These CO-RMs are also capable of consuming and reducing oxidized glutathione, highlighting the importance of control experiments in the future design of experiments using Ru-based CO-RMs.
ANALYTICAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Ladie Kimberly de la Cruz, Xingyue Ji, Xiaoxiao Yang, Binghe Wang
Summary: The article discusses recent advancements in utilizing prodrug approaches for the generation of carbon monoxide, including methods for CO release and formation of fluorescent reporters, and the construction of CO delivery platforms with additional functionalities. These approaches provide new insights for precise CO delivery and assessment of therapeutic efficacy.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Ladie Kimberly de la Cruz, Nicola Bauer, Alyssa Cachuela, Wing Sze Tam, Ravi Tripathi, Xiaoxiao Yang, Binghe Wang
Summary: A low-molecular-weight, solid CO surrogate that can release 2 equiv of CO with low-power LED activation is described. This surrogate can be widely used in various palladium-catalyzed carbonylative transformations and is compatible with protocols using blue-light activation for nonactivated alkyl halides. Additionally, the photolabile CO releasing scaffold can be incorporated into polymeric materials, resulting in the creation of new materials with CO-releasing capabilities.
Article
Biochemistry & Molecular Biology
Ravi Tripathi, Abiodun Anifowose, Wen Lu, Xiaoxiao Yang, Binghe Wang
Summary: By optimizing the substituents on the two phenol hydroxyl groups, we have discovered a potent series of anthraquinone analogs that exert cytotoxicity by inducing MDM2 degradation and upregulating p53. Among them, BW-AQ-350 is the most potent compound with high cytotoxic activity.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Ru Dong, Xiaoxiao Yang, Binghe Wang, Xingyue Ji
Summary: This article explores the potential of using proximity effects and click chemistry to mutually enhance chemical biology and drug discovery, and emphasizes the importance of this mutual leveraging approach in biomimicry.
MEDICINAL RESEARCH REVIEWS
(2023)
Review
Pharmacology & Pharmacy
Shameer M. Kondengadan, Shubham Bansal, Ce Yang, Dongning Liu, Zach Fultz, Binghe Wang
Summary: Click chemistry has proven to be useful in drug delivery, but selecting the appropriate chemistry is not easy. This review provides an overview of available click reactions for pharmaceutical researchers interested in click chemistry applications. It emphasizes the analysis of reaction kinetics, concentration effects, and reaction time scales to avoid failures. The review also discusses issues like chemical stability and provides recent examples and extensive references for a better understanding of technical details.
ACTA PHARMACEUTICA SINICA B
(2023)
Article
Chemistry, Multidisciplinary
Xiaoxiao Yang, Zhengnan Yuan, Wen Lu, Ce Yang, Minjia Wang, Ravi Tripathi, Zach Fultz, Chalet Tan, Binghe Wang
Summary: Extensive studies have shown that carbon monoxide (CO) can act as an endogenous signaling molecule and have therapeutic roles. However, there is still insufficient understanding of the quantitative correlations between CO concentration and biological responses. This is due to difficulties in examining concentration-response relationships of a gaseous molecule and the lack of appropriate tools for sensitive detection and concentration determination of CO in biological systems. In this study, researchers have developed a chemical approach to design fluorescent CO probes that allow for ultra-sensitive and selective CO detection. These probes have been extensively tested in quantifying CO in blood, tissue, and cell culture, as well as in cellular imaging. The use of these probes enables researchers to study the functions of CO in a concentration-dependent manner with high sensitivity and selectivity, and the principles described can be applied in designing fluorescent probes for other small molecules.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Analytical
Dongning Liu, Xiaoxiao Yang, Binghe Wang
Summary: It is important to use reliable sources of CO and verify their ability to detect CO when developing CO probes.
ANALYTICAL CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Xiaoxiao Yang, Ravi Tripathi, Minjia Wang, Wen Lu, Abiodun Anifowose, Chalet Tan, Binghe Wang
Summary: This study investigates the use of immobilized organic CO prodrugs on silica microparticles for oral CO delivery with the aim of reducing the potential negative impact of the prodrug and carrier portion. The immobilized CO prodrug demonstrates effective activation and stable attachment to the silica microparticles, and shows anti-inflammation activity in cells and systemic CO release in mice through oral administration. This strategy could be a promising approach for treating systemic and GI-specific inflammatory conditions.
MOLECULAR PHARMACEUTICS
(2023)
Article
Chemistry, Medicinal
Zhang Li, Yongming Wang, Miao Liu, Yiyao Pan, Zihui Ni, Qingqiang Min, Binghe Wang, Hengte Ke, Xingyue Ji
Summary: Carbon monoxide has shown promise as a therapeutic agent against cancers, and this study presents a new metal-free CO prodrug that can release CO with tunable release rates in response to multiple reactive oxygen species (ROS). The prodrug exhibits pronounced tumor suppression effects in a breast tumor model, and there is a direct impact of CO release rate on its antiproliferative potency. This research provides a potential starting point for further studies on how CO release kinetics affect anticancer activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Nicola Bauer, Xiaoxiao Yang, Zhengnan Yuan, Binghe Wang
Summary: CO is an endogenous signaling molecule that can modulate immune responses and engage circadian clock components. CORM-A1, one of the commonly used CO-release molecules, shows variable CO release efficiency and rate depending on factors such as the medium used and redox environment. The significant chemical reactivity of CORM-A1 suggests caution in using it as a CO surrogate in biological studies.
Article
Medicine, Research & Experimental
Nimisha Bhattarai, Jieqiong Wang, Daniel Nguyen, Xiaoxiao Yang, Linh Helmers, Jennifer Paruch, Li Li, Yiwei Zhang, Kun Meng, Alun Wang, Janarthanan Jayawickramarajah, Binghe Wang, Shelya Zeng, Hua Lu
Summary: The study demonstrated that nanoparticle encapsulation significantly enhanced the efficacy and bioavailability of INZ-C in targeting cancer cells, while minimizing impact on normal cells. This novel approach could potentially improve the therapeutic effectiveness of INZ-C as an anti-cancer agent.
Article
Chemistry, Multidisciplinary
Zhengnan Yuan, Xiaoxiao Yang, Binghe Wang
Summary: The article discusses the pathophysiological roles of the endogenous signaling molecule carbon monoxide (CO) in cell culture and animal models, as well as the therapeutic potential of CO-releasing molecules in human diseases. Some CO-releasing molecules were found to possess catalase-like activities and radical scavenging abilities, suggesting potential applications in CO biology research.
