Article
Chemistry, Organic
Shweta Rohilla, Sadhna Shah, Vinod K. K. Singh
Summary: A copper-(II)-P,N,N-ligand catalyzed propargylic [3 +2] cycloaddition approach has been developed for the synthesis of optically enriched dihydrofuro-[3,2-c]-coumarins. The reaction utilizes propargylic esters as C2-bis-electrophiles and 4-hydroxycoumarin derivatives as C,O-bis-nucleophiles. This method was also applied to 4-hydroxy-2-quinolinones and 4-hydroxythiocoumarins, leading to the synthesis of various dihydrofuro-[3,2-c]-coumarins and their analogues with high enantioselectivities in moderate to good yields.
Article
Chemistry, Organic
Suman Rani, Devinder Kumar, Nisha Kamra, Sumit Thakral, Ajeet Singh, Payare L. Sangwan, Shashank K. Singh
Summary: A number of highly oxygenated furo[3,2-c]pyran/chromen-4-one compounds were synthesized through a one-pot reaction using easily available starting materials. The synthesized compounds were characterized using various spectroscopic techniques and screened for their anticancer and antimicrobial activities.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Stefano Zoroddu, Paola Corona, Luca Sanna, Federica Borghi, Valentina Bordoni, Battistina Asproni, Gerard A. Pinna, Luigi Bagella, Gabriele Murineddu
Summary: A library of novel 1,3,4-oxadiazole bioisosteres was synthesized and evaluated for their cytotoxic activity. Several of the new compounds showed potent anticancer activity, surpassing the previously synthesized oxadiazole compound. The nature of the selenadiazole and thiadiazole rings may play a crucial role in the antitumor activity. These compounds exhibited strong cytotoxic effects in tumor cells compared to human primary cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Ju Guo
Summary: This paper provides an up-to-date review of the structural modification and activity of bistetrahydroisoquinoline natural products, highlighting their importance as antitumor lead compounds. It offers valuable scientific references for pharmaceutical chemists engaged in developing novel antitumor agents based on such alkaloid modifications.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Ghanshyam Mali, Sushobhan Maji, Kailas Arjun Chavan, Manjari Shukla, Manish Kumar, Sudipta Bhattacharyya, Rohan D. Erande
Summary: In this study, an eco-friendly and efficient one-pot green multicomponent approach was used to synthesize functionalized trans-2,3-dihydrofuro[3,2-c]coumarins (DHFCs). The catalyst used was imidazole and water was used as the solvent under mild conditions. The developed catalytic process showed outstanding activity, productivity, and broad functional group tolerance, resulting in the synthesis of a series of newly designed DHFC and derivatives in excellent yields (72-98%). Furthermore, the synthesized DHFC derivatives were found to have the ability to bind to human serum albumin (HSA) through in silico and in vitro-based structure-activity analysis.
Article
Chemistry, Medicinal
Zengxin Qin, Mengfei Zhao, Kaixin Zhang, Masuo Goto, Kuo-Hsiung Lee, Jizhen Li
Summary: Several neo-tanshinlactone derivatives with fluorine or trifluoromethyl group were synthesized and evaluated for their antiproliferative activities, showing broad activity spectrum against human tumor lines. The results also suggested specific structures in the derivatives might play crucial roles in selective antibreast cancer activity.
CHEMISTRY OF NATURAL COMPOUNDS
(2022)
Article
Chemistry, Multidisciplinary
Masafumi Okuno, Keita Yamana, Shogo Kawamura, Kotaro Nishimura, Shodai Hino, Riku Kawasaki, Atsushi Ikeda
Summary: Tetrakis(4-aminophenyl)porphyrin and tetrakis(4-acetamidophenyl)porphyrin were dissolved in water using a polysaccharide (λ-carrageenan) as a water-solubilizing agent. The photodynamic activity of the CGN-2 complex was lower than that of the CGN-1 complex, but the selectivity index (SI) of the CGN-2 complex was higher. In vivo experiments showed that the CGN-2 complex inhibited tumor growth with higher blood retention compared to the CGN-1 complex and Photofrin.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Plant Sciences
Ming Bai, Wei Xu, Qian Li, De-Feng Liu, Tian-Ming Lv, Ning-Ning Du, Guo-Dong Yao, Bin Lin, Shao-Jiang Song, Xiao-Xiao Huang
Summary: Seventeen highly oxidized germacranolides, including twelve new compounds, were isolated from Elephantopus tomentosus, showing potential cytotoxic properties against hepatocellular carcinoma cell lines.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Chemistry, Multidisciplinary
Yan Zhang, Zhenzhi Cai, Julia Struwe, Chanchan Ma, Wangyu Zeng, Xinyi Liao, Min Xu, Lutz Ackermann
Summary: In this study, a versatile strategy for constructing challenging seven-membered rings using a 7-endo-trig cyclization initiated by a phosphorus-centered radical is reported. This approach allows for the efficient synthesis of a wide range of phosphorylated dibenzocycloheptanones in a step-economical manner. Additionally, a traceless addition/exchange strategy was devised for the preparation of dephosphorylated products at room temperature with excellent yields, enabling concise synthesis of biorelevant allocochicine derivatives.
Article
Chemistry, Multidisciplinary
Mayursinh Zala, Jwalant J. Vora, Vijay M. Khedkar
Summary: To enhance the effectiveness of antitubercular drugs, a series of novel pyrazolylpyrazoline derivatives were synthesized through a one-pot multicomponent reaction. The green synthesis method offered advantages such as simplicity and shorter reaction time. Among the compounds tested, 9i, 9k, 9l, 9o, and 9p showed the highest efficacy against Mycobacterium tuberculosis H(37)Rv. Structural determination of the newly synthesized compounds was conducted using spectral methods. Molecular docking studies revealed strong binding affinities between these compounds and the active site of mycobacterial InhA enzyme.
Article
Chemistry, Inorganic & Nuclear
Iuliana Besleaga, Iryna Stepanenko, Tatsiana Petrasheuskaya, Denisa Darvasiova, Martin Breza, Marta Hammerstad, Malgorzata A. Marc, Alexander Prado-Roller, Gabriella Spengler, Ana Popovic-Bijelic, Eva A. Enyedy, Peter Rapta, Anatoly D. Shutalev, Vladimir B. Arion
Summary: Three new thiosemicarbazones with redox-active phenolic moiety were synthesized and formed copper(II) complexes with good stability and redox activity in various conditions. Electrochemical studies confirmed metal-centered reduction and ligand-centered oxidation processes, showing potential as antiproliferative agents against cancer cells.
INORGANIC CHEMISTRY
(2021)
Article
Microbiology
Fidelia Ijeoma Uche, Xiaozhen Guo, Jude Okokon, Imran Ullah, Paul Horrocks, Joshua Boateng, Chenggang Huang, Wen-Wu Li
Summary: This study investigates the in vitro and in vivo antiplasmodial activities of BBIQ alkaloids and their analogues, showing promising results with significant anti-parasitic effects at low concentrations. Cycleanine and its semisynthetic analogues demonstrate improved potency and selectivity, with potential as leads for further drug development.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Chemistry, Multidisciplinary
Chaoyu Hu, Shengjie Wu, Fei He, Deqin Cai, Zhuojia Xu, Wenjing Ma, Yating Liu, Bangguo Wei, Tiehai Li, Kan Ding
Summary: Bioactive polysaccharides are potential target molecules for drug development, but the synthesis of branched complex polysaccharides with well-defined structures is challenging. In this study, a highly branched heptadecasaccharide moiety of a native bioactive polysaccharide from Carthamus tinctorius L. was efficiently synthesized, and its biological activity in targeting galectin-3 and inhibiting pancreatic cancer cell growth was demonstrated.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Medicinal
Xiaqiu Qiu, Yuanqing Li, Bin Yu, Jie Ren, Huidan Huang, Min Wang, Hong Ding, Zhiyu Li, Jubo Wang, Jinlei Bian
Summary: CDK9 inhibitor BAY-1143572 converted into PROTACs leads to degradation of CDK9 in acute myeloid leukemia cells, with the most potent molecule B03 showing enhanced antiproliferative activity. This enhanced activity is mediated by increased kinase inhibitory activity and apoptosis induction levels. B03 can also induce CDK9 degradation in vivo, indicating its potential as a therapeutic strategy in acute myeloid leukemia.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Cassandra Yong, Shane M. Devine, Anne-Catherine Abel, Stefan D. Tomlins, Divya Muthiah, Xuexin Gao, Richard Callaghan, Michel O. Steinmetz, Andrea E. Prota, Ben Capuano, Peter J. Scammells
Summary: Extensive research has been conducted over the past two decades to discover noscapine derivatives with improved potency. This study focused on modifications to the 1,3-benzodioxole moiety of noscapine analogues, resulting in the discovery of potent cytotoxic agents against various types of cancer. Additionally, X-ray crystallography studies provided insight into the interactions between these noscapinoids and tubulin, which will aid in the development of future noscapine derivatives with enhanced properties.
Article
Cell Biology
Yunfei Wen, Anca Chelariu-Raicu, Sujanitha Umamaheswaran, Alpa M. Nick, Elaine Stur, Pahul Hanjra, Dahai Jiang, Nicholas B. Jennings, Xiuhui Chen, Sara Corvigno, Deanna Glassman, Gabriel Lopez-Berestein, Jinsong Liu, Mien-Chie Hung, Anil K. Sood
Summary: Anti-angiogenic therapies, such as anti-VEGF antibodies, have shown promise clinically but often face adaptive resistance. Research on adaptive resistance to AVA therapy in ovarian cancer models reveals mechanisms involving endothelial p130cas, VEGFR2 cleavage, and autophagy. Targeting these pathways, such as blocking autophagy or genomic ablation of vascular p130cas, can significantly improve survival in AVA-resistant ovarian tumors, providing new strategies for overcoming adaptive resistance.
Article
Gastroenterology & Hepatology
Chenhao Zhou, Jialei Weng, Yuan Gao, Chunxiao Liu, Xiaoqiang Zhu, Qiang Zhou, Chia-Wei Li, Jialei Sun, Manar Atyah, Yong Yi, Qinghai Ye, Yi Shi, Qiongzhu Dong, Yingbin Liu, Mien-Chie Hung, Ning Ren
Summary: By analyzing immune-related genes, we identified a prognostic signature that is associated with the prognosis and immunotherapy response in hepatocellular carcinoma (HCC) patients. This signature accurately predicts overall survival rates and can assist in personalized clinical management.
JOURNAL OF CLINICAL AND TRANSLATIONAL HEPATOLOGY
(2022)
Article
Oncology
Xixi Zhao, Yongkun Wei, Yu-Yi Chu, Yintao Li, Jung-Mao Hsu, Zhou Jiang, Chunxiao Liu, Jennifer L. Hsu, Wei-Chao Chang, Riyao Yang, Li-Chuan Chan, Jingkun Qu, Shuqun Zhang, Haoqiang Ying, Dihua Yu, Mien-Chie Hung
Summary: This study reveals the role of CK2 in immunosuppression by phosphorylation and stabilization of PD-L1, and suggests CK2 inhibition as a potential immunotherapeutic approach for treating cancer.
Article
Biochemistry & Molecular Biology
Jong-Ho Cha, Li-Chuan Chan, Ying-Nai Wang, Yu-Yi Chu, Chie-Hong Wang, Heng-Huan Lee, Weiya Xia, Woei-Cherng Shyu, Shih-Ping Liu, Jun Yao, Chiung-Wen Chang, Fan-Ru Cheng, Jielin Liu, Seung-Oe Lim, Jennifer L. Hsu, Wen-Hao Yang, Gabriel N. Hortobagyi, Chunru Lin, Liuqing Yang, Dihua Yu, Long-Bin Jeng, Mien-Chie Hung
Summary: The expression of EphA10, a receptor tyrosine kinase, is associated with tumor progression and poor prognosis in several malignancies. This study demonstrates high expression levels of EphA10 in tumor regions and immune suppressive myeloid cells in the tumor microenvironment. The development of anti-EphA10 monoclonal antibodies and chimeric antigen receptor-T cell therapy targeting EphA10 shows potential as a promising strategy for patients with EphA10-positive tumors.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Riyao Yang, Linlin Sun, Ching-Fei Li, Yu-Han Wang, Weiya Xia, Boning Liu, Yu-Yi Chu, Laura Bover, Long Vien, Mien-Chie Hung
Summary: This study reports the development of two novel Gal-9-neutralizing antibodies that effectively protect human T cells from Gal-9-induced cell death and promote T cell-mediated killing of tumor cells. These findings demonstrate the potential of targeting Gal-9 for cancer immunotherapy.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Jian Tu, Zijun Huo, Yao Yu, Dandan Zhu, An Xu, Mo-Fan Huang, Ruifeng Hu, Ruoyu Wang, Julian A. Gingold, Yi-Hung Chen, Kuang-Lei Tsai, Nicolas R. Forcioli-Conti, Sarah X. L. Huang, Thomas R. Webb, Jie Su, Danielle A. Bazer, Peilin Jia, Jason T. Yustein, Lisa L. Wang, Mien-Chie Hung, Zhongming Zhao, Chad D. Huff, Jingnan Shen, Ruiying Zhao, Dung-Fang Lee
Summary: The study reveals that the spliceosome is an up-regulated target in RB1-mutant cells responding to oncogenic stress, and pRB and E2F3a coregulate spliceosomal gene expression, affecting cell proliferation and tumorigenesis. These findings suggest that the spliceosomal machinery could be a potential therapeutic vulnerability for pRB-deficient cancers.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Multidisciplinary Sciences
Yun-Long Wang, Wan-Wen Zhao, Shao-Mei Bai, Li-Li Feng, Shu-Ying Bie, Li Gong, Fang Wang, Ming-Biao Wei, Wei-Xing Feng, Xiao-Lin Pang, Cao-Litao Qin, Xin-Ke Yin, Ying-Nai Wang, Weihua Zhou, Daniel R. Wahl, Quentin Liu, Ming Chen, Mien-Chie Hung, Xiang-Bo Wan
Summary: MRNIP forms liquid-like condensates to promote DSB repair. It concentrates the MRN complex to the damaged DNA in the nucleus, accelerating DSB sensing and end resection.
NATURE COMMUNICATIONS
(2022)
Article
Chemistry, Organic
Ryosuke Shimoi, Yohei Saito, Yuta Miura, Kyoko Nakagawa-Goto
Summary: In our study, we isolated a unique quinolone alkaloid, Waltherione A (1), from a methanol extract of Melochia umbellata, along with related compounds, paliasanines A-E. Compound 1 exhibited selective cytotoxicity against A549 and MCF-7 cell lines. Through a 21-step total synthesis starting from commercially available benzosuberone, we successfully accomplished the first total synthesis of 1 and elucidated its absolute configuration.
Review
Pharmacology & Pharmacy
Diana D. Kang, Haoyuan Li, Yizhou Dong
Summary: The accelerated progress and approval of two mRNA-based vaccines for SARS-CoV-2 were unprecedented, thanks to the solid foundation of research on in vitro transcribed mRNA (IVT mRNA). Through decades of research, mRNA-based vaccines or therapeutics offer many advantages to rapidly address a broad range of applications. This article describes the advances in IVT mRNA technology, including optimization of structural components, synthesis, and different classes of IVT RNA, and emphasizes the importance of continuing to drive this technology.
ADVANCED DRUG DELIVERY REVIEWS
(2023)
Article
Multidisciplinary Sciences
Shuying Chen, Xiangang Huang, Yonger Xue, Ester Alvarez-Benedicto, Yesi Shi, Wei Chen, Seyoung Koo, Daniel J. Siegwart, Yizhou Dong, Wei Tao
Summary: mRNA vaccines have revolutionized the field of infectious disease and cancer research, offering rapid and precise immune responses. This study discusses the development and evaluation of biomaterials and nanotechnology in mRNA vaccines, highlighting their advantages over traditional vaccines. The use of nanoparticles and nanotechnology provides innovative solutions to overcome challenges in mRNA delivery and enhance the potency of vaccines.
NATURE REVIEWS METHODS PRIMERS
(2023)
Article
Oncology
Hsiao-Fan Chen, Po-Ren Hsueh, Yen-Yi Liu, Yeh Chen, Sui-Yuan Chang, Wei-Jan Wang, Chen-Shiou Wu, Ya-Min Tsai, Yu-Shu Liu, Wen-Chi Su, Yu-Chi Chou, Mien-Chie Hung
Summary: Disulfiram has shown potential as a therapy against COVID-19 by inhibiting viral replication and blocking viral entry into host cells. It has demonstrated activity against different variants of SARS-CoV-2 in molecular and cellular biology assays.
AMERICAN JOURNAL OF CANCER RESEARCH
(2022)
Article
Oncology
Shih-Han Wang, Wen-Cheng Chou, Hsiang -Chi Huang, Te-An Lee, Tzu-Chun Hsiao, Ling -Hui Wang, Ke-Bin Huang, Chun-Tse Kuo, Chi -Hong Chao, Shing-Jyh Chang, Jung -Mao Hsu, Jialei Weng, Ning Ren, Fu -An Li, Yun-Ju Lai, Chenhao Zhou, Mien-Chie Hung, Chia -Wei Li
Summary: N-linked glycosylation of proteins is a post-translational modification that protects tumor antigens from immune attack. This study explores the role of N-glycosylation of SLAMF7 in breast cancer progression and highlights the potential strategy of using ADC to enhance immunotherapeutic agents through deglycosylation.
AMERICAN JOURNAL OF CANCER RESEARCH
(2022)
Article
Oncology
Yi-Chuan Li, Hirohito Yamaguchi, Yen-Yi Liu, Kai-Cheng Hsu, Ting-Hsuan Sun, Pei-Chi Sun, Mien-Chie Hung
Summary: This article investigates the interaction between ribonuclease 1 (RNase1) and EphA4 and reveals their structure and role in cellular activation. The study suggests that electrostatic force plays a crucial role in the binding and activation of RNase1 and EphA4.
AMERICAN JOURNAL OF CANCER RESEARCH
(2022)
Article
Oncology
Chun-Te Ho, Shih-Pei Lin, Ling-Ming Tseng, Mien-Chie Hung, Shih-Chieh Hung
Summary: This study found that a mutant form of Snail reduced the expression of Src in luminal A breast cancer cells and enhanced their migration and invasion abilities, while reducing their capacity to form tumor spheres. Additionally, human luminal A breast cancer samples showed a negative correlation between Vimentin and Src expression.
AMERICAN JOURNAL OF CANCER RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Chen-Shiou Wu, Hsiu-Mei Chiang, Yeh Chen, Chung-Yu Chen, Hsiao-Fan Chen, Wen-Chi Su, Wei-Jan Wang, Yu-Chi Chou, Wei-Chao Chang, Shao-Chun Wang, Mien-Chie Hung
Summary: This research explores natural plant extracts that have the potential to combat SARS-CoV-2 and provide alternative options for prevention and disinfection. The study identifies coffee leaf extract as an effective inhibitor of SARS-CoV-2 infection in various strains. Additionally, the extract proves to be more potent at preventing viral entry into cells when applied topically than the standard disinfectant ethanol. Compounds such as caffeine, chlorogenic acid, quinic acid, and mangiferin are found to be associated with the extract's antiviral activity.
INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES
(2022)
