Review
Biochemistry & Molecular Biology
Yu-Qing Zhao, Xiaoting Li, Hong-Yan Guo, Qing-Kun Shen, Zhe-Shan Quan, Tian Luan
Summary: This review summarizes the medicinal chemistry of quinoline-modified natural product derivatives developed by several research teams in the past 10 years and finds that these compounds have inhibitory effects on various diseases.
Article
Chemistry, Medicinal
Hairong Tang, Aisong Yu, Li Xing, Xiaoyu Chen, Huaqian Ding, Hong Yang, Zilan Song, Qiongyu Shi, Meiyu Geng, Xun Huang, Ao Zhang
Summary: Researchers conducted structural optimization based on the quinoline-5,8-dione scaffold and synthesized compound 15a, a potent NSD2 inhibitor. Compound 15a demonstrated high NSD2 inhibitory activity, strong anti-proliferative effects, and favorable pharmacokinetic properties. Additionally, it exhibited significant antitumor efficacy with desirable safety profile in multiple myeloma xenograft mice models, making it a promising candidate for further investigation.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Vineetha Telma D'Souza, Janardhana Nayak, Desmond Edward D'Mello, P. Dayananda
Summary: Triazoles and quinoline compounds have been well studied for their biological activities. In this study, a novel series of compounds were synthesized and screened for antimicrobial activities, with some showing significantly higher bioactivities compared to normal drugs.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Na Li, Jingru Song, Dianpeng Li
Summary: By modifying the mogrol core with ester derivatives, the antiproliferative activity against human cancer cells was significantly enhanced, with some derivatives showing even higher activity than the positive drug. The cytotoxicity of certain derivatives was much more potent than the control drug, indicating promising anticancer potential.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
Israa A. Seliem, Siva S. Panda, Adel S. Girgis, Yassmin Moatasim, Ahmed Kandeil, Ahmed Mostafa, Mohamed A. Ali, Eman S. Nossier, Fatma Rasslan, Aladdin M. Srour, Rajeev Sakhuja, Tarek S. Ibrahim, Zakaria K. M. Abdel-samii, Amany M. M. Al-Mahmoudy
Summary: Novel small molecules with quinoline scaffolds were synthesized and assessed for their anti-SARS-CoV2 activity, with compounds 10g and 12c showing high potency and significant efficacy in comparison to reference drugs.
BIOORGANIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
He Li, Linling Liu, Hong-ying Chen, Ru-li Li, Jie Lan, Kun-yue Xue, Xue Li, Cai-li Zhuo, Lan Lin, Ling-yu Li, Zhuang Wu, Die Zhang, Xue-mei Wang, Wen-jing Huang, Yingling Wang, Wei Jiang, Liming Zhou
Summary: Mogrol, a chemotherapy drug, effectively suppresses lung cancer cells by inducing excessive autophagy and autophagic cell death via activating the AMPK signaling pathway, as well as cell cycle arrest and apoptosis via activating the p53 pathway.
TOXICOLOGY AND APPLIED PHARMACOLOGY
(2022)
Review
Cell Biology
Heng Wee Tan, Yan-Ming Xu, San-Hai Qin, Guo-Feng Chen, Andy T. Y. Lau
Summary: Lung cancer is the leading cause of cancer-related deaths worldwide, with angiogenesis playing a crucial role in the growth and metastasis of lung cancer cells. While genetic regulation of angiogenesis in lung cancer is extensively studied, relatively less is known about the epigenetic regulation. Epigenetic alterations, including DNA epimodifications, histone posttranslational modifications, and noncoding RNA expression, contribute to regulating angiogenesis in lung cancer. In the future, epigenetic-based therapy is likely to emerge as a prominent approach for treating lung cancer.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Sunil Kumar, Sounok Sengupta, Iqra Ali, Manoj K. Gupta, H. Lalhlenmawia, Shavkatjon Azizov, Deepak Kumar
Summary: The purpose of this study was to find a novel anticancer agent that inhibits EGFR and reduces the chances of lung cancer. A series of triazole-substituted quinazoline hybrid compounds were designed and docked against five different crystallographic EGFR TKDs. Molecule-19 showed significant affinity and good pharmacokinetic properties, making it a potential EGFR inhibitor.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Hoda Jamshidi, Mohammad Reza Naimi-Jamal, Maliheh Safavi, Kimia RayatSanati, Parisa Azerang, Azar Tahghighi
Summary: A series of 1,2,3-triazole-based polyaromatic compounds containing chloroquinoline moiety were synthesized using click chemistry and showed promising antimicrobial and antifungal activities.
CHEMICAL BIOLOGY & DRUG DESIGN
(2022)
Review
Radiology, Nuclear Medicine & Medical Imaging
Guangyao Wu, Arthur Jochems, Turkey Refaee, Abdalla Ibrahim, Chenggong Yan, Sebastian Sanduleanu, Henry C. Woodruff, Philippe Lambin
Summary: Radiomics plays a crucial role in the detection, diagnosis, and prediction of lung cancer, covering pathology, gene mutation, treatment strategy, follow-up, treatment response evaluation, and prognosis. However, challenges such as limited large datasets, methodology standardization, the black-box nature of deep learning, and reproducibility need to be addressed for the clinical implementation of radiomics. Future directions include developing a safer and more efficient model training mode, merging multi-modality images, and combining multi-discipline or multi-omics to form Medomics.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2021)
Article
Biochemistry & Molecular Biology
Heba A. Hofny, Mamdouh F. A. Mohamed, Hesham A. M. Gomaa, Salah A. Abdel-Aziz, Bahaa G. M. Youssif, Nawal A. El-koussi, Ahmed S. Aboraia
Summary: New quinoline-1,3,4-oxadiazole and quinoline-1,2,4-triazole hybrids were developed and tested for their activity against DNA gyrase and topoisomerase IV. Some compounds showed strong antibacterial activity without cytotoxic effects, and molecular docking analysis was performed to investigate their binding mode and interactions with the enzymes.
BIOORGANIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Haodong Hou, Bin Qu, Chen Su, Guihua Hou, Feng Gao
Summary: The designed and synthesized hybrids showed higher antiproliferative activity against lung cancer cell lines compared to the parent drug, while exhibiting no cytotoxicity towards normal cells. The structure-activity relationships revealed the significant influence of substituents on the isatin moiety on the activity of the hybrids.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Arif Khan, Fatima Naaz, Rafia Basit, Deepak Das, Piyush Bisht, Majeed Shaikh, Bilal Ahmad Lone, Yuba Raj Pokharel, Qazi Naveed Ahmed, Shazia Parveen, Intzar Ali, Shashank Kumar Singh, Gousia Chashoo, Syed Shafi
Summary: A series of novel 1,2,3-triazole derivatives of capsaicin, including a new natural product hybrid capsaicinoid, were synthesized. Most of the synthesized compounds showed antiproliferative activity against various cancer cell lines, with lung cancer cell lines being the most sensitive. Compound 18f demonstrated the best antiproliferative activity and acted through inducing cell apoptosis and altering mitochondrial membrane potential.
Review
Chemistry, Medicinal
Isabela A. Graciano, Alcione S. de Carvalho, Fernando de Carvalho da Silva, Vitor F. Ferreira
Summary: This review highlights recent advances in the biological activities of new 1,2,3-triazole-and quinoline-based hybrids and their role in the development of new biologically active substances. It focuses on the synthetic methods used for the synthesis of hybrid 1,2,3-triazoles with quinoline nuclei. The quinoline nucleus and the 1,2,3-triazole heterocycle have both shown potential as scaffolds for new drugs, but only a few triazoles have been approved for market use. Many studies are being conducted to develop new substances that can overcome resistance developed by the malaria parasite.
MEDICINAL CHEMISTRY
(2022)
Article
Materials Science, Multidisciplinary
Yu Yang, Guoqing Wang, Longlin Lei, Yangkai Xiong, Zhiqiang Fang, Lei Huang, Jinbo Liu, Daxiong Hu, Jianhe Liao
Summary: This paper presents a new antibacterial nanofiller, triazole fluoroaromatic hydrocarbon-modified nano-zinc oxide, which can be mixed with zinc acrylate resin to produce a low surface energy antifouling coating. The coating exhibits a high bactericidal rate and is expected to be widely used in the field of marine antifouling.
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
