Article
Chemistry, Multidisciplinary
Leila Emami, Soghra Khabnadideh, Zahra Faghih, Farnoosh Farahvasi, Fatemeh Zonobi, Saman Zare Gheshlaghi, Shadi Daili, Ali Ebrahimi, Zeinab Faghih
Summary: A series of quinazolinone derivatives were synthesized as antiproliferative agents and evaluated for their structure and cytotoxic activity. Molecular docking studies confirmed their potential anticancer activity and most of the compounds fulfilled drug design rules. With further modification, these compounds could be promising antiproliferative agents.
Article
Chemistry, Medicinal
Bin Zhang, Zhikun Liu, Shengjin Xia, Qingqing Liu, Shaohua Gou
Summary: Multi-target, especially dual-target, drug design is a popular research field in cancer treatment. This study developed quinazoline derivatives as dual EGFR/CAIX inhibitors, with compound 8v showing potent anticancer activity against mutant-type lung cancer cells, especially under hypoxic conditions. Mechanism studies revealed that 8v exhibited strong inhibitory effects on both EGFR(T790M) and CAIX enzymes, making it a promising candidate for further research in cancer therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Shengchao Zhou, Kun Wang, Ziwei Hu, Tao Chen, Yao Dong, Rongmei Gao, Mengyuan Wu, Yuhuan Li, Xingyue Ji
Summary: This study identified a series of quinazoline derivatives with potent antiviral activity against coronavirus through screening of a compound library. The derivatives showed high selectivity and could be potentially used for further development of antiviral drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Bin Zhang, Zichen Xu, Qingqing Liu, Shengjin Xia, Zhikun Liu, Zhixin Liao, Shaohua Gou
Summary: This study focused on designing and synthesizing three series of EGFR inhibitors, among which compound 7g showed high potency against mutant-type H1975 cells and excellent inhibitory effect on EGFR(T790M) enzyme, potentially overcoming resistance.
BIOORGANIC CHEMISTRY
(2021)
Article
Infectious Diseases
Fan-Fei Meng, Ming-Hao Shang, Wei Wei, Zhen-Wu Yu, Jun-Lian Liu, Zheng-Ming Li, Zhong-Wen Wang, Jian-Guo Wang, Huan-Qin Dai
Summary: MRSA is a global health threat and new antibacterial agents are urgently needed. In this study, 21 novel sulfonylurea derivatives were designed and synthesized, and nine compounds showed inhibitory activities against MRSA. Compound 9i and 9q exhibited the lowest minimum inhibitory concentrations against MRSA, surpassing the positive controls vancomycin and methicillin. This is the first time that sulfonylurea derivatives have been identified as promising inhibitors against different MRSA clinical isolates. Additionally, all the synthesized compounds showed minimal inhibitory concentrations greater than 100μg/mL against Candida albicans.
Article
Biochemistry & Molecular Biology
Jinbao Xiang, Yuji Wang, Wanhe Wang, Jianxin Yu, Lianyou Zheng, Yuan Hong, Lingling Shi, Chunling Zhang, Na Chen, Jia Xu, Xuelian Gong, Zhuoqi Zhang, Hongming Cui, Qian Zhou, Dapeng Zhang, Yanjun Liu, Ying Ke, Jingkang Shen, Guangxin Xia, Xu Bai
Summary: We report the design, synthesis, and structure-activity relationships (SARs) of a series of novel quinazoline derivatives as JAK inhibitors. Among these inhibitors, compound 11n showed high potency against JAKs (JAK1/JAK2/JAK3/TYK2, IC50 = 0.40, 0.83, 2.10, 1.95 nM), desirable metabolic characters, and excellent pharmacokinetic properties. In collagen-induced arthritis (CIA) models, compound 11n exhibited significant reduction in joint swelling with good safety, which could be served as a potential therapeutic candidate for the treatment of inflammatory diseases.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Zhenxi Niu, Shuli Ma, Lei Zhang, Qibing Liu, Shengnan Zhang
Summary: A novel series of quinazoline derivatives were designed and synthesized, and compound 18 showed potent antitumor activity and selectivity against MGC-803 cells, with low micromolar cytotoxicity and inhibition of tumor growth.
Article
Chemistry, Multidisciplinary
Jing Pan, Long Ma, Yu-Xia Tang, Ying Tian, Yi-Hang Lin, Long-Jiang Zhang, Feng Gao, Guang-Ming Lu
Summary: A series of novel 4-aminoquinazoline derivatives were designed, synthesized, and evaluated for their inhibitory activity on the NF-Kb pathway and potential anti-proliferative effects on breast cancer cells in vitro. Compound LU1501 exhibited potent inhibition and showed a correlation between its anticancer activity and proliferation inhibition through the NF-Kb signal pathway in vivo.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Nader M. Boshta, Farag A. El-Essawy, Mohammed B. Alshammari, Safaa G. Noreldein, Osama M. Darwesh
Summary: This paper reports on the design and synthesis of a novel series of quinazoline-2,4(1H,3H)-dione derivatives as fluoroquinolone-like inhibitors of bacterial gyrase and DNA topoisomerase IV. The compounds were evaluated for their antimicrobial activities and compared with standard drugs. Compound 13 and 15 showed broad bioactive spectrum against Gram-positive and Gram-negative strains, making them the most promising candidates.
Article
Biochemistry & Molecular Biology
Yu-Chieh Wu, Meng-Tien Lu, Tai-Hui Lin, Po-Chen Chu, Chih-Shiang Chang
Summary: This study designed, synthesized, and evaluated a series of biarylquinoline derivatives as potential HIF-1α inhibitors based on structure-activity relationship. Compound 7f exhibited the best inhibitory effects on cell viability and hypoxia-induced migration, potentially by suppressing HIF-1α expression through blocking transcription and protein translation, and concomitantly inhibiting multiple signaling pathways.
BIOORGANIC CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
M. S. Raghu, H. A. Swarup, T. Shamala, B. S. Prathibha, K. Yogesh Kumar, Fahd Alharethy, M. K. Prashanth, Byong-Hun Jeon
Summary: The in vitro anticancer efficacy of a new series of quinazoline-based thiazole derivatives was explored. The synthesized compounds showed moderate to significant cytotoxic impact and were more effective than the widely used drug erlotinib in some cases. Compounds 4i and 4j were identified as potential candidates with higher anticancer activity for future research and design of more potent and selective EGFR kinase inhibitors.
Article
Chemistry, Inorganic & Nuclear
Li Hong-Xia, Qian Yu-Mei, Xu Li-Sheng
Summary: This study focused on designing and synthesizing a series of quinazoline derivatives targeting EGFR, evaluating their anticancer activity and apoptosis-inducing capacity on various tumor cell lines. The results showed that compound 4a exhibited the strongest anticancer activity and apoptosis-inducing ability, indicating its potential as a promising anticancer drug targeting EGFR.
CHINESE JOURNAL OF STRUCTURAL CHEMISTRY
(2021)
Review
Infectious Diseases
Zeinab Breijyeh, Rafik Karaman
Summary: The need for innovative antimicrobials has increased due to the spread of multidrug-resistant bacteria. Overuse, abuse, and misuse of antibiotics are linked to antibiotic resistance. This paper reviews various approaches to develop novel classes of antibiotics with no pre-existing resistance in bacterial pathogens. These include nanotechnology, computational methods, antibiotic alternatives, drug repurposing, synthesis of novel antibacterial agents, and prodrugs. Regulations, public education, research, and technological advancements are crucial in combating antibiotic resistance.
Article
Agronomy
Guangkai Yao, Mengfan Wang, Benjie Li, Hongxiang Peng, Shuai Yang, Chen Zhao, Hanhong Xu
Summary: This study designed and synthesized a series of new spiro-pyrazolo[1,5-a]quinazoline derivatives, which exhibited good insecticidal activity and low toxicity to honeybees.
PEST MANAGEMENT SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Andrey Smolobochkin, Almir S. Gazizov, Lola J. Yakhshilikova, Dmitrii D. Bekrenev, Alexander R. Burilov, Michail A. Pudovik, Anna P. Lyubina, Syumbelya K. Amerhanova, Alexandra D. Voloshina
Summary: A series of novel taurine-derived compounds with antibacterial and antifungal activity were synthesized using a modular three-stage approach. Some of the synthesized compounds showed higher activity and bactericidal effect, making them promising candidates for further studies.
CHEMISTRY & BIODIVERSITY
(2022)
