Article
Chemistry, Medicinal
Dong Liang, Chen Yu, Zhao Ma, Mingzhao Hu, Jiahui Wang, Xuhui Dong, Lupei Du, Minyong Li
Summary: In this study, the discovery of two series of parbendazole derivatives as tubulin inhibitors for the treatment of head and neck squamous cell carcinoma (HNSCC) was reported. Compound 9q exhibited the best pharmacological activities and pharmacokinetic properties, displaying reasonable inhibition activity on cell proliferation, induction of cell apoptosis, and suppression of cell migration and invasion.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Lingyu Shi, Shanbo Yang, Jing Chang, Yujing Zhang, Wenjing Liu, Jun Zeng, Jingsen Meng, Renshuai Zhang, Chao Wang, Dongming Xing
Summary: A series of new compounds were synthesized and evaluated for their antitumor activity as tubulin polymerization inhibitors. Compound 7k showed the strongest anti-proliferative activity and could block the cell cycle and induce apoptosis.
FRONTIERS IN CHEMISTRY
(2022)
Article
Medicine, Research & Experimental
In-ho Song, Su Jeong Park, Gyu Seong Yeom, Keum-soo Song, Taisun Kim, Satish Balasaheb Nimse
Summary: In recent years, there has been significant interest in developing microtubule-targeting agents (MTAs) as novel small-molecule anticancer drugs. Most research on benzimidazole scaffold-based MTAs has focused on developing microtubule-destabilizing agents, with little focus on microtubule-stabilizing agents. In this study, benzimidazole derivatives NI-11 and NI-18 were found to exhibit profound anticancer activity as microtubule-stabilization agents. They showed higher selectivity indexes compared to currently available anticancer agents, inhibited cancer cell motility and migration, and induced early phase apoptosis. The compounds also upregulated DeY-alpha-tubulin expression and downregulated Ac-a-tubulin expression in cancer cells, indicating their microtubule-stabilizing activity.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Chemistry, Medicinal
Cheng-Jun Wu, Jia-Qiang Wu, Yunfei Hu, Suyun Pu, Yuying Lin, Zimai Zeng, Jinhui Hu, Wen-Hua Chen
Summary: A series of novel microtubulin polymerization inhibitors based on indole were designed and synthesized, among which compound 12d exhibited the highest antiproliferative activity by inducing cellular apoptosis, cell cycle arrest, and inhibiting tubulin polymerization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Baoxia Liang, Qing Zou, Lintao Yu, Yali Wang, Jun Yan, Baiqi Huang
Summary: Novel indole-containing hybrids derived from Millepachine were synthesized and evaluated for their antitumor activities. Compound 14b showed the most potent cytotoxic activity against human cancer cell lines, being almost 100 times more active than Millepachine. It also demonstrated low cytotoxicity towards normal human cells and equivalent sensitivity towards drug-resistant cells, highlighting its potential for the development of antitumor drugs.
Article
Chemistry, Multidisciplinary
Dalal Sulaiman Alshaya, Rana M. O. Tawakul, Islam Zaki, Ali H. Abu Almaaty, Eman Fayad, Yasmin M. Abd El-Aziz
Summary: A new series of acrylic acid and acrylate ester derivatives were synthesized and evaluated for their antiproliferative activity against MCF-7 breast carcinoma cells. Methyl acrylate ester 6e showed the highest cytotoxicity with an IC50 value of 2.57 +/- 0.16 mu M and exhibited inhibition of beta-tubulin polymerization. Compound 6e arrested MCF-7 cells at the G2/M phase and enhanced apoptotic power, while also affecting the gene expression levels of p53, Bax, and Bcl-2.
Article
Chemistry, Multidisciplinary
Guangcheng Wang, Min He, Wenjing Liu, Meiyan Fan, Yongjun Li, Zhiyun Peng
Summary: A series of new 2-phenyl-4,5,6,7-tetrahydro-1H-indole derivatives were synthesized and evaluated for their anti-proliferative activities, with one compound showing the most potent anticancer activity against breast cancer and lung cancer cells while sparing normal liver cells. Mechanism studies revealed that the compound arrested cell cycle and induced apoptosis, and effectively inhibited tubulin polymerization with an inhibitory mechanism similar to colchicine. Molecular docking studies indicated high binding affinities for the colchicine binding pocket of tubulin, suggesting potential as new tubulin polymerization inhibitors.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Xiang-Yu Yan, Jia-Fu Leng, Ting-Ting Chen, Yong-Jun Zhao, Ling-Yi Kong, Yong Yin
Summary: A series of novel diphenylamine derivatives were synthesized and evaluated for their anti-proliferative activities against human cancer cell lines. Among them, compound 5f exhibited promising anti-proliferative activity against HT29 cells and showed inhibitory effects on cancer cell migration, colony formation, and angiogenesis. Further studies revealed that compound 5f inhibited tubulin polymerization, arrested HT29 cell cycle, induced cell apoptosis, and inhibited tumor growth in animal models. The compound also demonstrated good pharmacokinetic properties. These findings suggest that compound 5f has potential as an antitumor candidate and warrants further investigation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
N. Perin, L. Hok, A. Bec, L. Persoons, E. Vanstreels, D. Daelemans, R. Vianello, M. Hranjec
Summary: In this study, novel N-substituted benzimidazole-based acrylonitriles were designed, synthesized, and evaluated for their antiproliferative activity. The N,N-dimethylamino substituted acrylonitriles exhibited strong and selective antiproliferative activity with low toxicity. Mechanism of action studies revealed that the most active compounds inhibited tubulin polymerization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ashish Ranjan Dwivedi, Suraj Singh Rawat, Vijay Kumar, Naveen Kumar, Piyush Anand, Ravi Prakash Yadav, Somesh Baranwal, Amit Prasad, Vinod Kumar
Summary: In this study, 16 novel compounds were synthesized and evaluated for their anticancer activity. It was found that two of the compounds exhibited inhibitory effects on cancer cell proliferation and induced mitochondria-mediated apoptosis. Additionally, one of the compounds showed significant tubulin polymerization inhibition activity. Computational studies revealed that this compound had good binding affinities in the colchicine domain and thermodynamic stability. Therefore, these compounds have the potential to be developed as potent anticancer agents.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Sara Rahimzadeh Oskuei, Salimeh Mirzaei, Mohammad Reza Jafari-Nik, Farzin Hadizadeh, Farhad Eisvand, Fatemeh Mosaffa, Razieh Ghodsi
Summary: The novel imidazole-chalcone derivatives showed potent cytotoxicity against human cancer cell lines, particularly A549 cells, inducing cell cycle arrest at the G2/M phase at low concentrations and increasing apoptotic cells at higher concentrations. They also inhibited tubulin polymerization and induced apoptosis in A549 cells, presenting potential interactions with tubulin as indicated by molecular docking studies.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Yuchen Tan, Han Hu, Wenjian Zhu, Tao Wang, Tian Gao, Hongqi Wang, Jian Chen, Jinyi Xu, Shengtao Xu, Huajian Zhu
Summary: A series of novel dihydroquinolin-4(1H)-one derivatives were synthesized and evaluated for their anticancer activity. The most potent compound 6t showed remarkable antiproliferative activities, inhibited tubulin polymerization, and inhibited tumor growth in vitro and in vivo.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Medicine, Research & Experimental
Filip Borys, Piotr Tobiasz, Marcin Poterala, Hanna Krawczyk
Summary: This review provides a brief overview of new compounds targeting the dynamic of microtubule-tubulin polymerization/depolymerization. It is divided into three parts focusing on derivatives of stilbene, photoswitchable inhibitors, and macrocyclic compounds as tubulin inhibitors. The authors primarily highlight reports from the past five years and the latest strategies in this field.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Chemistry, Medicinal
Hui Wu, Long-Shan Wang, Pei Li, Jia Yu, Sha Cheng, Gang Yu, Mashaal Ahmad, Xue-Ling Meng, Heng Luo, Bi-Xue Xu
Summary: A series of new N-aryl-2-trifluoromethylquinazoline-4-amine analogs were synthesized and their structures were confirmed. The anti-cancer activity of these compounds against different cancer cell lines was evaluated. Some of these compounds showed stronger growth inhibitory activity on certain cancer cells compared to positive controls. These compounds inhibited tubulin polymerization and disrupted cellular microtubule networks, leading to cell cycle arrest and cell apoptosis. These findings suggest that these compounds can be potential lead compounds for anti-leukemia agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Sarah H. M. Khairat, Mohamed A. Omar, Fatma A. F. Ragab, Sonam Roy, Ahmad A. Turab Naqvi, Ahmed S. Abdelsamie, Anna K. H. Hirsch, Shadia A. Galal, Md Imtaiyaz Hassan, Hoda El Diwani
Summary: A novel series of benzimidazoles was synthesized and evaluated as SphK1 inhibitors, with most compounds showing effective inhibition against SphK1 and compound 41 standing out as the most potent one. Molecular docking revealed the potential of these compounds to fit well into the ATP-binding site of SphK1 and form hydrogen bond interactions with catalytically important residues, suggesting their therapeutic potential in the clinical management of SphK1-associated diseases.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Multidisciplinary
Jian Wu, Chenwen Shao, Xiaolian Ye, Xiaojiao Di, Dongdong Li, Hu Zhao, Bing Zhang, Guiquan Chen, Hong-Ke Liu, Yong Qian
Summary: This study introduces a novel near-infrared fluorescent probe named CAQ for selective monitoring of A beta aggregates in vivo, which shows promise in providing comprehensive information for neurodegenerative disease research, promoting a deeper understanding of Alzheimer's pathological processes.
Article
Chemistry, Applied
Jian-Fei Xu, Jin Gu, Ya-Lin Qi, Meng Zhang, Jian Chen, Dong-Dong Li, Yu-Shun Yang, Peng-Cheng Lv, Hai-Liang Zhu
Summary: The novel rotor P7-B with an improved auxochromic dynamic motor of azepanyl showed comparable targeting capability and better auxochroming potential for monitoring lysosomal viscosity. This work not only provides practical tools for lysosomal viscosity monitoring, but also significant information for transcending structural limits in future investigations.
Article
Chemistry, Analytical
Xiao-Wei Hu, Mei-Hui Zhang, Jia-Yi Cheng, Ruo-Jun Man, Dong-Dong Li
Summary: The study developed a fluorescent probe BER9-HZ for detecting hydrazine in real samples, which showed excellent performance including wide linear range, high sensitivity, stability, and selectivity. The probe could work steadily in various samples and provide useful information for future investigations on Nitrogen circulation.
ANALYTICA CHIMICA ACTA
(2021)
Article
Biotechnology & Applied Microbiology
Qi Li, Xinyi Tong, Yunpeng Jiang, Dongdong Li, Linguo Zhao
Summary: This study successfully enhanced the xylose tolerance of GH39 family beta-xylosidase Xln-DT through gene mutation, significantly improving its activity and thermal stability.
ENZYME AND MICROBIAL TECHNOLOGY
(2021)
Review
Chemistry, Medicinal
Yuan Kong, Lin Li, Lin-Guo Zhao, Pan Yu, Dong-Dong Li
Summary: Berberine, as an important compound with various pharmacological activities, has great potential for optimization in drug development. However, the lack of research on the biomolecular targets of berberine restricts its development in the pharmaceutical field. Consideration of poor bioavailability and cytotoxicity issues is also important in the development of berberine-based drugs.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2022)
Article
Chemistry, Physical
Hua Zhang, Ting Xu, Dongdong Li, Tao Cheng, Jing Chen, Yang Zhou
Summary: A novel series of bis Indy-NHC gold complexes were developed and investigated via a mild Agcarbene transfer route. The catalytic properties of these complexes, especially gold complex E1, showed high catalytic activity in the oxidation of various benzylic substrates with excellent yields using TBHP as oxidant.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Multidisciplinary Sciences
Tingting Wu, Lihu Zhang, Dongdong Li, Tao Wu, Yan Jiang, Linguo Zhao
Summary: The incidence of bronchitis has been increasing with global environmental deterioration and air pollution, resulting in a rapid growth in anti-bronchitis drug sales. Research suggests that Ginkgo seeds may have the potential to treat bronchitis, and the mechanism of action is being investigated through various molecular networks such as active ingredients-targets and proteins interactions.
Article
Biochemistry & Molecular Biology
Yuan Kong, Yong-Jia Yi, Xiao-Qing Liu, Pan Yu, Lin-Guo Zhao, Dong-Dong Li
Summary: In this study, a series of berberine analogs were synthesized and evaluated for their lipid-lowering activities. Compound 1m was found to exhibit potent cholesterol inhibitory activity and had significant effects on LDLC and HDLC levels. The results suggest that 1m has the potential to be a new lipid-lowering agent.
BIOORGANIC CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Zhu-Gui Zhou, Dong-Dong Li, Ying Chen, Xi Chen, Ruo-Jun Man
Summary: Flavonoids are secondary metabolites of plants with complex molecular structures. They have various biological activities in nature, but their bioavailability is limited due to poor solubility and stability. Modifying their structure through drug design methods gives them special properties. Flavonoids have broad application prospects in tumor treatment and other areas.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Article
Engineering, Environmental
Changhui Wang, Zheng Hao, Chenghao Huang, Qianhong Wang, Zaisheng Yan, Leilei Bai, Helong Jiang, Dongdong Li
Summary: A novel recycling method using drinking water treatment residue (DWTR) is proposed in this study, which was shown to be highly feasible for simultaneously controlling PAHs and phosphorus pollution in sediment.
JOURNAL OF HAZARDOUS MATERIALS
(2022)
Article
Chemistry, Physical
Lin-Guo Zhao, Dong-Dong Li, Xiao-Qing Liu, Yong-Jia Yi, Yuan Kong, Pan Yu
Summary: The study trained twelve EGFR consensus scoring models, with the best model 3 showing acceptable statistical parameters and potent scoring power for various types of EGFR inhibitors, making it suitable for large-scale virtual screening.
CHEMICAL PHYSICS LETTERS
(2022)
Article
Chemistry, Applied
Yuan Kong, Qi-Qi Xing, Yu-Xuan Tian, Lin Li, Pan Yu, Lin-Guo Zhao, Dong-Dong Li
Summary: This study designed and synthesized a series of cinnamoylberberine and cinnamoyltetrahydroberberine derivatives and evaluated their lipid-lowering activity. Two promising candidate molecules (5p and 7u) were discovered and showed potential as new lipid-lowering agents for further investigation.
NATURAL PRODUCT RESEARCH
(2023)
Article
Chemistry, Analytical
Yumeng Song, Xueting Wang, Huan Liu, Xueao Wang, Dongdong Li, Hai-Liang Zhu, Yong Qian
Summary: A selective fluorescent probe, AgP, was developed for convenient and rapid detection of silver ions in vitro and in vivo. AgP exhibits stable detection of Ag+ with a wide measurement range and a quench-type fluorescence response. It can be directly used for colorimetric detection in aqueous samples and is suitable for in vivo imaging in plants. This probe provides a new tool for studying the distribution of Ag+ in the environment and live plants.
Article
Materials Science, Multidisciplinary
Shuai-Jun Guo, Hao-Yun Chang, Meng-Jia Xu, Chen-Xu Wang, Hua Wei, Dong-Dong Li, Jing Chen, Yang Zhou, Yi Liu
Summary: This research presents a facile one-step fabrication method for poly(sodium methacrylate-co- vinylimidazole)-Co2+ hydrogels with high mechanical strength, good elasticity, and excellent sensitivity. The hydrogels can be used to manufacture wearable strain sensors and have been proven effective in monitoring human motion. Additionally, the hydrogels can be used to construct a pressure distribution sensor array for the early detection and clinical diagnosis of foot-related disorders.
ACS APPLIED POLYMER MATERIALS
(2022)
Article
Energy & Fuels
Pingping Qu, Dongdong Li, Raudah Lazim, Rui Xu, Dunchi Xiao, Fei Wang, Xun Li, Yu Zhang
Summary: The thermostability of Thermomyces lanuginosus lipase was improved through molecular dynamics simulation and in silico mutation prediction. The engineered G91C mutant showed enhanced catalytic efficiency and increased biodiesel yield at high temperatures.