Article
Oncology
Yuhang Bao, Xiuxian Wu, Xinghua Jin, Akihiro Kanematsu, Michio Nojima, Yoshiyuki Kakehi, Shingo Yamamoto
Summary: Apigenin has inhibitory effects on renal cell carcinoma (RCC), suppressing cell growth and inducing cell cycle arrest. It shows potential as a novel therapeutic strategy for RCC treatment due to its anticancer activity and ability to modulate the cell cycle.
Article
Oncology
Hanan R. H. Mohamed, Maria M. H. Ibrahim, Ayman Diab
Summary: The study found that CaTiO3-NPs induced cytotoxicity, genomic instability, and apoptosis in human MCF-7 cells. These effects were time- and concentration-dependent.
CANCER CELL INTERNATIONAL
(2022)
Article
Biochemistry & Molecular Biology
Aso Hameed Hasan, Sonam Shakya, Faiq H. S. Hussain, Sankaranarayanan Murugesan, Subhash Chander, Mohammad Rizki Fadhil Pratama, Shajarahtunnur Jamil, Basundhara Das, Subhrajit Biswas, Joazaizulfazli Jamalis
Summary: Acetylcholinesterase inhibitors are commonly prescribed medications for the treatment of Alzheimer's disease and dementia. In this study, a series of novel compounds were designed, synthesized, and tested for their ability to inhibit acetylcholinesterase activity. The results showed that these compounds exhibited significant inhibition and low cytotoxicity.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Darja Koutova, Radim Havelek, Eva Peterova, Darina Muthna, Karel Kralovec, Katerina Breiterova, Lucie Cahlikova, Martina Rezacova
Summary: Pancracine, a potent compound among natural isoquinolines, exhibited strong antiproliferative activity on A549 cells and induced apoptotic cell death in MOLT-4 cells. The mechanistic understanding of pancracine activity in vitro revealed perturbation of the cell cycle and induction of apoptotic cell death as key mechanisms.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Environmental Sciences
Ozgur Vatan
Summary: This study investigated the effects of Fe-Ni ANP exposure on human health at the cellular level. The results showed that Fe-Ni ANPs had cytotoxic and genotoxic potentials, and exerted their effects through apoptotic pathways and cell cycle arrest mechanisms. Additionally, the increased intracellular ROS was identified as the primary mechanism leading to cytotoxic, genotoxic, and apoptotic activity. These findings further demonstrated the potential risks of Fe-Ni ANPs to human health.
Article
Chemistry, Multidisciplinary
Eman M. Radwan, Eman Abo-Elabass, Atef E. Abd El-Baky, Hussah Abdullah Alshwyeh, Riyad A. Almaimani, Ghassan Almaimani, Ibrahim Abdel Aziz Ibrahim, Abdulaziz Albogami, Mariusz Jaremko, Samar Z. Alshawwa, Essa M. Saied
Summary: This study designed, synthesized, and characterized a new class of N-(substituted phenyl)-8-methoxycoumarin-3-carboxamide analogues. The synthesized compounds showed significant cytotoxicity against Hep-G2 cells with low impact on normal cells. Compound 7 exhibited the most potent cytotoxic effect, inducing cell cycle arrest and apoptosis in Hep-G2 cells. Additionally, compound 7 displayed dual inhibitory activity against cytochrome P450 and VEGFR-2 proteins. These findings suggest that the newly synthesized compounds, particularly compound 7, hold promise as effective anticancer agents against liver cancer.
FRONTIERS IN CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Fawzia F. Albalawi, Mohammed A. A. El-Nassag, Raafat A. El-Eisawy, Mahmoud Basseem I. Mohamed, Ahmed M. Fouda, Tarek H. Afifi, Ahmed A. Elhenawy, Ahmed Mora, Ahmed M. El-Agrody, Heba K. A. El-Mawgoud
Summary: Beta-enaminonitriles with 9-hydroxy-1H-benzo[f]chromene moiety were synthesized and evaluated for their anti-proliferative activity. The compounds showed potent inhibitory effects against human tumor cell lines PC-3, SKOV-3, and HeLa, outperforming Vinblastine and Doxorubicin. Some compounds exhibited strong activity against MCF-7/ADR cells and were tested as P-gp inhibitors. Moreover, halogenated substituents 2,4-F-2, 2,3-Cl-2, 2,5-Cl-2, and 3,4-Cl-2 showed good potency against P-gp-mediated multidrug resistance in MCF-7/ADR cells compared to Doxorubicin. These compounds also inhibited P-gp efflux function and induced apoptosis and cell cycle arrest in treated MCF-7/ADR cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Alicja Urbaniak, Chandramohan Bathula, Jyoti Chauhan, Prateek Rai, Joshua Thammathong, Christopher Clark, Billie Heflin, Annick De Loose, Nathan Avaritt, Analiz Rodriguez, Alan J. Tackett, Subhabrata Sen, Souvik Banerjee
Summary: This study designed and synthesized a series of compounds with potential anti-metastatic melanoma activity and provided initial insights into their mechanism of action.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Engineering, Environmental
Yuanyuan Wang, Fengbang Wang, Zihan Chen, Maoyong Song, Xinglei Yao, Guibin Jiang
Summary: In this study, a high-throughput single-cell imaging method was used to investigate the crosstalk among quantum dot-induced ROS generation, apoptosis, and changes in nucleus size in macrophages. Results indicated a positive correlation between changes in nucleus size and ROS generation, with QDot exposure leading to ROS generation, cell apoptosis, and subsequent changes in nucleus size. These findings provide detailed insights into the heterogeneity of nanoparticle exposure in cellular responses.
ENVIRONMENTAL SCIENCE & TECHNOLOGY
(2021)
Article
Chemistry, Applied
Larica Pathaw, Themmila Khamrang, Balasubramaniam Selvakumaran, Mariappan Murali, Pitchan Arul Prakash, Mohamed Sultan Mohamed Jaabir, Marappan Velusamy
Summary: The synthesis and characterization of copper(I) complexes show potential antitumor activity, moderate cytotoxicity against A549 cancer cells, relative inactivity against normal cells, and induction of apoptosis in cancer cells.
APPLIED ORGANOMETALLIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Angela-Patricia Hernandez, Paula Diez, Pablo A. Garcia, Martin Perez-Andres, Anzhela Veselinova, Pablo G. Jambrina, Arturo San Feliciano, David Diez, Manuel Fuentes, Ma Angeles Castro
Summary: New lignohydroquinone conjugates (L-HQs) were synthesized using the hybridization strategy and showed dual cytotoxic effect against colorectal cancer cells. These conjugates were obtained from natural product podophyllotoxin and semisynthetic terpenylnaphthohydroquinones. The results demonstrate the validity of the hybridization strategy and suggest further research on non-lactonic cyclolignans.
Article
Oncology
Adem Guner, Hakan Bektas, Emre Mentese
Summary: This study reveals that novel synthesized coumarin-triazole hybrid compounds can enhance the effect of cisplatin in cancer cells. These compounds exhibit relatively low toxicity in normal cells, reducing the dose requirement of cisplatin.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Emre Mentese, Adem Guner, Elifsu Polatli, Mustafa Emirik, Hakan Bektas, Bahittin Kahveci
Summary: This study reported the synthesis of coumarin derivatives containing the triazole ring and investigated their anticancer activities, showing strong cytotoxic effects against various cancer cell lines. In silico studies were also conducted to explore the binding interactions of the molecules.
ARCHIV DER PHARMAZIE
(2021)
Article
Biochemistry & Molecular Biology
Mohmmad Younus Wani, Majed Saeed Saleh Alghamidi, Vartika Srivastava, Aijaz Ahmad, Faisal M. Aqlan, Abdullah Saad Al-Bogami
Summary: This study aimed to synthesize novel pyrrolidine-based 1,2,3-triazole derivatives using Click Chemistry and evaluate their antifungal activity against C. auris based on CLSI guidelines. The most potent derivative (P6) showed fungicidal activity, which was quantitatively confirmed by the MUSE cell viability assay. Further analysis revealed that P6 arrested the cells in S-phase and induced apoptosis through cytochrome c release and mitochondrial depolarization. The hemolytic assay confirmed the safety of P6 for in vivo studies.
BIOORGANIC CHEMISTRY
(2023)
Article
Oncology
Upasana Yadav, Yogesh Vanjari, Kritika Laxmikeshav, Ramya Tokala, Praveen K. Niggula, Manoj Kumar, Venu Talla, Ahmed Kamal, Nagula Shankaraiah
Summary: This study synthesized a series of phenanthrene-thiazolidinedione hybrids and found that compound 17b demonstrated promising cytotoxic activity against HCT-116 human colon cancer cells, inducing apoptosis and cell cycle arrest. Computational studies indicated the potential for developing these derivatives as DNA interactive agents for colon cancer therapy.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)