Article
Biochemistry & Molecular Biology
Mohamed S. Ibrahim, Basant Farag, Jehan Y. Al-Humaidi, Magdi E. A. Zaki, Maher Fathalla, Sobhi M. Gomha
Summary: The green synthesis of new benzaldazine and ketazine derivatives using the grinding method with acetic acid as a catalyst is reported in this study. The synthesized derivatives exhibited potential anti-tumor activities against different cancer cell lines. Molecular docking studies and drug-likeness analysis indicated that one of the derivatives had better pharmacokinetics and oral bioavailability compared to the reference medication.
Article
Biochemistry & Molecular Biology
M. S. Raghu, K. Yogesh Kumar, T. Shamala, Fahad A. Alharti, M. K. Prashanth, Byong-Hun Jeon
Summary: In this study, promising quinazolinone-based pyridine derivatives were synthesized and tested for their antimycobacterial activities against drug-sensitive and drug-resistant Mycobacterium tuberculosis strains. The results showed that compounds 4e and 4f exhibited potential anti-TB action. Molecular docking studies revealed the binding patterns of these compounds with the mycobacterial membrane protein MmpL3, providing a structural rationale for Mtb inhibition.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Applied
Lin Zhu, Xuebo Song, Fei Pan, Tuohetisayipu Tuersuntuoheti, Fuping Zheng, Qing Li, Siqi Hu, Feifei Zhao, Jinyuan Sun, Baoguo Sun
Summary: In this study, the interactions between kafirin and ferulic acid, tetramethyl pyrazine were investigated using various spectroscopic and molecular modeling techniques. The results showed that the combination of kafirin with these compounds led to structural changes in kafirin, affecting the quality of baijiu.
Article
Neurosciences
Xin Liu, Ling-yun Lai, Jiang-xia Chen, Xiang Li, Nan Wang, Li-jun Zhou, Xiao-wen Jiang, Xiao-long Hu, Wen-wu Liu, Xin-ming Jiao, Zhen-tong Qi, Wen-jie Liu, Li-meng Wu, Yao-guang Huang, Zi-hua Xu, Qing-chun Zhao
Summary: In this study, the harmine derivatives ZDWX-12 and ZDWX-25 were found to effectively inhibit Tau hyperphosphorylation. The inhibition effect of ZDWX-25 was superior to that of ZDWX-12, as demonstrated by cell-based and mouse models. These findings suggest that ZDWX-25 is a promising drug for the treatment of Alzheimer's disease.
Article
Chemistry, Multidisciplinary
Alaa M. Alqahtani, Abrar A. Bayazeed
Summary: Ten new pyridine-linked thiazole hybrids were synthesized using a specific strategy, and their cytotoxicity against various cancer cell lines was studied. Two of the compounds showed promising anticancer activity.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ebtehal M. Husseiny, Hamada S. Abulkhair, Nehad M. El-Dydamony, Kurls E. Anwer
Summary: This study reports the design and synthesis of two new sets of sulfaguanidine-based azopyrazolidine-3,5-diones and 3,5-diaminoazopyrazoles with potential anticancer and CDK-9 inhibiting activity. Among these compounds, four derivatives (VII, VIII, X, and XIII) showed potent cytotoxicity against selected tumor cells. The 3,5-diaminopyrazole-1-carboxamide derivative XIII exhibited high selectivity towards cancer cells and is a promising CDK-9 inhibitor candidate for further investigation in breast, colorectal, and hepatic malignancies.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Mohamed G. Abouelenein, Ahmed A. El-Rashedy, Hanem M. Awad, Ahmed F. El Farargy, Ibrahim F. Nassar, Amr Nassrallah
Summary: The present study describes the synthesis of a novel series of polyfunctionalized pyridine congeners and their evaluation for cytotoxic efficacy against cancer cells and normal cells. Some of the compounds showed potential as anticancer candidate drugs. Molecular impact studies revealed the influence of certain compounds on gene expression, promoting apoptosis in cancer cells. Docking studies and molecular dynamic simulations provided insights into the binding modes of the compounds with target proteins. Finally, POM analysis facilitated the identification of promising compounds.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Yuxi Ge, Bin Huang
Summary: A series of light-emitting analogues, TPA-DPQ and TPA-DPP, were synthesized and characterized. These compounds displayed similar donor-acceptor structures but showed different emission properties and mechanochromic luminescence behaviors. Crystallographic analysis revealed that intermolecular interactions were responsible for the distinct mechanochromic luminescence behaviors. This work provides guidance for rational design of mechanochromic luminescent fluorophores.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Rohit Shukla, Anuj Kumar, David J. Kelvin, Tiratha Raj Singh
Summary: Alzheimer's disease is a neurological disorder caused by abnormal protein accumulation. In this study, a virtual screening approach was used to identify compounds that can inhibit DYRK1A, a key enzyme involved in the phosphorylation of amyloid-beta and neurofibrillary tangles. Four compounds, including ZINC3843365, ZINC2123081, ZINC5220992, and ZINC68569602, showed the highest affinity for DYRK1A and have the potential to reduce the burden of amyloid-beta and neurofibrillary tangles in Alzheimer's disease.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2023)
Article
Chemistry, Medicinal
Baljit Kaur, Sahil Mishra, Ramandeep Kaur, Shikha Kalotra, Palwinder Singh
Summary: The study focused on designing and synthesizing new indole derivatives as potential agents for inhibiting tumor growth by targeting TNF-α. Results indicated that compounds 2d and 2g exhibited significant cytotoxicity against a panel of human cancer cell lines.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Endocrinology & Metabolism
Yuxuan Yong, Qinfen Wu, Xinling Meng, Ranran Lu, Huan Xia, Feifei Pei, Xinling Yang
Summary: This study reveals the role of DYRK1A in the phosphorylation of alpha-synuclein and regulation of the PI3K/Akt/GSK3β pathway in DA neuronal apoptosis.
JOURNAL OF BIOLOGICAL REGULATORS AND HOMEOSTATIC AGENTS
(2023)
Article
Chemistry, Medicinal
Anthi Petrou, Athina Geronikaki, Victor Kartsev, Antonios Kousaxidis, Aliki Papadimitriou-Tsantarliotou, Marina Kostic, Marija Ivanov, Marina Sokovic, Ioannis Nicolaou, Ioannis S. Vizirianakis
Summary: In this study, the antimicrobial activity of seventeen new derivatives was evaluated. The compounds exhibited strong antibacterial activity against both Gram-positive and Gram-negative bacteria, surpassing the activity of ampicillin and streptomycin by 10-50 fold. The most sensitive bacterium was En. Cloacae, while E. coli and M. flavus were the most resistant ones. Compound 8 was found to be the most potent, and exhibited excellent antifungal activity. Docking studies revealed that the antibacterial activity was likely due to the inhibition of E. coli MurB, while the antifungal mechanism involved inhibition of 14a-lanosterol demethylase of CYP51Ca. Drug-likeness and ADMET profile prediction were also performed, and cytotoxicity studies against normal MRC5 cells were conducted for the most active compounds.
Article
Biochemistry & Molecular Biology
Naglaa M. Ahmed, Mahmoud M. Youns, Moustafa K. Soltan, Ahmed M. Said
Summary: The study synthesized a series of novel indolyl-pyrimidine hybrids with potent antitumor activity, among which compound 4g showed the most potent antitumor activity and could be used as a potential anticancer agent.
Article
Biochemistry & Molecular Biology
Tanveer A. A. Wani, Ahmed H. H. Bakheit, Seema Zargar, Nojood Altwaijry, Mashooq Ahmad Bhat, Hamad M. M. Alkahtani, Lamees S. S. Al-Rasheed
Summary: The presence of the p-aryl/cyclohexyl ring in the N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazine carbothioamide derivative (2C) enhances its antifungal properties. This study investigates the interaction of 2C with BSA using spectroscopic methods and molecular docking. The results demonstrate a strong binding interaction between BSA and 2C through hydrogen and van der Waals forces, with binding constants ranging from 2.91 x 10(5) to 1.29 x 10(5).
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Tamer El Malah, Hanan A. Soliman, Bahaa A. Hemdan, Randa E. Abdel Mageid, Hany F. Nour
Summary: A series of new compounds with antibacterial properties were synthesized by the research team, and their inhibitory and antibiofilm activities against methicillin-resistant Staphylococcus aureus (MRSA) were evaluated. The results showed that some compounds exhibited significant growth inhibition activity against MRSA cells, with antibiofilm effects superior to Vancomycin.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Chemistry, Applied
Julia K. Keppler, Anja Heyse, Eva Scheidler, Maximilian J. Uttinger, Laura Fitzner, Uwe Jandt, Timon R. Heyn, Vanessa Lautenbach, Joanna Loch, Jonas Lohr, Helena Kieserling, Gabriele Guenther, Elena Kempf, Jan-Hendrik Grosch, Krzysztof Lewinski, Dieter Jahn, Christian Luebbert, Wolfgang Peukert, Ulrich Kulozik, Stephan Drusch, Rainer Krull, Karin Schwarz, Rebekka Biedendieck
FOOD HYDROCOLLOIDS
(2021)
Article
Respiratory System
Laurent Meijer, Genevieve Hery-Arnaud, Cyril Leven, Emmanuel Nowak, Sophie Hillion, Yves Renaudineau, Isabelle Durieu, Raphael Chiron, Anne Prevotat, Isabelle Fajac, Dominique Hubert, Marlene Murris-Espin, Sandrine Huge, Isabelle Danner-Boucher, Bruno Ravoninjatovo, Sylvie Leroy, Julie Macey, Thierry Urban, Gilles Rault, Dominique Mottier, Rozenn Le Berre
Summary: A study was conducted to evaluate the safety and effects of roscovitine in patients with Cushing disease. The results showed that roscovitine was relatively safe and well-tolerated, but did not show significant efficacy in treating the disease. The variability in pharmacokinetics of roscovitine may have contributed to the lack of effectiveness.
JOURNAL OF CYSTIC FIBROSIS
(2022)
Article
Chemistry, Medicinal
Tania Tahtouh, Emilie Durieu, Benoit Villiers, Celine Bruyere, Thu Lan Nguyen, Xavier Fant, Kwang H. Ahn, Leepakshi Khurana, Emmanuel Deau, Mattias F. Lindberg, Elodie Severe, Frederic Miege, Didier Roche, Emmanuelle Limanton, Jean-Martial L'helgoual'ch, Guillaume Burgy, Solene Guiheneuf, Yann Herault, Debra A. Kendall, Francois Carreaux, Jean-Pierre Bazureau, Laurent Meijer
Summary: Leucettines, derived from marine sponge alkaloid Leucettamine B, have potential therapeutic applications for Alzheimer's disease, Down syndrome, diabetes, and other diseases. There is a correlation between the inhibition of specific kinase targets and cellular effects.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Katarzyna Wojtowicz, Teresa Steliga, Piotr Kapusta, Joanna Brzeszcz, Tomasz Skalski
Summary: This research focuses on the biodegradation of petroleum hydrocarbons in soil, and found that the addition of gamma-PGA to a biopreparation A1 can enhance the degradation efficiency and reduce toxicity.
Article
Clinical Neurology
B. Souchet, M. Audrain, Y. Gu, M. F. Lindberg, N. S. Orefice, E. Rey, N. Cartier, N. Janel, L. Meijer, Jerome Braudeau
Summary: The presence of both soluble forms of Aβ 342 and p-tau may be responsible for the onset of mild cognitive impairment (MCI) in Alzheimer's disease (AD).
JPAD-JOURNAL OF PREVENTION OF ALZHEIMERS DISEASE
(2022)
Article
Chemistry, Multidisciplinary
Joanna Loch, Jakub Barciszewski, Joanna Sliwiak, Piotr Bonarek, Paulina Wrobel, Kinga Pokrywka, Ivan G. Shabalin, Wladek Minor, Mariusz Jaskolski, Krzysztof Lewinski
Summary: This study identified alternative ligand-binding sites in the beta-lactoglobulin molecule, providing important evidence through crystal structure analysis. The importance of shape complementarity for ligand recognition and selectivity was highlighted in the analysis.
Article
Biochemistry & Molecular Biology
Sreenivas Avula, Xudan Peng, Xingfen Lang, Micky Tortorella, Beatrice Josselin, Stephane Bach, Stephane Bourg, Pascal Bonnet, Frederic Buron, Sandrine Ruchaud, Sylvain Routier, Cleopatra Neagoie
Summary: A library of simplified Lamellarin isosters, substituted indolo[2,3-c]quinolone-6-ones, was developed and evaluated for their inhibitory activity on Haspin kinase. Two derivatives exhibited good selectivity and interesting cell effects on osteosarcoma cell line.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Cell Biology
Priyanka Gupta, Keehn Strange, Rahul Telange, Ailan Guo, Heather Hatch, Amin Sobh, Jonathan Elie, Angela M. Carter, John Totenhagen, Chunfeng Tan, Yogesh A. Sonawane, Jiri Neuzil, Amarnath Natarajan, Ashley J. Ovens, Jonathan S. Oakhill, Thorsten Wiederhold, Karel Pacak, Hans K. Ghayee, Laurent Meijer, Sushanth Reddy, James A. Bibb
Summary: Metabolic dysfunction mutations can lead to cancer. Loss of SDHB triggers a signaling cascade that disrupts energy sensing and promotes cancer progression.
Review
Biochemistry & Molecular Biology
Yashoda Krishna Sunkari, Laurent Meijer, Marc Flajolet
Summary: Protein kinases are essential in biology and their deregulation is linked to various diseases. However, the high conservation of ATP-binding sites among kinases makes it challenging to develop highly specific inhibitors. In the context of neurodegenerative diseases, CK1 and other kinases have been implicated. Currently, there are no specific regulators for CK1, and known inhibitors target the ATP-binding site. DNA-encoded library technology may be a promising approach to discover allosteric modulators instead of ATP competitors.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2022)
Article
Environmental Sciences
Joanna Brzeszcz, Tomasz Skalski, Leszek Jankowski, Piotr Kapusta
Summary: Hand-dug oil wells located in natural crude oil seep sites are remnants of historical exploitation activities that pose a threat to soil ecosystems. However, there are currently no common environmental policies regarding these soils. This study found that natural attenuation processes might occur in seep soils, as a result of long-term adaptation to hydrocarbon exposure, leading to a diversified and stable bacterial community structure and eventual utilization of these compounds.
LAND DEGRADATION & DEVELOPMENT
(2023)
Article
Chemistry, Medicinal
Mattias F. Lindberg, Emmanuel Deau, Jonas Arfwedson, Nicolas George, Pascal George, Patricia Alfonso, Ana Corrionero, Laurent Meijer
Summary: This study evaluates the kinase inhibitory activity of a library of DYRKs/CLKs inhibitors and finds a diverse range of potencies and selectivities among these inhibitors, highlighting the challenges of targeting kinases in this area of research. The use of a panel of inhibitors is suggested for studying the functions of these kinases in cellular processes.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Emmanuel Deau, Mattias F. F. Lindberg, Freideiric Miege, Didier Roche, Nicolas George, Pascal George, Andreas Kra''mer, Stefan Knapp, Laurent Meijer
Summary: Dual-specificity,tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases (CLKs) have been identified as important targets for various pathologies. In this study, a family of DYRK/CLK inhibitors called Leucettinibs, derived from Leucettines and Leucettamine B, were synthesized and characterized. These inhibitors showed subnanomolar IC50 on DYRK1A and demonstrated potential for therapeutic drug development. Kinase-inactive isomers, iso-Leucettinibs, were also synthesized as suitable negative control compounds. Leucettinibs were found to inhibit DYRK1A substrate phosphorylation in cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Katarzyna Wojtowicz, Teresa Steliga, Piotr Kapusta, Joanna Brzeszcz
Summary: This research focuses on the remediation of oil-contaminated land using biological methods. The results show that inoculation with biopreparations B1 and B2 can significantly reduce the concentrations of aliphatic hydrocarbons and PAHs in the soil, with B2 being more effective. Additionally, phytoremediation using Zea mays can effectively degrade petroleum hydrocarbons in pre-treated soil. Toxicological tests further confirm the effectiveness of bioremediation practices. Overall, the results demonstrate the great potential of using microbial biopreparations and Zea mays in the treatment of soils contaminated with petroleum hydrocarbons.
Correction
Clinical Neurology
B. Souchet, M. Audrain, Y. Gu, M. F. Lindberg, N. S. Orefice, E. Rey, N. Cartier, N. Janel, L. Meijer, Jerome Braudeau
JPAD-JOURNAL OF PREVENTION OF ALZHEIMERS DISEASE
(2023)
Correction
Geriatrics & Gerontology
B. Souchet, M. Audrain, Y. Gu, M. F. Lindberg, N. S. Orefice, E. Rey, N. Cartier, N. Janel, L. Meijer, Jerome Braudeau
JOURNAL OF NUTRITION HEALTH & AGING
(2022)
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)