Article
Oncology
Jia-xin Chen, Da Xu, Jian-wei Cao, Li Zuo, Zhi-tao Han, Yi-jun Tian, Chuan-min Chu, Wang Zhou, Xiu-wu Pan, Xin-gang Cui
Summary: This study demonstrated the crucial role of TRIM47 in promoting malignant biological behavior in renal cell carcinoma, by interacting with P53 protein to increase its ubiquitination and degradation; The TRIM47-P53 axis might be a potential therapeutic target for RCC progression.
CANCER CELL INTERNATIONAL
(2021)
Article
Biochemistry & Molecular Biology
Shanshan Wang, Qian Hao, Jiajia Li, Yajie Chen, Hua Lu, Xiaohua Wu, Xiang Zhou
Summary: DTX3 plays a promoting role in ovarian cancer by enhancing the activity of mutant p53, and its expression is correlated with the expression of mutant p53 target genes and associated with unfavorable prognosis.
Article
Biochemistry & Molecular Biology
Orsolya Bilkei-Gorzo, Tiaan Heunis, Jose Luis Marin-Rubio, Francesca Romana Cianfanelli, Benjamin Bernard Armando Raymond, Joseph Inns, Daniela Fabrikova, Julien Peltier, Fiona Oakley, Ralf Schmid, Anetta Hartlova, Matthias Trost
Summary: This study reveals the importance of phagosomal ubiquitylation and the E3 ubiquitin ligase RNF115 in regulating innate immune functions during bacterial infections.
Article
Chemistry, Medicinal
Adam G. Bond, Conner Craigon, Kwok-Ho Chan, Andrea Testa, Athanasios Karapetsas, Rotimi Fasimoye, Thomas Macartney, J. Julian Blow, Dario R. Alessi, Alessio Ciulli
Summary: This study describes the design and development of a new protein degradation system utilizing a variant of the Brd4 bromodomain as a degradation tag. The system effectively degrades BromoTagged proteins in a fast, selective manner, showing favorable pharmacokinetic profile in mice. This system expands the arsenal of chemical genetic degradation tools for manipulating protein levels and exploring therapeutic potential in cells and in vivo.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Cell Biology
Martin P. Schwalm, Lena M. Berger, Maximilian N. Meuter, James D. Vasta, Cesear R. Corona, Sandra Roehm, Benedict-Tilman Berger, Frederic Farges, Sebastian M. Beinert, Franziska Preuss, Viktoria Morasch, Vladimir V. Rogov, Sebastian Mathea, Krishna Saxena, Matthew B. Robers, Susanne Mueller, Stefan Knapp
Summary: E3 ligases play a crucial role in regulating protein homeostasis by recruiting substrate proteins to the proteasomal degradation machinery. Recent research has focused on the Baculovirus IAP Repeat (BIR) family of E3 ligases, which contain a structurally conserved but diverse protein interaction domain. The Inhibitors of Apoptosis (IAP) family, which typically have three BIR domains, are promising drug targets. However, there is currently a lack of assay tools to evaluate the selectivity of inhibitors in this target area.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Rui Zhang, Shaoqing Shi
Summary: HECT-type E3 ubiquitin ligases play a vital role in controlling protein function and stability, and members of the NEDD4 family have critical roles in dysregulation of autophagy in cancer cells. This review focuses on the role of NEDD4 E3 ligases in defective autophagy in cancer cells, discussing their function, substrates, and signaling pathways, providing a basis for cancer treatment through modulation of these ligases.
MOLECULAR MEDICINE
(2023)
Review
Immunology
Haoran Cui, Yaxian Zhang, Leiliang Zhang
Summary: Poxviruses have evolved various mechanisms to evade innate immunity, some of which involve poxvirus-encoded E3 ubiquitin ligases and adaptor proteins. These proteins can be categorized into five groups based on their functional domains and ubiquitin transfer mechanisms. Most known substrates of poxvirus E3 ubiquitin ligases are components of the innate immune system. Current research progress provides mechanistic insights into the interaction between these viruses and their hosts.
FRONTIERS IN IMMUNOLOGY
(2021)
Article
Chemistry, Medicinal
Flavia F. Silveira, Juliana O. de Souza, Lucas V. B. Hoelz, Vinicius R. Campos, Valquiria A. P. Jabor, Anna C. C. Aguiar, M. Cristina Nonato, Magaly G. Albuquerque, Rafael V. C. Guido, Nubia Boechat, Luiz C. S. Pinheiro
Summary: In this study, 35 new compounds were designed and synthesized as inhibitors of P. falciparum, with 30 showing strong anti-parasitic activity and potential as new lead compounds for antimalarial drug discovery.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Plant Sciences
Jialing Zhang, Chaonan Li, Long Li, Yajun Xi, Jingyi Wang, Xinguo Mao, Ruilian Jing
Summary: TaAIRP2-1B regulates spike length by facilitating TaHIPP3 degradation, and the haplotype Hap-1B-1 of TaAIRP2-1B is a favorable natural variation for increasing spike length in wheat. This study provides insights into the role of E3 ubiquitin ligase genes in wheat development and identifies TaAIRP2-1B as a key regulator of spike length. The findings also offer genetic resources and markers for wheat molecular breeding.
JOURNAL OF EXPERIMENTAL BOTANY
(2023)
Review
Biochemistry & Molecular Biology
Ishita Tripathi-Giesgen, Christian Behrends, Arno F. Alpi
Summary: The ubiquitin system plays a crucial role in the host cellular defense program against bacterial infection, especially when certain bacteria are exposed to the host cytosol during invasion. Host cell E3 ubiquitin ligases contribute to the formation of a protective ubiquitin coat on invading pathogens, with their divergent ubiquitin conjugation mechanisms influencing the complexity of the anti-bacterial coating. Bacteria have evolved strategies to evade the activities of the host ubiquitin system.
Review
Biochemistry & Molecular Biology
Dong Wang, Yuanming Zou, Xinyue Huang, Zeyu Yin, Mohan Li, Jiaqi Xu, Boquan Wu, Da Li, Ying Zhang, Yingxian Sun, Xingang Zhang, Naijin Zhang
Summary: The ubiquitin-proteasome system is crucial for regulating protein levels in cells, and SMURF1 and SMURF2 are important components that maintain physiological processes by regulating the stability of multiple proteins. The regulatory functions of SMURFs in disease progression are complex, either facilitative or inhibitory, and understanding their mechanisms offers potential therapeutic targets and new avenues for research.
Review
Biochemistry & Molecular Biology
Dong Wang, Yuanming Zou, Xinyue Huang, Zeyu Yin, Mohan Li, Jiaqi Xu, Boquan Wu, Da Li, Ying Zhang, Yingxian Sun, Xingang Zhang, Naijin Zhang
Summary: The ubiquitin-proteasome system plays a crucial role in regulating protein levels in cells. SMURF1 and SMURF2 are key components in this system, responsible for regulating protein stability and maintaining physiological processes such as cell migration, proliferation, and apoptosis. They also play significant roles in disease progression, with complex regulatory functions. This review focuses on the mechanisms by which SMURF1 and SMURF2 regulate disease progression in non-cancerous diseases, providing potential therapeutic targets for various diseases and new research avenues for SMURF proteins.
Article
Biochemistry & Molecular Biology
Yi Zheng, Jian Deng, Lulu Han, Meng-Wei Zhuang, Yanwen Xu, Jing Zhang, Mei-Ling Nan, Yang Xiao, Peng Zhan, Xinyong Liu, Chengjiang Gao, Pei-Hui Wang
Summary: This study reveals the involvement of the stress response pathway and innate antiviral immunity in the pathogenic mechanism of SARS-CoV-2. NSP5 and N protein of SARS-CoV-2 were found to attenuate the formation of antiviral stress granules (avSG). NSP5 suppressed avSG formation and disrupted the RIG-I-MAVS complex to weaken the RIG-I-mediated antiviral response, while N protein specifically targeted cofactors upstream of RIG-I and affected the recognition of dsRNA by RIG-I.
SIGNAL TRANSDUCTION AND TARGETED THERAPY
(2022)
Article
Biochemistry & Molecular Biology
Qian Lv, Liqun Li, Ying Meng, Huimin Sun, Liuping Chen, Bingxin Wang, Xuejun Li
Summary: The study revealed that TaGW2-6A interacts with TaAGPS and degrades TaAGPS through the 26S proteasome pathway, influencing seed size. This mechanism provides new insights into the formation of wheat grain weight.
Article
Multidisciplinary Sciences
Xiaolan Liu, Xufeng Cen, Ronghai Wu, Ziyan Chen, Yanqi Xie, Fengqi Wang, Bing Shan, Linghui Zeng, Jichun Zhou, Bojian Xie, Yangjun Cai, Jinyan Huang, Yingjiqiong Liang, Youqian Wu, Chao Zhang, Dongrui Wang, Hongguang Xia
Summary: This study reveals that cisplatin enhances the anti-tumor effect of PD-L1 blockade and upregulates ARIH1 expression, promoting T cell infiltration and sensitizing tumors to immune checkpoint blockade. ARIH1 mediates activation of the STING pathway by ubiquitination and degradation of DNA-PKcs, which is a mechanism of tumor resistance to ICB. Activating ARIH1 is an effective strategy to improve the efficacy of cancer immunotherapy.
NATURE COMMUNICATIONS
(2023)
Article
Chemistry, Organic
Jehan Y. Al-Humaidi, A. A. Nayl, Mohamed M. Abdalla, Sobhi M. Gomha
Summary: This study synthesized and tested the in-vivo activity of different compounds, and found that triazolo-tetrazine derivatives have excellent anticonvulsant and CNS-depressant activities. Further structure-activity relationship studies demonstrated that electron-releasing groups increase activity while electron-withdrawing groups decrease activity.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Chemistry, Organic
Sobhi M. Gomha, Sayed M. Riyadh, Thoraya A. Farghaly, Reda A. Haggam
Summary: This recent review highlights the synthetic utility of bis-(4-amino-5-mercapto[1,2,4] triazoles) as versatile building blocks for the synthesis of diverse bis-fused [1,2,4]triazoles and pharmacological polymeric materials. The synthesis of macrocycles containing [1,2,4]triazole subunits is also demonstrated. The review encompasses the period from 2000 to February 2022.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Chemistry, Organic
Tariq Z. Abolibda, Maher Fathalla, Ghadah F. Aljohani, Ehab M. Zayed, Sobhi M. Gomha
Summary: In this study, a series of pyrimidine derivatives with broad-spectrum biological activity were synthesized, and their antiviral activity against SARS-CoV-2 main protease (Mpro) was investigated using molecular docking and molecular dynamics simulation. Among them, pyrazolinone 19 exhibited the strongest inhibitory activity with good affinity towards Mpro, making it a potential candidate for antiviral drug development.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Biochemistry & Molecular Biology
Tariq Z. Abolibda, Maher Fathalla, Basant Farag, Magdi E. A. Zaki, Sobhi M. Gomha
Summary: One crucial strategy for the treatment of breast cancer involves targeting the VEGFR-2 signaling system. In this study, new 3-thiazolhydrazinylcoumarins were synthesized and assessed for their inhibitory activity against VEGFR-2. The most active compounds exhibited comparable activities to the approved medicine Sorafenib and demonstrated greater anticancer activities than Sorafenib in breast cancer cell lines.
Article
Crystallography
Sobhi M. Gomha, Sayed M. Riyadh, Reem A. K. Alharbi, Magdi E. A. Zaki, Tariq Z. Abolibda, Basant Farag
Summary: A novel catalytic approach using cellulose sulfuric acid (CSA) as a green catalyst was developed for the synthesis of symmetric and asymmetric azines. The method showed high percentage yield, mild reaction conditions, broad substrate range, and environmentally benign characteristics, making it suitable for large-scale industrial manufacturing. Molecular docking analysis revealed the possible binding interactions between the azine derivatives and the target protein MAO-A, with some derivatives showing major conserved interactions, while others exhibited low binding activity.
Article
Biochemistry & Molecular Biology
Fayza O. Ashmawy, Sobhi M. Gomha, Magda A. Abdallah, Magdi E. A. Zaki, Sami A. Al-Hussain, Mohamed A. El-desouky
Summary: A new series of thiazolyl pyridines linked with thiophene moiety via hydrazone group were successfully synthesized by one-pot multi-component reaction. These compounds demonstrated excellent anticancer activities against lung cancer cells by inhibiting epidermal growth factor receptor (EGFR) tyrosine kinase, except for compounds 8c and 8f.
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
Chemistry, Organic
Mohamed G. Badrey, Sobhi M. Gomha, Aboubakr H. Abdelmonsef, Ahmed A. M. El-Reedy
Summary: A series of new three-armed heterocycles, such as thiazoles and thiazines linked to triazine moiety, were synthesized using cyanuaric chloride and thiothemicarbazide as starting materials to obtain the target compound 1. Thiazole derivatives were obtained through the reaction of tris-thiosemicarbazide with various hydrazonoyl halides. Additionally, a thiazole derivative could be prepared from the reaction of target compound 1 with DMAD. Thiazine derivatives were synthesized from compound 1 through interaction with benzylidinemalonitrile. In this study, molecular docking analysis and in silico ADMET predictions were conducted to investigate the molecular interactions and pharmacokinetic properties of the compounds. The new compounds show potential as chemical scaffolds for the development of anti-obesity drug candidates.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Polymer Science
Khaled D. Khalil, Sayed M. Riyadh, Ali H. Bashal, Tariq Z. Abolibda, Sobhi M. Gomha
Summary: A novel hybrid barium oxide-chitosan nanocomposite was synthesized and its structure and properties were analyzed and characterized. The nanocomposite showed promising catalytic performance and can be used for the synthesis of compounds with potential applications.
Article
Chemistry, Physical
Jehan Y. Al-Humaidi, Sobhi M. Gomha, Nahed A. Abd El-Ghany, Basant Farag, Magdi E. A. Zaki, Tariq Z. Abolibda, Nadia A. Mohamed
Summary: In this study, an ecofriendly biopolymeric catalyst was prepared and used for the synthesis of novel thiazole and thiadiazole derivatives. The catalyst showed mild reaction conditions, quick reaction durations, and high reaction yields. It also retained its potency after multiple reuses.
Article
Chemistry, Multidisciplinary
Jehan Y. Al-Humaidi, Sobhi M. Gomha, Sayed M. Riyadh, Mohamed S. Ibrahim, Magdi E. A. Zaki, Tariq Z. Abolibda, Ohoud A. Jefri, Amr S. Abouzied
Summary: A series of thiazolylhydrazonothiazoles with an indole moiety were synthesized, and the synthesized compounds showed significant anticancer activity against colon carcinoma cell line (HCT-116), liver carcinoma cell line (HepG2), and breast carcinoma cell line (MDA-MB-231), with minimal toxic effects on normal cells, indicating their potential safety for pharmacological studies. Docking studies comparing their binding scores and modes to a reference standard (W19) suggested that these compounds act as inhibitors of the epidermal growth factor receptor tyrosine kinase domain (EGFR TK) protein, endorsing their anticancer activity.
Article
Biochemistry & Molecular Biology
Adel Alghamdi, Amr S. S. Abouzied, Abdulwahab Alamri, Sirajudheen Anwar, Mukhtar Ansari, Ibrahim Khadra, Yasser H. H. Zaki, Sobhi M. M. Gomha
Summary: In this study, a novel series of N-aminothiazole-hydrazineethyl-pyridines were designed, synthesized, and characterized. Molecular docking and molecular dynamics simulation were applied to investigate their binding energy with the SARS-CoV-2 main protease. The results obtained from in vitro and in vivo research on these synthesized compounds are expected to make a significant contribution to the fight against COVID-19.
CURRENT ISSUES IN MOLECULAR BIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Hanzada T. Nour T. El-Din, Mohamed M. Elsebaie, Nader S. Abutaleb, Ahmed M. M. Kotb, Ahmed S. Attia, Mohamed N. Seleem, Abdelrahman S. Mayhoub
Summary: In this study, a series of structurally related acetylenic-diphenylurea derivatives carrying the aminoguanidine moiety were tested for their antibacterial efficacy against multidrug-resistant Gram-positive clinical isolates. Compound 18 showed superior bacteriological characteristics compared to the lead compound I. In addition, compound 18 demonstrated excellent in vitro antibacterial profile, high tolerability towards mammalian cells, and significant effectiveness in controlling MRSA infection in an animal model.
RSC MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Refaie M. Kassab, Sami A. Al-Hussain, Aboubakr H. Abdelmonsef, Magdi E. A. Zaki, Sobhi M. Gomha, Zeinab A. Muhammad
Summary: A new series of xylenyl-spaced bis-carbazones were successfully synthesized and used as building blocks to construct a variety of bis-thiazole/thiazine derivatives. These newly synthesized compounds exhibited remarkable antiviral activity, especially compound 6d. Molecular docking study further confirmed the antiviral mechanism of these compounds.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Sobhi M. Gomha, Magdi E. A. Zaki, Deepika Maliwal, Raghuvir R. S. Pissurlenkar, Mohamed S. Ibrahim, Maher Fathalla, Ahmed M. Hussein
Summary: This study synthesized novel 3-thiazolyl-indole derivatives and evaluated their ability to inhibit CDK2 using molecular docking analyses. The compounds exhibited significant inhibitory activity against CDK2 and showed potential as anticancer drugs.
RESULTS IN CHEMISTRY
(2023)
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)
