Article
Pharmacology & Pharmacy
Vladislava V. V. Matveevskaya, Dmitry I. I. Pavlov, Anastasia R. R. Kovrizhina, Taisiya S. S. Sukhikh, Evgeniy H. H. Sadykov, Pavel V. V. Dorovatovskii, Vladimir A. A. Lazarenko, Andrei I. I. Khlebnikov, Andrei S. S. Potapov
Summary: The stereochemical configuration of the oxime carbon-nitrogen double bond in IQ-1 and tryptanthrin-6-oxime compounds was determined as the E-configuration using single crystal X-ray diffraction, 1D and 2D NMR techniques, and DFT calculations. This finding contradicts the previous assumption of a Z-configuration and demonstrates the stability of the E-configuration through intermolecular hydrogen bonds.
Article
Biochemistry & Molecular Biology
Serhii A. Liakhov, Igor A. Schepetkin, Olexander S. Karpenko, Hanna Duma, Nadiia M. Haidarzhy, Liliya N. Kirpotina, Anastasia R. Kovrizhina, Andrei Khlebnikov, Irina Y. Bagryanskaya, Mark T. Quinn
Summary: In this study, 13 derivatives of a JNK inhibitor were synthesized, with 8 compounds showing submicromolar binding affinity for at least one JNK isoform, and most of them exhibiting anti-inflammatory effects. Selected compounds also directly confirmed JNK inhibition, indicating their potential as lead compounds for anti-inflammatory drug development.
Article
Biochemistry & Molecular Biology
Igor A. Schepetkin, Oleksander S. Karpenko, Anastasia R. Kovrizhina, Liliya N. Kirpotina, Andrei I. Khlebnikov, Stepan I. Chekal, Alevtyna V. Radudik, Maryna O. Shybinska, Mark T. Quinn
Summary: The JNK family, including JNK1-3 proteins, regulates various physiological processes. The study aimed to find JNK inhibitors with high selectivity for JNK3. 26 new tryptanthrin-6-oxime analogs were synthesized and evaluated, and compounds 4d and 4e showed high selectivity for JNK3 and inhibited inflammatory responses. The results suggest the potential for developing anti-inflammatory drugs with selectivity for JNK3.
Article
Pharmacology & Pharmacy
Igor A. Schepetkin, Anastasia R. Kovrizhina, Ksenia S. Stankevich, Andrei I. Khlebnikov, Liliya N. Kirpotina, Mark T. Quinn, Matthew J. Cook
Summary: This study synthesized a panel of novel tryptanthrin oxime analogs and evaluated their binding affinity to JNK1-3 and inhibition of cellular inflammatory responses. Compound 1j exhibited high binding affinity to JNK1-3 and demonstrated anti-inflammatory activity by inhibiting the production of multiple proinflammatory cytokines. Molecular modeling confirmed the binding mode of 1j to JNK3.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Inorganic & Nuclear
Vladislava V. Matveevskaya, Dmitry Pavlov, Andrei S. Potapov
Summary: This study investigated the crystal structures of two iridium(III) and rhodium(III) complexes through X-ray diffraction analysis, comparing their structural features to understand the factors leading to the spontaneous enantiomer resolution of the rhodium(III) complex.
Article
Chemistry, Physical
Nakul Kumar, Gajendra Kumar Inwati, Emad M. Ahmed, Chhagan Lal, Bharat Makwana, Virendra K. Yadav, Saiful Islam, Hyun-Jo Ahn, Krishna K. Yadav, Byong-Hun Jeon
Summary: This study reports a method for synthesis of spirocyclic compounds in a one-pot reaction with high yield and selectivity. The synthesized spiro compounds show good biological activity and exhibit strong inhibitory effects on Gram-positive bacteria.
Article
Chemistry, Medicinal
Mark B. Plotnikov, Galina A. Chernysheva, Vera I. Smol'yakova, Oleg I. Aliev, Anna M. Anishchenko, Olga A. Ulyakhina, Eugene S. Trofimova, Anastasia A. Ligacheva, Nina D. Anfinogenova, Anton N. Osipenko, Anastasia R. Kovrizhina, Andrei I. Khlebnikov, Igor A. Schepetkin, Anastasia G. Drozd, Evgenii V. Plotnikov, Dmitriy N. Atochin, Mark T. Quinn
Summary: The study aimed to investigate the neuroprotective effects of TRYP-Ox in a rat model of transient focal cerebral ischemia. The results showed that TRYP-Ox could alleviate neurological deficits, decrease infarction size, inhibit inflammation, and exhibit antioxidant activity, suggesting that it may be a promising neuroprotective agent.
Article
Chemistry, Organic
Anastasia R. Kovrizhina, Elizaveta I. Samorodova, Andrei I. Khlebnikov
Summary: This study introduced a new 11H-indeno[1,2-b]quinoxaline derivative compound 3 and investigated its structural and bioavailability properties. According to ADME predictions, compound 3 shows potential for the treatment of neuroinflammation and ischemia-reperfusion injury.
Article
Chemistry, Applied
Corentin Antoine Baratay, Wenhai Li, Mitch Mathiew, Lei Yu, Sara Helen Kyne, Weidong Rao, Philip Wai Hong Chan
Summary: A synthetic method for preparing 11H-benzo[a]fluorenes and 13H-indeno[1,2-l]phenanthrenes using gold(I) and Bronsted acid-mediated reactions without excluding moisture or air is described. The reaction mechanism involves gold(I)-catalysed migration and cyclization, followed by rearrangement and deacyloxylative aromatization assisted by Bronsted acid, resulting in the formation of polyaromatic hydrocarbon (PAH) products.
ADVANCED SYNTHESIS & CATALYSIS
(2022)
Article
Chemistry, Physical
Ghada A. Eldeken, Fatma A. El-Samahy, Ehab M. Zayed, Fayez H. Osman, Galal E. H. Elgemeie
Summary: In this study, olefin adducts were synthesized through Wittig reactions and their stereo-isomerism was investigated. The structures of the compounds were confirmed based on chemical and spectroscopic evidence. The cytotoxic activity of the new compounds against liver and breast cancer cell lines was evaluated.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Multidisciplinary Sciences
Diogo Henrique Kita, Nathalie Guragossian, Ingrid Fatima Zattoni, Vivian Rotuno Moure, Fabiane Gomes de Moraes Rego, Sabrina Lusvarghi, Thomas Moulenat, Billel Belhani, Geraldo Picheth, Sofiane Bouacida, Zouhair Bouaziz, Christelle Marminon, Malika Berredjem, Joachim Jose, Marcos Brown Goncalves, Suresh V. Ambudkar, Glaucio Valdameri, Marc Le Borgne
Summary: A new generation of indeno[1,2-b]indole compounds were synthesized and tested as ABCG2 inhibitors, showing potent inhibition activity and ability to fully chemosensitize cancer cells. These compounds exert their effects by stimulating ABCG2 ATPase activity and stabilizing the protein structure.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Organic
Guodong Yin, Yuan Li, Ling Fan
Summary: Zirconium tetrachloride was used as a catalyst to synthesize two fused-ring compounds, confirmed by H-1 NMR, C-13 NMR, IR, HRMS and X-ray single crystal diffraction analysis. The method provides a complementary approach to enriching the library of corresponding heterocyclic compounds due to its mild reaction conditions and easily available starting materials.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Forough Nasuhipur, Zarrin Ghasemi, Morgane Poupon, Michal Dusek
Summary: A class of indenopyrroles was synthesized by the treatment of dihydroxy-2-methyl-4-oxoindeno[1,2-b]pyrroles with phosphorus oxychloride. The elimination of vicinal hydroxyl groups, formation of a p bond, and electrophilic chlorination produced fused aromatic pyrrole structures. Benzylic substitution of nucleophiles resulted in diverse 4-oxoindeno[1,2-b]pyrrole derivatives with yields of 58-93%. The reaction showed the highest yield when conducted in DMF. The structures of the products were confirmed using spectroscopic methods, elemental analysis, and X-ray crystallography.
Article
Oncology
Ntlotlang Mokgautsi, Yu-Cheng Kuo, Sung-Ling Tang, Feng-Cheng Liu, Shiang-Jiun Chen, Alexander T. H. Wu, Hsu-Shan Huang
Summary: This study aims to identify molecular gene signatures in glioblastoma multiforme (GBM) and evaluate the potential of a novel compound SJ10 as a target agent. Through computational simulations and experimental validation, it was demonstrated that SJ10 compound has antiproliferative and cytotoxic effects on GBM and possesses the potential to inhibit oncogenic signatures in GBM.
Article
Biochemistry & Molecular Biology
Rongrong Su, Yanyan Diao, Wenjie Sha, Dou Dou, Zhixiao Yu, Limin Leng, Zhenjiang Zhao, Zhuo Chen, Honglin Li, Yufang Xu
Summary: This study developed selective non-covalent BTK inhibitors by scaffold hopping and found that compound 2 and 4 exhibited high BTK inhibition potency. These compounds showed great ability to inhibit tumor growth in cell and animal models.
BIOORGANIC CHEMISTRY
(2022)
Review
Immunology
Scott D. Kobayashi, Frank R. DeLeo, Mark T. Quinn
Summary: Neutrophils are an important component of innate host defense, with a high production rate and rapid mobilization to infected tissues. They contain abundant antimicrobial molecules, but their turnover and activation are tightly regulated. Microbial pathogens can affect the apoptosis and cytolysis of neutrophils, altering their function.
IMMUNOLOGICAL REVIEWS
(2023)
Article
Biochemistry & Molecular Biology
Madina Zh. Sadvakassova, Andrei I. I. Khlebnikov, Abdigali A. A. Bakibaev, Oleg A. A. Kotelnikov, Rakhmetulla Sh. Erkassov, Madeniyet A. A. Yelubay, Manar A. A. Issabayeva
Summary: N-Benzhydrylformamides are pharmacologically active compounds with various biological activities. The conformation of these compounds is influenced by the presence of substituents, particularly at the nitrogen atom and in the ortho-positions of the diphenylmethane moiety. Through NMR and DFT calculations, the rotational barriers of the formyl and aryl fragments in N-benzhydrylformamides were investigated. The results showed that the DFT method satisfactorily reproduced the experimental rotational barrier of the formyl group, while ortho-substituents significantly hindered the rotation of the aryl fragment.
Article
Biochemistry & Molecular Biology
Anna A. Zhdankina, Dmitry I. Tikhonov, Sergey V. Logvinov, Mark B. Plotnikov, Andrei I. Khlebnikov, Nataliya G. Kolosova
Summary: Age-related macular degeneration (AMD) is the leading cause of irreversible visual impairment worldwide. JNK inhibitor IQ-1S shows potential in preventing and treating AMD, as it improves histological abnormalities associated with retinopathy in the OXYS rat model, including improved blood circulation, increased functional activity of the retinal pigment epithelium, reduced VEGF expression, and increased PEDF expression.
Article
Biochemistry & Molecular Biology
Igor A. Schepetkin, Zhangeldy S. Nurmaganbetov, Serik D. Fazylov, Oralgazy A. Nurkenov, Andrei I. Khlebnikov, Tulegen M. Seilkhanov, Anarkul S. Kishkentaeva, Elvira E. Shults, Mark T. Quinn
Summary: Alzheimer's disease is a common neurodegenerative disease characterized by memory loss and cognitive impairment. The loss of cholinergic neurons is one of the main causes of this disease. Current acetylcholinesterase inhibitors have limitations, so there is ongoing research to find more effective inhibitors. In this study, new lupinine triazole derivatives were synthesized and evaluated for their inhibitory activity. The most promising compound showed mixed-type inhibition and molecular docking studies revealed the interaction between the compound and the target enzyme. A structure-activity relationship model was also developed to guide the design of more potent inhibitors.
Article
Biochemistry & Molecular Biology
Igor A. Schepetkin, Oleksander S. Karpenko, Anastasia R. Kovrizhina, Liliya N. Kirpotina, Andrei I. Khlebnikov, Stepan I. Chekal, Alevtyna V. Radudik, Maryna O. Shybinska, Mark T. Quinn
Summary: The JNK family, including JNK1-3 proteins, regulates various physiological processes. The study aimed to find JNK inhibitors with high selectivity for JNK3. 26 new tryptanthrin-6-oxime analogs were synthesized and evaluated, and compounds 4d and 4e showed high selectivity for JNK3 and inhibited inflammatory responses. The results suggest the potential for developing anti-inflammatory drugs with selectivity for JNK3.
Article
Crystallography
Lixin You, Rui Tan, Xiaojuan Wang, Jianhong Hao, Shiyu Xie, Gang Xiong, Fu Ding, Andrei S. Potapov, Yaguang Sun
Summary: In this study, a new heterogeneous catalyst Pd-NHC@Eu-BCI was synthesized by incorporating N-heterocyclic carbene-palladium active sites into a 2D coordination polymer based on a 1,3-bis(carboxymethyl)imidazolium ligand. The catalyst was thoroughly characterized using various analytical techniques. The Pd-NHC@Eu-BCI catalyst exhibited excellent catalytic activity in the Suzuki-Miyaura cross-coupling reaction. It could be easily recovered from the reaction mixture and maintained its catalytic activity and structure even after five cycles.
Article
Chemistry, Inorganic & Nuclear
Vladislava V. V. Matveevskaya, Dmitry I. I. Pavlov, Alexey A. A. Ryadun, Vladimir P. P. Fedin, Andrei S. S. Potapov
Summary: A supramolecular 3D Zn(II) coordination polymer was synthesized and characterized. It exhibited blue luminescence with emission quenching response towards Fe3+ and chromate/dichromate ions.
Review
Chemistry, Inorganic & Nuclear
Na Sun, Hongyan Yu, Andrei S. Potapov, Yaguang Sun
Summary: Propylene and propane separation is an important and challenging task, and the current cryogenic distillation method is inefficient and energy-consuming. Metal-organic frameworks (MOFs) with their designability, modifiability, and flexibility have emerged as promising candidates for propylene/propane separation.
COMMENTS ON INORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Noura S. Dosoky, Liliya N. Kirpotina, Igor A. Schepetkin, Andrei I. Khlebnikov, Brent L. Lisonbee, Jeffrey L. Black, Hillary Woolf, Trever L. Thurgood, Brittany L. Graf, Prabodh Satyal, Mark T. Quinn
Summary: Echinacea purpurea essential oils have antimicrobial and immunomodulatory properties, and can be used for the treatment of respiratory infections and wound healing.
Article
Pharmacology & Pharmacy
Vladislava V. V. Matveevskaya, Dmitry I. I. Pavlov, Anastasia R. R. Kovrizhina, Taisiya S. S. Sukhikh, Evgeniy H. H. Sadykov, Pavel V. V. Dorovatovskii, Vladimir A. A. Lazarenko, Andrei I. I. Khlebnikov, Andrei S. S. Potapov
Summary: The stereochemical configuration of the oxime carbon-nitrogen double bond in IQ-1 and tryptanthrin-6-oxime compounds was determined as the E-configuration using single crystal X-ray diffraction, 1D and 2D NMR techniques, and DFT calculations. This finding contradicts the previous assumption of a Z-configuration and demonstrates the stability of the E-configuration through intermolecular hydrogen bonds.
Article
Plant Sciences
Igor A. Schepetkin, Gulmira Ozek, Temel Ozek, Liliya N. Kirpotina, Robyn A. Klein, Andrei I. Khlebnikov, Mark T. Quinn
Summary: Analysis of essential oils extracted from Agastache urticifolia, Achillea millefolium, and Perideridia gairdneri showed that they can activate human neutrophils with varying efficacy, indicating their immunomodulatory activity.
Article
Chemistry, Medicinal
Mark B. Plotnikov, Galina A. Chernysheva, Vera I. Smol'yakova, Oleg I. Aliev, Anna M. Anishchenko, Olga A. Ulyakhina, Eugene S. Trofimova, Anastasia A. Ligacheva, Nina D. Anfinogenova, Anton N. Osipenko, Anastasia R. Kovrizhina, Andrei I. Khlebnikov, Igor A. Schepetkin, Anastasia G. Drozd, Evgenii V. Plotnikov, Dmitriy N. Atochin, Mark T. Quinn
Summary: The study aimed to investigate the neuroprotective effects of TRYP-Ox in a rat model of transient focal cerebral ischemia. The results showed that TRYP-Ox could alleviate neurological deficits, decrease infarction size, inhibit inflammation, and exhibit antioxidant activity, suggesting that it may be a promising neuroprotective agent.
Article
Chemistry, Inorganic & Nuclear
Xiaolin Yu, Alexey A. Ryadun, Konstantin A. Kovalenko, Tatiana Y. Guselnikova, Valentina G. Ponomareva, Andrei S. Potapov, Vladimir P. Fedin
Summary: Lanthanide metal-organic frameworks (Ln-MOFs) can be utilized in various research fields by combining the luminescent characteristics of lanthanides and the advantages of porous materials. A water-stable and high-temperature resistant Eu-MOF with high photoluminescence quantum yield was synthesized, showing excellent selectivity and quenching sensing for Fe3+ and ofloxacin. It also demonstrated color modulation with Tb3+ and La3+ for developing white LED components, and rare reverse adsorption selectivity in a CO2/C2H2 gas mixture. The protonated carboxyl groups in the Eu-MOF provided an efficient conducting platform for proton transfer.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Medicinal
Fabio Francavilla, Federica Sarcina, Igor A. Schepetkin, Lilya N. Kirpotina, Marialessandra Contino, Annalisa Schirizzi, Giampiero De Leonardis, Andrei I. Khlebnikov, Rosalba D'Alessandro, Mark T. Quinn, Enza Lacivita, Marcello Leopoldo
Summary: FPR1 is expressed in tumor cells and plays a role in tumor growth and invasiveness. A new series of compounds with potent FPR1 antagonist activity has been designed, which can inhibit cell growth by regulating cell proliferation, apoptosis, and migration.
EUROPEAN JOURNAL OF MEDICINAL 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)