Article
Biochemistry & Molecular Biology
Jianwei Shi, Zhichuan Wang, Xiaoxu Teng, Bing Zhang, Kai Sun, Xin Wang
Summary: In this study, we achieved a C3-selenylation of pyrido[1,2-a]pyrimidin-4-ones using an electrochemically driven external oxidant-free strategy. Various structurally diverse seleno-substituted N-heterocycles were obtained in moderate to excellent yields. A plausible mechanism for this selenylation was proposed based on radical trapping experiments, GC-MS analysis, and cyclic voltammetry study.
Article
Chemistry, Multidisciplinary
Sumeyye Yalduz, Mehmet Yilmaz
Summary: In this study, furo[2,3-d]pyrido[1,2-a]pyrimidin-4-ones were synthesized by microwave-assisted radical cyclizations. The reaction was performed between 2-hydroxy-4H-pirido[1,2-a]pirimidin-4-ones and conjugated alkenes and phenylacetylene using Mn(OAc)(3) as a catalyst. Different reaction conditions were compared to optimize the reaction. The obtained compounds were characterized using spectroscopic techniques and XRD analysis.
Article
Chemistry, Organic
Rajesh T. T. Bhawale, Umesh A. A. Kshirsagar
Summary: A metal-catalyst-free, organic dye-catalyzed C3-H arylation of pyrido[1,2-a]pyrimidin-4-ones using visible light irradiation was developed. This simple and direct C-H functionalization approach effectively produced biologically significant C3 arylated pyrido[1,2-a]pyrimidin-4-one and thiazolo[3,2-a]pyrimidin-5-one derivatives, including medicinally important endothelial cell dysfunction inhibitor and anti-inflammatory agents with good functional group tolerance. The photoinduced direct C3-H arylation approach is suitable for scale-up synthesis.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Review
Chemistry, Organic
Rajesh T. T. Bhawale, Abhinay S. S. Chillal, Umesh A. A. Kshirsagar
Summary: 4H-pyrido[1,2-a]pyrimidin-4-one and their derivatives are highly bioactive and multipurpose heterocyclic motifs, with applications in drugs, natural products, agrochemical, material science, and organic synthesis. The C-H functionalization of the basic core structure of heterocycles is an indispensable tool in the pharmaceutical industry for the synthesis of various useful heterocyclic molecules and their derivatives. This review summarizes various routes to synthesize 4H-pyrido[1,2-a]pyrimidin-4-one derivatives, as well as various derivatization methods such as cross-coupling, C-H functionalization through arylation, alkenylation, sulfenylation, selenylation, phosphonation, etc., considering the synthetic potential and significant influence of this scaffold in drug discovery.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Prasanjit Ghosh, Gautam Chhetri, Sajal Das
Summary: An expeditious metal-free synthesis method has been developed for synthesizing diverse 3-ArS/ArSe derivatives with high yields (up to 95%) of 4H-pyrido[1,2-a]pyrimidin-4-one. This operationally simple reaction, conducted under mild conditions, can be scaled up to gram quantities and shows broad functional group tolerance. Preliminary experimental investigations suggest a radical mechanistic pathway for these transformations.
Article
Chemistry, Applied
Prasanjit Ghosh, Gautam Chhetri, Eliyahu Perl, Sajal Das
Summary: The methodology reported involves the arylselenylation of 4H-Pyrido-[1,2-a]-Pyrimidin-4-ones using readily available organodiselenides in high yields up to 98%, without the need for a metal catalyst. Additionally, it can be applied for the synthesis of ArSe substituted 5H-thiazolo-pyrido[3,2-a]pyrimidin-4-ones.
ADVANCED SYNTHESIS & CATALYSIS
(2021)
Article
Chemistry, Medicinal
Caroline C. Sousa, Godwin Akpeko Dziwornu, Helenita C. Quadros, Joao Honorato Araujo-Neto, Kelly Chibale, Diogo R. M. Moreira
Summary: This study examines the cellular uptake and antiplasmodium activity of Pyrido[1,2-a]benzimidazoles (PBIs), synthetic antiplasmodium agents. The results show that PBIs have potent antiparasitic effects against both chloroquine-susceptible and chloroquine-resistant Plasmodium strains, with a high rate of uptake by parasite cells but limited uptake by host cells. The mechanism of cellular uptake differs from other 4-aminoquinolines.
ACS INFECTIOUS DISEASES
(2022)
Article
Chemistry, Organic
Abhinay S. Chillal, Rajesh T. Bhawale, Umesh A. Kshirsagar
Summary: A lenient approach for regioselective C3-H chalcogenation and thiocyanation of 4H-pyrido[1,2-a] pyrimidin-4-ones is developed using visible light photocatalysis. This method provides a wide range of functionalized derivatives with moderate to high yields. The protocol utilizes visible light as an environmentally friendly energy source, cost-effective oxidant, and easily obtainable dichalcogenides for selective C-H chalcogenation at room temperature. Additionally, a regioselective thiocyanation method for 4H-pyrido[1,2-a] pyrimidin-4-ones is also developed. Mechanistic pathways for these transformations are proposed based on light on/off and Stern-Volmer studies, as well as quantum yield calculations.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Jinyang Chen, Yao Xiao, Xianhui You, Shiqi Li, Yuwei Fu, Yuejun Ouyang
Summary: An environmentally friendly protocol for the synthesis of C-3-selenylated 4H-pyrido[1,2-a]pyrimidin-4-ones was developed via electrochemical oxidation and iodide-catalyzed selenation. The reaction proceeds efficiently with 10 mol % of KI as catalyst and electrolyte, giving the desired products in good to excellent yields without the use of excess oxidant or iodinated reagents.
Article
Chemistry, Organic
Meiyun Su, Lina Guo, Peiyu Mao, Meng Xiao, Wenjie Liu, Shaohua Wang
Summary: The catalyst-free electrochemical halogenation and trifluoromethylation of 4H-pyrido[1,2-a]pyrimidin-4-ones was successfully achieved under external-oxidant-free conditions. This strategy provides an easy and green approach for the synthesis of functionalized new 4H-pyrido[1,2-a]pyrimidin-4-one derivatives with broad scope, good functional group tolerance, and high regioselectivity.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Lina Guo, Meiyun Su, Haiying Zhan, Wenjie Liu, Shaohua Wang
Summary: An efficient and simple protocol for silver-catalyzed direct C3 phosphonation of 4H-pyrido[1,2-a]pyrimidin-4-ones with dialkyl phosphites has been developed, showing high regioselectivity, broad scope of substrates, and good functional group compatibility. Importantly, the phosphorylated product can be used as efficient probes for Fe3+.
ASIAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Sonam Rai, Faraz Ghous, Soni Shukla, Pulkit Sharma, Prince Trivedi, Abha Bishnoi
Summary: This work presents an efficient synthesis of a novel compound, 4-phenyl-2-thioxo-3,4-dihydro-1H-pyrido[1,2-a]pyrimido[4,5-d]pyrimidin-5(2H)-one, which was characterized by various spectral techniques. Quantum chemical calculations and computational analysis were performed to investigate the molecule's characteristics and reactivity sites. Docking studies and molecular dynamics simulations were conducted to assess the binding sites and stability of protein-ligand complexes.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Pharmacology & Pharmacy
Joseph Hawadak, Shewta Chaudhry, Veena Pande, Vineeta Singh
Summary: This study evaluated the drug efficacy of Chloroquine, Artemisinin, and Azadirachta indica silver nanoparticles against Plasmodium falciparum 3D7 strain using pLDH and SYBR Green I assay methods. The results showed that the IC50 values determined by both methods were similar, indicating the consistency between pLDH and SYBR Green I assays.
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
(2023)
Article
Chemistry, Organic
Lina Guo, Meiyun Su, Junliang Lv, Wenjie Liu, Shaohua Wang
Summary: A novel and efficient method for regioselective selenylation of 4H-pyrido-[1,2-a]-pyrimidin-4-ones with diselenides at room temperature has been developed. The procedure is catalyzed by N-iodosuccinimide under metal-free conditions and provides good to excellent yields of C3 selenylation products across a broad range of substrates. Furthermore, sulfenylation with diphenyl disulfides and 4-methylbenzenethiol in this transformation is also successful.
ASIAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Romain Mustiere, Prisca Lagardere, Sebastien Hutter, Celine Deraeve, Florian Schwalen, Dyhia Amrane, Nicolas Masurier, Nadine Azas, Vincent Lisowski, Pierre Verhaeghe, Dominique Mazier, Patrice Vanelle, Nicolas Primas
Summary: This study describes the synthesis of 33 new compounds in the 2-aminothieno[3,2-d]pyrimidin-4(3H)-one series via three palladium-catalyzed cross coupling reactions. The synthesized compounds were evaluated for their antiplasmodial activity and cytotoxicity. Although a better compound than the existing drug was not obtained, compound 1g with improved cytotoxicity and metabolic stability was identified as a potential starting point for further research.
Article
Biochemistry & Molecular Biology
Gaurangkumar C. Brahmbhatt, Tushar R. Sutariya, Hiralben D. Atara, Narsidas J. Parmar, Vivek K. Gupta, Irene Lagunes, Jose M. Padron, Prashant R. Murumkar, Mange Ram Yadav
MOLECULAR DIVERSITY
(2020)
Review
Pharmacology & Pharmacy
Prashant R. Murumkar, Rahul B. Ghuge, Monica Chauhan, Rahul R. Barot, Sharmishtha Sorathiya, Kailash M. Choudhary, Karan D. Joshi, Mange Ram Yadav
EXPERT OPINION ON DRUG DISCOVERY
(2020)
Article
Biochemistry & Molecular Biology
Ashish M. Kanhed, Dushyant Patel, Divya M. Teli, Nirav R. Patel, Mahesh T. Chhabria, Mange Ram Yadav
Summary: COVID-19 is a worldwide pandemic caused by the novel coronavirus, requiring structural and non-structural proteins for replication mainly by the main protease (Mpro). Systematic screening of approved drug library and Asinex BioDesign library identified potential antiviral agents, with structural modifications needed for stability and safety.Screenings of the libraries resulted in molecules with promising interactions with the target protein Mpro, categorized into different classes for further drug development.
MOLECULAR DIVERSITY
(2021)
Article
Parasitology
Cheryl Sachdeva, Dinesh Mohanakrishnan, Sandeep Kumar, Naveen Kumar Kaushik
EXPERIMENTAL PARASITOLOGY
(2020)
Article
Biochemistry & Molecular Biology
Kishan B. Patel, Dushyant Patel, Nirav R. Patel, Ashish M. Kanhed, Divya M. Teli, Bhumi Gandhi, Bhavik S. Shah, Bharat N. Chaudhary, Navnit K. Prajapati, Kirti Patel, Mange Ram Yadav
Summary: Carbazole-based derivatives were designed, synthesized, and evaluated for their inhibitory activity against cholinesterase, antioxidant properties, and metal chelating abilities. Two compounds showed promising ChE inhibitory activity and specific copper ion chelating ability, along with strong interactions with the active sites of ChE enzymes. These compounds also demonstrated significant in silico drug-like pharmacokinetic properties.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Gurprit Bhardwaj, Mitul Vakani, Abhay Srivastava, Dhaval Patel, Anju Pappachan, Prashant Murumkar, Hemal Shah, Rushabh Shah, Sarita Gupta
Summary: Swertisin effectively lowers blood glucose levels by inhibiting SGLT2 and reducing its expression, leading to improved glucose homeostasis in diabetic mice.
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
(2021)
Article
Biochemistry & Molecular Biology
Honnavalli Yogish Kumar, Prashant R. Murumkar, B. P. Srinivasan, Vijay Pawar, M. R. Yadav
Summary: This study reported the design, synthesis, and cytotoxicity studies of a series of derivatives, with two compounds showing remarkable cytotoxicity and inducing cell cycle arrest and apoptosis in leukemia cancer cells.
MOLECULAR DIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
M. R. Suryawanshi, A. M. Kanhed, V. M. Kulkarni, S. H. Bhosale, M. R. Yadav
Summary: In this study, a hit molecule with antidepressant activity was discovered and modified chemically to obtain different derivatives. The synthesized compounds showed moderate to good antidepressant activity, with the most potent compound exhibiting better potential than standard drugs. Molecular dynamics and acute oral toxicity tests were also performed.
MOLECULAR DIVERSITY
(2022)
Article
Chemistry, Multidisciplinary
Mange Ram Yadav, Mukesh Kumar, Prashant R. Murumkar
Summary: Gene therapy has the potential to address a wide range of health issues, but the lack of a suitable vector is a major obstacle. Gemini amphiphiles show promise in transfection efficiency, although they exhibit concentration-dependent toxicity in MTT assays.
Review
Chemistry, Medicinal
Prashant R. Murumkar, Mayank Kumar Sharma, Pradeep Gupta, Niyati M. Patel, Mange Ram Yadav
Summary: The selection of the right protein structure is crucial for the success of drug discovery through structure-based design. This study presents a systematic approach for choosing the appropriate type of protein structure, with case studies on TACE, 11 beta-HSD1, DprE1, and SARS-CoV-2 M-pro enzymes for illustration.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2023)
Article
Oncology
Kaushik Neogi, Prashant R. Murumkar, Priyanshu Sharma, Poonam Yadav, Mallika Tewari, Devarajan Karunagaran, Prasanta Kumar Nayak, Mange Ram Yadav
Summary: In this study, novel 4,7-disubstituted 8-methoxyquinazoline derivatives were designed as potential cytotoxic agents against cancers by inhibiting the protein-protein interactions of beta-catenin/TCF4. The most potent compound (18B) showed significant cytotoxicity, inducing apoptosis and inhibiting cell migration in HCT116 and HepG2 cells. Mechanistic studies revealed that compound (18B) downregulated the beta-catenin/TCF4 signaling pathway, protein expression, and mRNA levels of c-MYC andCyclin D1. It also exhibited cytotoxicity against primary human gallbladder cancer cells. These findings suggest that compound (18B) is a promising lead molecule for anticancer therapy targeting the beta-catenin/TCF4 signaling pathway.
TRANSLATIONAL ONCOLOGY
(2022)
Article
Chemistry, Physical
Drishti Panjwani, Shruti Patel, Deepak Mishra, Viral Patel, MangeRam Yadav, Abhay Dharamsi, Asha Patel
Summary: This study developed and characterized biotin-streptavidin conjugated bovine serum albumin nanoparticles containing Gefitinib using the desolvation method. The nanoparticles exhibited monodispersity and a negatively charged surface. They showed high drug loading and sustained drug release at physiological pH. In cytotoxicity studies, these nanoparticles demonstrated better cell growth inhibition and reduced side effects compared to other formulations of Gefitinib.
JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY
(2022)
Article
Chemistry, Physical
Atul N. Khadse, Hardik H. Savsani, Rupesh V. Chikhale, Rahul B. Ghuge, Dixit R. Prajapati, Goshiya Kureshi, Prashant R. Murumkar, Kirti V. Patel, Sadhana J. Rajput, Mange Ram Yadav
Summary: Direct inhibition of FXa has been proven effective in anticoagulation with minimal bleeding risks. A novel series of anthranilamide derivatives were designed and synthesized to improve selectivity and physicochemical properties. These compounds showed potent FXa inhibitory activities and high selectivity over thrombin, as well as good anticoagulant activity and safety in animal models.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Oncology
Esther P. Jane, Matthew C. Reslink, Taylor A. Gatesman, Matthew E. Halbert, Tracy A. Miller, Brian J. Golbourn, Stephanie M. Casillo, Steven J. Mullett, Stacy G. Wendell, Udochukwu Obodo, Dinesh Mohanakrishnan, Riya Dange, Antony Michealraj, Charles Brenner, Sameer Agnihotri, Daniel R. Premkumar, Ian F. Pollack
Summary: In previous studies, the combination of panobinostat and bortezomib showed synergistic therapeutic activity against high-grade gliomas but resistance eventually emerged. In this study, the authors investigated the molecular mechanisms underlying the anticancer effects of panobinostat and marizomib, and identified glycolysis and the electron transport chain (ETC) as potential targets for overcoming resistance. In vivo experiments using a glycolysis and mitochondrial function inhibitor confirmed the efficacy of targeting these pathways. These findings provide new insights into treatment resistance in gliomas.
MOLECULAR ONCOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Ashish M. Kanhed, Dushyant V. Patel, Nirav R. Patel, Anshuman Sinha, Priyanka S. Thakor, Kishan B. Patel, Navnit K. Prajapati, Kirti V. Patel, Mange Ram Yadav
Summary: To confront the complex pathogenesis of Alzheimer's disease, the development of multitarget-directed ligands has emerged as a promising approach. In this study, a series of indoloquinoxaline derivatives were designed and synthesized for Alzheimer's disease. The synthesized compounds exhibited moderate to good cholinesterase inhibitory activity and compound 9f was identified as the most potent and selective BuChE inhibitor. Compound 9f also showed self-induced Aβ(1-42) aggregation inhibitory activity and favorable in silico ADMET properties. These findings suggest that compound 9f has potential as a multitarget-directed ligand for developing novel anti-AD drugs.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(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)
