Review
Chemistry, Inorganic & Nuclear
Rakesh Kumar Gupta, Parashuram Kallem, Geng-Geng Luo, Ping Cui, Zhi Wang, Fawzi Banat, Chen-Ho Tung, Di Sun
Summary: Metal-organic frameworks (MOFs) are crystalline materials with unique and tunable properties, which have been widely used in various applications, especially in sensing, catalysis, drug delivery, and luminescence. This review summarizes the design, synthesis, and applications of these MOFs, and discusses the future development in this field.
COORDINATION CHEMISTRY REVIEWS
(2023)
Article
Chemistry, Physical
Bakr F. Abdel-Wahab, Benson M. Kariuki, Hanan A. Mohamed, Mohamed S. Bekheit, Hanem M. Awad, Gamal A. El-Hiti
Summary: The synthesis of heterocycles containing 1,2,3-triazole and pyrazole moieties has been explored for their potential applications in the agrochemical and pharmaceutical fields. These heterocycles have shown promising anti-proliferation properties against cancer cells. In this study, several new 1H-1,2,3-triazole derivatives were successfully synthesized using simple procedures, and their activity against different types of cancer cells and normal cells was evaluated.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Zhiwei Zeng, Yuji Liu, Wei Huang, Jean'ne M. Shreeve, Yongxing Tang
Summary: A facile and efficient nitrogen-centered-radical-mediated approach to cleave C-N bonds in a monocyclic pyrazole has been described. The reaction achieved high yields and led to an energetic compound with promising application prospects.
JOURNAL OF MATERIALS CHEMISTRY A
(2022)
Article
Biochemistry & Molecular Biology
Gita Matuleviciute, Egle Arbaciauskiene, Neringa Kleiziene, Vilija Kederiene, Greta Ragaite, Migle Dagiliene, Aurimas Bieliauskas, Vaida Milisiunaite, Frank A. Slok, Algirdas Sackus
Summary: A series of novel heterocyclic amino acid compounds were developed and regioselectively synthesized as N-Boc protected esters, serving as achiral and chiral building blocks. The structures of these compounds were confirmed through H-1, C-13, and N-15-NMR spectroscopy and HRMS investigation.
Article
Chemistry, Physical
Kayed Abu-Safieh, Musa El-Barghouthi, Monther A. Khanfar, Bader A. Salameh, Islam S. Al-Aqrabawi, Baker Jawabrah Al Hourani, Basem F. Ali
Summary: The title compound with three independent molecules in the asymmetric unit forms a compact 3D supramolecular structure through hydrogen bonding. Molecular docking techniques were used to study interactions with proteins and interpret cytotoxic activities against cancer cell lines. Strong interactions were observed between the title compound and a closely related structure with modifications at position 5 in the pyrazole ring.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Physical
Km Pooja, Aysha Fatima, Arun Sharma, Km Garima, Sandhya Savita, Mukesh Kumar, Indresh Verma, Nazia Siddiqui, Saleem Javed
Summary: In this study, the drug Fomepizole was investigated experimentally and theoretically. Theoretical calculations using Density Functional Theory (DFT) and Hirshfeld surface analysis were conducted to optimize and analyze the molecular structure, vibrational modes, and chemical activity. The analysis of electronic properties, intermolecular interactions, and drug-likeness was also performed.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Sarah Preston, Jose Garcia-Bustos, Liam G. Hall, Sheree D. Martin, Thuy G. Le, Abhijit Kundu, Atanu Ghoshal, Nghi H. Nguyen, Yaqing Jiao, Banfeng Ruan, Lian Xue, Fei Huang, Bill C. H. Chang, Sean L. McGee, Timothy N. C. Wells, Michael J. Palmer, Abdul Jabbar, Robin B. Gasser, Jonathan B. Baell
Summary: A series of novel compounds were synthesized as potent inhibitors of Haemonchus contortus, the parasitic nematode of sheep, showing high selectivity in mammalian cell lines but causing acute toxicity in rodents, possibly due to respiratory inhibition. Additionally, potent cytotoxicity was observed in rat hepatocytes, unrelated to toxicity in respiring cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Xiaosheng Luo, Ping Wang
Summary: In this study, the conversion of 4-aryl-1,4-dihydropyridines (DHPs) into ynones under electrochemical conditions is reported. The reaction proceeds via the homolysis of acyl-DHP under electron activation and resulting acyl radicals react with hypervalent iodine(III) reagents to form the target ynones or ynamides in acceptable yields. This methodology shows wider functionality tolerance and synthetic utility for late-stage modification of complex molecules.
Article
Biochemistry & Molecular Biology
Biruk Sintayehu Fanta, Laychiluh Mekonnen, Sunita K. C. Basnet, Theodosia Teo, Jimma Lenjisa, Nishat Z. Khair, Lianmeng Kou, Solomon Tadesse, Matthew J. Sykes, Mingfeng Yu, Shudong Wang
Summary: CDK2 deregulation is associated with various human cancers and resistance to anticancer drugs. Bioisosteric replacement of CDKI-73 by a pyrazole group yielded compounds with potent CDK2 inhibition and antiproliferative activity against cancer cell lines. The results highlight the potential of the 2-anilino-4-(1-methyl-1H- pyrazol-4-yl)pyrimidine series in developing selective CDK2 inhibitors for cancer treatment.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Khalid Karrouchi, Silvia A. Brandan, Yusuf Sert, Miloud El Karbane, Smaail Radi, Marilena Ferbinteanu, Yann Garcia, M'hammed Ansar
Summary: In this study, (E)-N'-4-methoxybenzylidene-5-methyl-1H-pyrazole-3-carbohydrazide was synthesized and characterized, and its properties were investigated using various experimental and computational methods. The compound showed potential as an anti-diabetic agent in molecular docking studies with 4AMJ protein.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Inorganic & Nuclear
Liu Lu, Cheng Mei-Ling, Tang Li-Zhi-Peng, Liu Zheng, Liu Qi
Summary: In the absence/presence of chelating N ancillary ligand, treatment of 5-methyl-1H-pyrazole-3-carboxylic acid with corresponding Mn(II)/Ni(II) metal salts yielded two complexes with distinct molecular networks, leading to the formation of a 3D supramolecular structure and a chainlike structure, respectively. The structures of the two complexes were analyzed, revealing different coordination geometries for each metal ion and the role of intermolecular hydrogen bonds in shaping their supramolecular architectures. Additionally, the electrochemical and luminescent properties of the complexes were investigated, providing insights into their potential applications.
CHINESE JOURNAL OF INORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ru Dong, Cheng Zhang, Chao Wang, Xin Zhou, Wen Li, Jin-Yang Zhang, Min Wang, Yong Xu, Li-Ping Sun
Summary: This study designed a new series of 3-methyl-1H-indazole derivatives targeting the inhibitory activities of protein BRD4-BD1 and cancer cell proliferation. Compound 9d showed excellent selectivity for BRD4 and effectively suppressed c-Myc. The study provided new lead compounds for further evaluation on BRD4.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Tukaram S. Choudhare, Devendra S. Wagare, Sagar E. Shirsath, Prashant D. Netankar
Summary: By utilizing formic acid as a medium, one-pot condensation of pyrazole-4-aldehydes and hydroxylamine hydrochloride, followed by dehydration with a catalytic amount of orthophosphoric acid, leads to the formation of novel pyrazole-4-carbonitrile. This metal-free and cost-effective method yields excellent results and provides a versatile precursor for the synthesis of various valuable compounds.
JOURNAL OF CHEMICAL SCIENCES
(2021)
Article
Crystallography
David Kocovic, Snezana Mugosa, Sergiu Shova, Zoran D. Tomic, Zeljko K. Jacimovic
Summary: This is an article describing the crystal structure of a certain organic compound.
ZEITSCHRIFT FUR KRISTALLOGRAPHIE-NEW CRYSTAL STRUCTURES
(2023)
Article
Chemistry, Medicinal
Yunong Zhang, Shinpan Chan, Rui He, Yiling Liu, Xiaojuan Song, Zheng-Chao Tu, Xiaomei Ren, Yang Zhou, Zhang Zhang, Zhen Wang, Fengtao Zhou, Ke Ding
Summary: A newly designed RET kinase inhibitor was found to effectively suppress resistant mutants and exhibit significant anti-tumor efficacy in cell and mouse models.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Oncology
Demet Celebi, Ali Taghizadehghalehjoughi, Sumeyye Baser, Sidika Genc, Aysegul Yilmaz, Yesim Yeni, Fatma Yesilyurt, Serkan Yildirim, Ismail Bolat, Saban Kordali, Ferah Yilmaz, Ahmet Hacimuftuoglu, Ozgur Celebi, Denisa Margina, George Mihai Nitulescu, Demetrios A. A. Spandidos, Aristidis Tsatsakis
Summary: This study investigated the effect of boric acid and potassium metaborate on MRSA infection. The results showed that potassium metaborate was more effective and less toxic to fibroblast cells compared to boric acid. It also decreased the level of prooxidant species and increased the antioxidant status more effectively. Furthermore, both boric acid and potassium metaborate significantly decreased the expression levels of inflammatory markers.
MOLECULAR MEDICINE REPORTS
(2022)
Article
Infectious Diseases
Christina Zalaru, Florea Dumitrascu, Constantin Draghici, Isabela Tarcomnicu, Maria Marinescu, George Mihai Nitulescu, Rodica Tatia, Lucia Moldovan, Marcela Popa, Mariana Carmen Chifiriuc
Summary: A new series of pyrazolo-benzimidazole hybrid Mannich bases were synthesized and characterized. In vitro cytotoxicity tests showed that the compounds were noncytotoxic at a certain concentration and exhibited high biocompatibility. The newly synthesized compounds demonstrated good antibacterial and antibiofilm activity against several bacterial strains.
Article
Plant Sciences
Liliana Costea, Carmen Lidia Chitescu, Rica Boscencu, Manuela Ghica, Dumitru Lupuliasa, Dragos Paul Mihai, Teodora Deculescu-Ionita, Ligia Elena Dutu, Maria Lidia Popescu, Emanuela-Alice Luta, George Mihai Nitulescu, Octavian Tudorel Olaru, Cerasela Elena Gird
Summary: Oxidative stress is a major factor in human functional disorders, and this study aimed to obtain standardized plant extracts containing active compounds that protect liver cells against free radicals. The extracts were analyzed to identify and quantify therapeutic compounds using UHPLC-HRMS/MS. The extracts contained various flavonoids, phenolic acids, and polyphenols. In vitro experiments confirmed the extracts' antioxidant activity, and a correlation was found between the content of polyphenolic compounds and the antioxidant effect. The extracts also showed hepatoprotective potential in silico. This study validates the use of these extracts in phytotherapy due to their ability to reduce oxidative stress and protect liver cells.
Article
Engineering, Chemical
Theodora-Venera Apostol, Mariana Carmen Chifiriuc, Laura-Ileana Socea, Constantin Draghici, Octavian Tudorel Olaru, George Mihai Nitulescu, Diana-Carolina Visan, Luminita Gabriela Marutescu, Elena Mihaela Pahontu, Gabriel Saramet, Stefania-Felicia Barbuceanu
Summary: In this article, the design and synthesis of novel compounds containing an L-valine residue and a 4-[(4-bromophenyl)sulfonyl]phenyl moiety were presented. These compounds belong to various chemotypes and were characterized through different techniques. The compounds were then tested for antimicrobial activity, antioxidant effect, and toxicity. In silico studies were also performed. The results showed promising potential for developing novel antimicrobial agents.
Article
Plant Sciences
Emanuela Alice Luta, Andrei Bita, Alina Morosan, Dan Eduard Mihaiescu, Manuela Ghica, Dragos Paul Mihai, Octavian Tudorel Olaru, Teodora Deculescu-Ionitaa, Ligia Elena Dutu, Maria Lidia Popescu, Liliana Costea, George Mihai Nitulescu, Dumitru Lupuliasa, Rica Boscencu, Cerasela Elena Gird
Summary: This study investigated the impact of phytosociological cultivation and fertilization on the polyphenolic content of peppermint and lemon balm leaves. The results showed that phytosociological cultivation and the use of organic fertilizers increased the concentration of polyphenols and enhanced the antioxidant activity of the extracts.
Article
Chemistry, Medicinal
Ana-Madalina Maciuca, Alexandra-Cristina Munteanu, Mirela Mihaila, Mihaela Badea, Rodica Olar, George Mihai Nitulescu, Cristian V. A. Munteanu, Valentina Uivarosi
Summary: Drug repositioning was used to discover new applications for nalidixic acid, which is a member of the quinolone class. Nine new metal complexes with lanthanide cations were synthesized and their cytotoxicity, DNA affinity, and serum protein affinity were studied. The complexes exhibited selective activity against LoVo and preferred binding to the major and minor grooves of DNA.
Review
Biochemistry & Molecular Biology
Laura-Ileana Socea, Stefania-Felicia Barbuceanu, Elena Mihaela Pahontu, Alexandru-Claudiu Dumitru, George Mihai Nitulescu, Roxana Corina Sfetea, Theodora-Venera Apostol
Summary: Acylhydrazones exhibit various pharmacological activities and can be used for the treatment of multiple diseases. Due to their importance in several drugs, studying the structural and biological properties of these compounds is beneficial.
Article
Pharmacology & Pharmacy
Corina Andrei, Dragos Paul Mihai, Anca Zanfirescu, George Mihai Nitulescu, Simona Negres
Summary: This study aimed to develop a computational framework to predict potential TRPV1 ligands among approved drugs for treating different types of pain. The researchers built predictive models and validated them using molecular docking and neural network algorithms. After screening and validation, certain approved drugs were identified as potential TRPV1 agonists or antagonists. However, further research is needed to confirm the predicted activity and evaluate the efficacy of these candidate drugs in alleviating pain.
Review
Plant Sciences
Corina Andrei, Anca Zanfirescu, George Mihai Nitulescu, Octavian Tudorel Olaru, Simona Negres
Summary: This narrative review aims to summarize the diverse natural scaffolds of TRPV1 modulators and analyze the structure-activity relationships between the ligands and molecular targets. The authors provide an exhaustive collection of TRPV1 modulators grouped by relevant chemical features, hoping that this information will contribute to the design of novel effective and safe TRPV1 modulators.
Article
Biochemistry & Molecular Biology
Stefania-Felicia Barbuceanu, Elena-Valentina Rosca, Theodora-Venera Apostol, Laura-Ileana Socea, Constantin Draghici, Ileana Cornelia Farcasanu, Lavinia Liliana Ruta, George Mihai Nitulescu, Lucian Iscrulescu, Elena-Mihaela Pahontu, Rica Boscencu, Gabriel Saramet, Octavian Tudorel Olaru
Summary: This paper describes the synthesis of new heterocycles from oxazol-5(4H)-one and 1,2,4-triazin-6(5H)-one classes containing a phenyl-/4-bromophenylsulfonylphenyl moiety. The compounds were characterized using spectral and elemental analysis. Toxicity assays on Daphnia magna and Saccharomyces cerevisiae showed that the heterocyclic nucleus and halogen atoms significantly influenced the toxicity. The compounds also showed potential for anticancer investigations based on predictive analyses and similarity studies.
Review
Biochemistry & Molecular Biology
George Mihai Nitulescu, Gheorghe Stancov, Oana Cristina Seremet, Georgiana Nitulescu, Dragos Paul Mihai, Cosmina Gabriela Duta-Bratu, Stefania Felicia Barbuceanu, Octavian Tudorel Olaru
Summary: The altered activation or overexpression of protein kinases is a major focus in cancer research, and using small molecule protein kinase inhibitors is the best option for cancer treatment. The pyrazole ring is widely used in medicinal chemistry and drug development strategies, playing a crucial role as a fundamental framework in the structure of protein kinase inhibitors.
Review
Plant Sciences
Cosmina-Gabriela Duta-Bratu, George Mihai Nitulescu, Dragos Paul Mihai, Octavian Tudorel Olaru
Summary: The use of natural compounds a an alternative to synthetic molecules has gained significant interest. Stilbenoids, especially resveratrol, have been extensively studied for their therapeutic potential in various diseases. Natural stilbenes possess diverse biological activities and their chemical structures and sources simplify compound isolation and drug design. While resveratrol is well-studied, further research is needed to explore the therapeutic potential of other less popular stilbenoid compounds.
Article
Chemistry, Medicinal
Corina Andrei, Dragos Paul Mihai, Georgiana Nitulescu, Anca Ungurianu, Denisa Marilena Margina, George Mihai Nitulescu, Octavian Tudorel Olaru, Radu Mihai Busca, Anca Zanfirescu
Summary: This study found that cetirizine exhibits anti-inflammatory and analgesic effects in osteoarthritis, making it a promising starting point for the development of new drugs for the treatment of this condition.
Article
Biology
George Nicolae Daniel Ion, George Mihai Nitulescu, Dragos Paul Mihai
Summary: PIM-1 kinase has implications in multiple types of malignancies. Developing better search methodologies for inhibitors and using post-processing docking results can improve drug discovery success rates.
Review
Biochemistry & Molecular Biology
Georgiana Nitulescu, Dumitru Lupuliasa, Ines Adam-Dima, George Mihai Nitulescu
Summary: This review provides an overview of UV filters in sunscreen products, discussing their classification, structural characteristics, photostability, mechanism of action, optical properties, and regulatory status based on their chemical structure. Major classes of organic UV filters include aminobenzoic acid derivatives, salicylic acid derivatives, cinnamic acid derivatives, benzophenones, dibenzoylmethane derivatives, benzylidene camphor derivatives, triazines, benzimidazole derivatives, and benzotriazole derivatives. The pursuit of new UV filters through research is crucial for advancing sunscreen technology and ensuring effective and safe sun protection options.
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)