Article
Chemistry, Inorganic & Nuclear
Alba Hernandez-Garcia, Lenka Markova, Maria Dolores Santana, Jitka Pracharova, Delia Bautista, Hana Kostrhunova, Vojtech Novohradsky, Viktor Brabec, Jose Ruiz, Jana Kasparkova
Summary: This study presents the synthesis and characterization of six new heteroleptic osmium(II) complexes with varying substituents in the R3 position of the phenyl ring of the cyclometalating C^N ligand. These complexes are highly kinetically inert and absorb a full-wavelength range of visible light. The antiproliferative activity of these complexes has been investigated using human cancer and noncancerous cell cultures, showing that they are more potent than conventional cisplatin. The mechanism of action involves the activation of the endoplasmic reticulum stress pathway and disruption of calcium homeostasis.
INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Menier Al-Anazi, Melati Khairuddean, Belal O. Al-Najjar, Mohammad Murwih Alidmat, Nik Nur Syazni Nik Mohamed Kamal, Musthahimah Muhamad
Summary: This article introduces the design and synthesis of new chalcone, pyrazoline, and pyrimidine derivatives as potential EGFR kinase inhibitors, and evaluates their binding affinities and anticancer activities.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Lamya H. Al-Wahaibi, Hesham A. Abou-Zied, Eman A. M. Beshr, Bahaa G. M. Youssif, Alaa M. Hayallah, Mohamed Abdel-Aziz
Summary: New Bis-pyrazoline hybrids 8-17 with dual EGFR and BRAF(V600E) inhibitors were developed and tested against four cancer cell lines in vitro. Compounds 12, 15, and 17 showed strong antiproliferative activity with GI(50) values of 1.05 μM, 1.50 μM, and 1.20 μM, respectively. These hybrids demonstrated dual inhibition of EGFR and BRAFV600E and exhibited promising anticancer activity, especially compound 12. Molecular docking studies supported their potential as dual EGFR/BRAFV600E inhibitors. Additionally, in silico ADMET prediction revealed low toxicity and adverse effects of the synthesized bis-pyrazoline hybrids.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Physical
Umut Dogan, Ozge Ozcan, Gizem Alaca, Aydan Ari, Salih Gunnaz, H. Tansel Yalcin, Onur Sahin, Sevil Irisli
Summary: Three new Platinum complexes were synthesized and characterized, showing moderate cytotoxic activities against cancer cell lines and antimicrobial effects on both gram positive and gram negative bacteria.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Pharmacology & Pharmacy
Min Dong, Guili Zheng, Feng Gao, Min Li, Chen Zhong
Summary: A series of dihydroartemisinin-isatin hybrids were designed and synthesized, and their antiproliferative activity against lung cancer cell lines was evaluated. The hybrids showed significant activity, surpassing the activity of dihydroartemisinin and artemisinin. In particular, hybrid 6a demonstrated comparable activity to common chemotherapeutic drugs and showed higher potency against multidrug-resistant lung cancer cell lines. Furthermore, hybrid 6a exhibited good selectivity and stability, making it a promising candidate for further development as an anti-lung cancer chemotherapeutic agent.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Anita Raducka, Marcin Swiatkowski, Izabela Korona-Glowniak, Barbara Kapron, Tomasz Plech, Malgorzata Szczesio, Katarzyna Gobis, Malgorzata Iwona Szynkowska-Jozwik, Agnieszka Czylkowska
Summary: In this study, a series of coordination compounds containing zinc and benzimidazole derivatives were synthesized and characterized using various analytical and spectroscopic techniques. The results indicated that these new compounds showed improved anticancer properties, as well as antibacterial and antifungal activities, demonstrating potential as antitumor agents.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Antonino N. Fallica, Valeria Ciaffaglione, Maria N. Modica, Valeria Pittala, Loredana Salerno, Emanuele Amata, Agostino Marrazzo, Giuseppe Romeo, Sebastiano Intagliata
Summary: The overexpression of sigma receptors in tumors has prompted a deep investigation of their role in cancer pathophysiology. Sigma receptor ligands are gaining attention due to their potential as anticancer agents and imaging tracers.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Inorganic & Nuclear
Delia Hernandez-Romero, Sharon Rosete-Luna, Aracely Lopez-Monteon, Aracely Chavez-Pina, Nury Perez-Hernandez, Jazmin Marroquin-Flores, Antonio Cruz-Navarro, Gustavo Pesado-Gomez, David Morales-Morales, Raul Colorado-Peralta
Summary: Cancer is characterized by irregular cell cycle function and uncontrolled cell growth. Chemotherapy is effective but often faces issues such as limited efficacy and drug resistance. Research on first-row transition metal compounds containing benzimidazole ligands may lead to the development of novel and potent metallodrugs.
COORDINATION CHEMISTRY REVIEWS
(2021)
Article
Biochemistry & Molecular Biology
Mariam M. Fakhry, Amr A. Mattar, Marwa Alsulaimany, Ebtesam M. Al-Olayan, Sara T. Al-Rashood, Hatem A. Abdel-Aziz
Summary: A new series of thiazolyl-pyrazoline derivatives have been designed and synthesized, and they exhibit potent anticancer activity against breast cancer cells and dual inhibitory activity against EGFR and HER2.
Review
Biochemistry & Molecular Biology
Qing-Shan Li, Bang-Nian Shen, Zhen Zhang, Shuying Luo, Ban-Feng Ruan
Summary: Substituted pyrazole derivatives, as nitrogen-containing five-membered heterocyclic structural units, exhibit a wide range of pharmacological activities, especially the 2-pyrazolines known as 4,5-dihydro-1H-pyrazoles. Studies since 2010 have shown that 2-pyrazoline derivatives have potent anti-cancer activities, which could provide important pharmacophore clues for the discovery of new anti-cancer agents. This review covers literature-reported pyrazoline derivatives from 2010 to 2019 and aims to establish the relationship between anticancer activities variation and different substituents introduced into a 2-pyrazoline core.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Anja Bec, Lucija Hok, Leentje Persoons, Els Vanstreels, Dirk Daelemans, Robert Vianello, Marijana Hranjec
Summary: The study prepared a series of novel acrylonitrile compounds using different synthesis methods, showing strong anti-proliferative activity against malignant tumor cells with good selectivity towards normal cells. The compounds were also tested for their inhibition of tubulin polymerization in vitro, revealing a potential mechanism of action for their biological activity.
Article
Biochemistry & Molecular Biology
Luka Krstulovic, Katarina Miskovic Spoljaric, Vesna Rastija, Nikolina Filipovic, Miroslav Bajic, Ljubica Glavas-Obrovac
Summary: Novel quinoline-benzimidazole hybrids containing two types of triazole-methyl-phenoxy linkers were synthesized and characterized. The derivatives were tested for their effects on different cell lines, and their inhibitory effects on lymphoma cell growth were found to be the most potent. The synthesized compounds violated at most two of Lipinski's rules, but showed potential as drug candidates.
Article
Chemistry, Multidisciplinary
Thi-Dan Thach, T. My-Thao Nguyen, T. Anh-Thu Nguyen, Chi-Hien Dang, Thanh-Binh Luong, Van-Su Dang, Kien-Sam Banh, Van-Sieu Luc, Thanh-Danh Nguyen
Summary: Novel 1,3,5-substituted pyrazoline sulphonamides were synthesized and evaluated for their antimicrobial, antiproliferative, and anti-inflammatory properties, showing promising potential for drug discovery.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Rasha A. Hassan, Soha H. Emam, Dukhyun Hwang, Gun-Do Kim, Soha O. Hassanin, Mona G. Khalil, Amr M. Abdou, Amr Sonousi
Summary: Two series of pyrazoline compounds were synthesized as antiproliferative agents targeting the VEGFR pathway. Compound 3f showed the highest anticancer activity against ovarian and breast cancer cell lines, inhibiting cell proliferation and inducing apoptosis. It also down-regulated the expression of VEGF and p-VEGFR-2. Docking studies revealed its similar interaction pattern to axitinib on VEGFR-2 receptor and its ability to fit into the STAT3 binding site, explaining the down-regulation of VEGF.
BIOORGANIC CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Dumitrela Diaconu, Vasilichia Antoci, Violeta Mangalagiu, Dorina Amariucai-Mantu, Ionel I. Mangalagiu
Summary: Two new classes of hybrid quinoline-imidazole/benzimidazole derivatives were designed and synthesized to evaluate their anticancer and antimicrobial activity. The results showed that certain compounds exhibited excellent nonselective or selective anticancer activity against different cancer cell lines, as well as good antimicrobial activity against Gram-negative bacteria and one compound against Gram-positive bacteria. These findings suggest that these compounds have the potential to be candidates for future drug development.
SCIENTIFIC REPORTS
(2022)
Review
Chemistry, Organic
Ajay Kumar, Salahuddin, Avijit Mazumder, Mohammad Shahar Yar, Rajnish Kumar, Mohamed Jawed Ahsan
Summary: Quinoline and its derivatives show high activity against various cancer cells and can serve as potential lead compounds for anticancer drug research. These drugs have potential therapeutic effects on various cancers such as prostate cancer and breast cancer.
MINI-REVIEWS IN ORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Nida Nehal, Bushra Nabi, Saleha Rehman, Ankita Pathak, Ashif Iqubal, Saif Ahmad Khan, M. Shahar Yar, Suhel Parvez, Sanjula Baboota, Javed Ali
Summary: The research developed a Ropinirole hydrochloride nanoemulsion for Parkinson's disease treatment, showing promising results in in vitro release and permeation studies. The formulation exhibited enhanced transmittance and stable pH, suggesting potential for improved management of PD symptoms.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Chemistry, Physical
Rajarshi Nath, M. Shahar Yar, Shelly Pathania, Gourav Grover, Biplab Debnath, Md Jawaid Akhtar
Summary: A series of novel anticonvulsant compounds were designed and synthesized, with the most active compound N-(5-chlorobenzo[d]thiazol-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a) showing significant anticonvulsant activity and potential pharmaceutical value. In silico studies and molecular docking were conducted to investigate the molecular interactions and drug likeness properties of the compounds.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Pharmacology & Pharmacy
Noorul Hasan, Saima Zameer, Abul Kalam Najmi, Suhel Parvez, Mohammad Shahar Yar, Mohd Akhtar
Summary: The study explored the therapeutic potential of RFM and TDF phosphodiesterase inhibitors in treating AD induced by ICV Aβ1-42 in rats. RFM and TDF were found to significantly attenuate memory deficits and neuropathological alterations induced by Aβ1-42.
PHARMACOLOGICAL REPORTS
(2021)
Article
Chemistry, Multidisciplinary
Mohammad Mustaqeem Abdullah, Nasir A. Siddiqui, Ramzi A. Mothana, Fahd A. Nasr, Adnan J. Al-Rehaily, Omer M. Almarfadi, Shahid Karim, Kashif Haider, Md Rafi Haider, M. Shahar Yar
Summary: Benzofuran is a heterocyclic scaffold found in natural products with anti-tubercular activity. A novel series of compounds containing 3-chlorobenzofuran derivatives were designed, synthesized, and screened in vitro, with compound 3b showing the strongest inhibitory potency.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Kashif Haider, Sara Rehman, Ankita Pathak, Abul K. Najmi, Mohammad S. Yar
Summary: Targeted therapy is crucial in cancer treatment, overcoming drawbacks of conventional therapy. Heterocyclic derivatives have gained attention as cytotoxic agents, with benzothiazole being explored for its therapeutic potential. Benzothiazole-based derivatives have emerged as potent inhibitors of enzymes, with some already in clinical trials. This review highlights recent advancements in benzothiazole-based derivatives as potent anticancer agents.
ARCHIV DER PHARMAZIE
(2021)
Review
Chemistry, Medicinal
Divya Sharma, Salahuddin, Vikas Sharma, Rajnish Kumar, Sagar Joshi, Sunita Kumari, Shivani Saxena, Avijit Mazumder, Mohammad Shahar Yar, Mohamed Jawed Ahsan
Summary: This paper summarizes the general synthetic methods and anticancer activity of 1,3,4-oxadiazole, discusses the different receptors on which these drugs act, and presents pharmacophore models for topoisomerase-I, histone deacetylase, and epidermal growth factor enzymes.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Organic
Devleena Tiglani, Salahuddin, Avijit Mazumder, Mohammad Shahar Yar, Rajnish Kumar, Mohamed Jawed Ahsan
Summary: Benzimidazole and quinoline are compounds with broad spectrum activities in various pharmacological fields, and their hybrid structures have shown positive results against different diseases.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Review
Pharmacology & Pharmacy
Kashif Haider, Anku Sharma, M. Shahar Yar, Prasanna Anjaneyulu Yakkala, Syed Shafi, Ahmed Kamal
Summary: This review article summarizes the developments of small molecule KRAS inhibitors as drug candidates and the rational approaches for selectively targeting KRAS signaling in mutant cancer cells. After achieving initial success in targeting the mutant KRAS G12C variants, the current challenge is to address the resistance and efficacy issues of small molecule KRAS inhibitors. In the development of KRAS targeted therapies, the design of small molecule inhibitors that can inhibit KRAS signaling and also target other signaling pathways like RAS-SOS and RAS-PI3K needs to be extensively explored.
EXPERT OPINION ON DRUG DISCOVERY
(2022)
Review
Chemistry, Medicinal
Kashif Haider, Subham Das, Alex Joseph, M. Shahar Yar
Summary: Heterocyclic compounds containing quinazoline and quinazolinone core have shown high efficacy in cancer treatment and have been widely used in clinical practice. These drugs work by different pathways to prevent the progression of cancer cells, achieving significant results.
DRUG DEVELOPMENT RESEARCH
(2022)
Review
Chemistry, Medicinal
Shaikh Yahya, Kashif Haider, Ankita Pathak, Akram Choudhary, Pooja Hooda, Mohd Shafeeq, Mohammad Shahar Yar
Summary: Heterocyclic scaffolds of natural and synthetic origin offer a wide range of pharmacological activities, including ALR2 inhibitors for the treatment of complications related to diabetes. This study summarizes the recent developments in the pharmacologically active ALR2 heterocyclic scaffold and discusses the design, structure-activity relationships, and biological studies of these molecules.
ARCHIV DER PHARMAZIE
(2022)
Review
Chemistry, Organic
Abhishek Shankar Sharma, Salahuddin, Avijit Mazumder, Rajnish Kumar, Vimal Datt, Km Shabana, Sonakshi Tyagi, Mohammad Shahar Yar, Mohamed Jawed Ahsan
Summary: Due to their diverse applications, quinoline and 1,3,4-oxadiazole have become important heterocyclic compounds in industrial and synthetic organic chemistry. They have shown potential in various medical conditions and synthetic protocols have been developed to explore their structure-activity relationship for further research.
CURRENT ORGANIC SYNTHESIS
(2023)
Review
Biochemistry & Molecular Biology
Vikas Pradhan, Salahuddin Salahuddin, Rajnish Kumar, Avijit Mazumder, Mohammad Mustaqeem Abdullah, Mohammad Shahar Yar, Mohamed Jawed Ahsan, Zabih Ullah
Summary: Cancer is a leading cause of death worldwide, posing substantial risks to society and individuals. Despite advances in cancer prevention, therapy remains challenging. Therefore, continuous research is being conducted to search for novel anticancer agents with broader cytotoxicity range. Quinoline derivatives, which are double ring structures of the heterocyclic aromatic nitrogen molecule formed by the fusion of a benzene ring and a pyridine ring at two carbon atoms close to each other, have been found to possess a wide range of pharmacological activities, including anticancer properties. Many quinoline derivatives are available as anticancer drugs, targeting various molecular mechanisms such as topoisomerase inhibition, tyrosine kinases inhibition, heat shock protein 90 (Hsp90) inhibition, histone deacetylases (HDACs) inhibition, cell cycle arrest and apoptosis inhibition, and tubulin polymerization inhibition.
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Review
Chemistry, Medicinal
Vivek K. Gour, Shaikh Yahya, Mohammad Shahar Yar
Summary: Oxadiazoles and thiadiazoles have versatile biological applications and stability, making them potential candidates for the development of new drugs.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Organic
Ajay Kumar, Salahuddin, Avijit Mazumder, Rajnish Kumar, Rakesh Sahu, Shivali Mishral, Chanchal Singh, Mohammad Shahar Yar, Mohamed Jawed Ahsan
Summary: The study synthesized and evaluated a series of quinoline derivatives with promising anti-diabetic potentials, especially compound 4e and 4d showing excellent activity. These compounds exhibited better activity compared to the standard drug pioglitazone, indicating the potential for developing new and more effective anti-diabetic agents.
INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY
(2021)
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)