Article
Biochemistry & Molecular Biology
Xin Zhang, Tingting Yang, Xin Jin, Kaige Lin, Xiling Dai, Ting Gao, Guozheng Huang, Minghui Fan, Liang Ma, Zi Liu, Jianguo Cao
Summary: In this study, podophyllotoxin derivatives incorporating piperazinyl-cinnamic amide moieties at the 4-position were synthesized. Compound 6e showed the best anti-proliferative properties and inhibited mitochondria-associated apoptosis in MCF-7 cells.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Dalal Sulaiman Alshaya, Rana M. O. Tawakul, Islam Zaki, Ali H. Abu Almaaty, Eman Fayad, Yasmin M. Abd El-Aziz
Summary: A new series of acrylic acid and acrylate ester derivatives were synthesized and evaluated for their antiproliferative activity against MCF-7 breast carcinoma cells. Methyl acrylate ester 6e showed the highest cytotoxicity with an IC50 value of 2.57 +/- 0.16 mu M and exhibited inhibition of beta-tubulin polymerization. Compound 6e arrested MCF-7 cells at the G2/M phase and enhanced apoptotic power, while also affecting the gene expression levels of p53, Bax, and Bcl-2.
Article
Biochemistry & Molecular Biology
Baoxia Liang, Qing Zou, Lintao Yu, Yali Wang, Jun Yan, Baiqi Huang
Summary: Novel indole-containing hybrids derived from Millepachine were synthesized and evaluated for their antitumor activities. Compound 14b showed the most potent cytotoxic activity against human cancer cell lines, being almost 100 times more active than Millepachine. It also demonstrated low cytotoxicity towards normal human cells and equivalent sensitivity towards drug-resistant cells, highlighting its potential for the development of antitumor drugs.
Article
Chemistry, Multidisciplinary
Heba M. Abosalim, Manal A. Nael, Tarek F. El-Moselhy
Summary: Twenty derivatives of chalcones were synthesized and evaluated for their anticancer activities, with five compounds showing broad antitumor activity against breast and liver cancer cell lines. Compound 3 h exhibited the most powerful anticancer activity and effective inhibition on tubulin, with low toxicity towards normal human cell lines. The docking study revealed that 3 h had the best binding mode among all the derivatives.
Article
Chemistry, Medicinal
Dong Liang, Chen Yu, Zhao Ma, Mingzhao Hu, Jiahui Wang, Xuhui Dong, Lupei Du, Minyong Li
Summary: In this study, the discovery of two series of parbendazole derivatives as tubulin inhibitors for the treatment of head and neck squamous cell carcinoma (HNSCC) was reported. Compound 9q exhibited the best pharmacological activities and pharmacokinetic properties, displaying reasonable inhibition activity on cell proliferation, induction of cell apoptosis, and suppression of cell migration and invasion.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Lingyu Shi, Shanbo Yang, Jing Chang, Yujing Zhang, Wenjing Liu, Jun Zeng, Jingsen Meng, Renshuai Zhang, Chao Wang, Dongming Xing
Summary: A series of new compounds were synthesized and evaluated for their antitumor activity as tubulin polymerization inhibitors. Compound 7k showed the strongest anti-proliferative activity and could block the cell cycle and induce apoptosis.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Mei-Mei Li, Hui Huang, Yiru Pu, Wanrong Tian, Yun Deng, Jun Lu
Summary: The fusion of pyrazole scaffold with other skeletons creates attractive molecules with significant biological and chemical potential in medicinal chemistry. Over the past few decades, numerous biologically active molecules featuring fused pyrazole moieties have been discovered and synthesized, some of which have become marketed drugs. This review focuses on the biological importance of fused pyrazoles and highlights recent progress in their synthesis over the past 10 years, while also discussing limitations, challenges, and future prospects.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Pharmacology & Pharmacy
Ashima Dhiman, Rupam Sharma, Rajesh K. Singh
Summary: Cancer, the second leading cause of death after heart disease, is characterized by the uncontrolled growth of cells. Targeting specific genes and proteins involved in the growth and survival of cancer cells has become a top priority in global research. Indole moiety, a combination of aromatic-heterocyclic compounds, has emerged as a promising scaffold for the development of anticancer drugs due to its bioavailability, unique chemical properties, and significant pharmacological behaviors. Recent advances in the medicinal chemistry of indole derivatives, including the synthesis of potential anticancer compounds and their mechanism of action, are discussed in this review.
ACTA PHARMACEUTICA SINICA B
(2022)
Article
Chemistry, Medicinal
Sisi Zhang, Min Mo, Mengfan Lv, Wen Xia, Kun Liu, Gang Yu, Jia Yu, Guangcan Xu, Xiaoping Zeng, Sha Cheng, Bixue Xu, Heng Luo, Xueling Meng
Summary: A series of novel trifluoromethylquinoline derivatives were synthesized and evaluated for their antitumor activities. Compound 6b was found to exhibit remarkable antiproliferative activities across multiple cell lines, potentially inhibiting tubulin polymerization through targeting the colchicine binding site. Docking studies confirmed the binding of compound 6b to the colchicine binding site.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Nam Q. H. Doan, Ngan T. K. Nguyen, Vu B. Duong, Ha T. T. Nguyen, Long B. Vong, Diem N. Duong, Nguyet-Thu T. Nguyen, Tuyen L. T. Nguyen, Tuoi T. H. Do, Tuyen N. Truong
Summary: This study aims to address the burden of cancer and the limitations of chemotherapy. By improving the anticancer activity of curcumin, researchers synthesized 32 asymmetric monocarbonyl analogues (MACs) fused with 1-aryl-1H-pyrazole and identified several compounds that showed potential growth inhibition against cancer cells and affected microtubule assembly activity. Three compounds were found to induce apoptosis in breast cancer cells. This study serves as a foundation for the design of promising synthetic compounds as anticancer agents in the future.
Article
Chemistry, Medicinal
Huajian Zhu, Wenlong Li, Wen Shuai, Yang Liu, Limei Yang, Yuchen Tan, Tiandong Zheng, Hong Yao, Jinyi Xu, Zheying Zhu, Dong-Hua Yang, Zhe-Sheng Chen, Shengtao Xu
Summary: Novel N-benzylbenzamide derivatives 20b and its corresponding disodium phosphate 20b-P show significant anti-cancer activity with excellent safety profile, making them promising anti-tubulin agents for further investigation in cancer therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Huajian Zhu, Wenjian Zhu, Yang Liu, Tian Gao, Jingjie Zhu, Yuchen Tan, Han Hu, Wenhao Liang, Lingyue Zhao, Jian Chen, Zheying Zhu, Jichao Chen, Jinyi Xu, Shengtao Xu
Summary: A series of novel stilbene-based derivatives were synthesized and evaluated for their dual-target inhibition of tubulin and HDAC enzymes. Compound II-19k showed significant anti-proliferative activity in K562 hematological cell line and inhibited the growth of various solid tumor cell lines. Mechanism studies revealed its ability to inhibit microtubules and HDACs, induce cell cycle arrest and apoptosis, and reduce tumor cell metastasis. In vivo antitumor assay demonstrated its superiority as a dual-target inhibitor, suppressing tumor volume and weight without apparent toxicity. Overall, the bioactivities of II-19k make it a valuable candidate for further development as an antitumor agent.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yingying Kang, Yuanyuan Pei, Jinling Qin, Yixin Zhang, Yongtao Duan, Hua Yang, Yongfang Yao, Moran Sun
Summary: A library of new pyrimidine analogs was synthesized and compound K10 showed the most potent activity against four cancer cell lines, inhibiting microtubule polymerization and inducing apoptosis in HepG2 cells. It also inhibited the migration and invasion of HepG2 cells. Overall, this study suggests that the tubulin polymerization inhibitor incorporating pyrimidine and the 3,4,5-trimethoxyphenyl ring may be a promising candidate for cancer therapy.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Gang Li, Jia-Qiang Wu, Xiaojia Cai, Wen Guan, Zhijun Zeng, Yanghui Ou, Xiaoyun Wu, Jiayu Li, Xiangxiang Fang, Jinling Liu, Yali Zhang, Huamin Wang, Canqiang Yin, Hongliang Yao
Summary: A series of diaryl heterocyclic analogues were synthesized as tubulin polymerization inhibitors. Compound 6y exhibited the highest antiproliferative activity against HCT-116 colon cancer cells and effectively inhibited tubulin polymerization in vitro. It also showed high metabolic stability on human liver microsomes and suppressed tumor growth in a HCT-116 mouse colon model without toxicity. These results suggest that 6y represents a new class of tubulin inhibitors worthy of further investigation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Yuru Liang, Mao Zhang, Pengfei Zhou, Mingming Liu, Jianqi Li, Yang Wang
Summary: A novel class of diaryl substituted azetidin-2-one derivatives were designed, synthesized, and evaluated for antiproliferative activities, with compound B7c showing potent anticancer effects through multiple mechanisms. These results suggest that B7c and its analogues may serve as promising new antitumor agents.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Matteo Lusardi, Chiara Rotolo, Marco Ponassi, Erika Iervasi, Camillo Rosano, Andrea Spallarossa
Summary: A series of highly functionalized pyrazole derivatives were synthesized through a one-pot, versatile, and regioselective procedure. These derivatives exhibited antiproliferative activity against tumor cells, with compounds 21-23 showing inhibition of melanoma and cervical cancer cell growth. Compound 23 was identified as the most active derivative and was predicted to interact with estrogen receptors through docking simulations.
Review
Biochemistry & Molecular Biology
Alessia Catalano, Domenico Iacopetta, Jessica Ceramella, Domenica Scumaci, Federica Giuzio, Carmela Saturnino, Stefano Aquaro, Camillo Rosano, Maria Stefania Sinicropi
Summary: Multidrug resistance, including resistance to anticancer agents and antimicrobial drugs, is a significant concern in public health. The widespread use of antibiotics has led to the emergence of pathogenic bacteria resistant to multiple drugs, and the ongoing COVID-19 pandemic may worsen antimicrobial resistance. Nanodrug delivery systems have shown promise in overcoming resistance.
Article
Immunology
Mariangela Rutigliani, Matteo Bozzo, Andrea Barberis, Marco Greppi, Emanuela Anelli, Luca Castellaro, Alessandro Bonsignore, Antonio Azzinnaro, Silvia Pesce, Marco Filauro, Gian Andrea Rollandi, Patrizio Castagnola, Simona Candiani, Emanuela Marcenaro
Summary: We present a case of inflammatory colitis resulting from SARS-CoV-2 infection, leading to the death of a patient with no additional co-morbidity within three weeks of hospitalization. Our findings suggest that SARS-CoV-2 infection can cause immunological alterations, with increased expression of the inhibitory checkpoint PD-1 and its ligand PD-L1 in inflamed mucosal tissue. The presence of the virus in colon tissue was confirmed, and the altered expression of PD-1/PD-L1 indicates a potential link between SARS-CoV-2 infection and an aberrant autoinflammatory response, contributing to early mortality.
FRONTIERS IN IMMUNOLOGY
(2022)
Review
Chemistry, Multidisciplinary
Alessia Catalano, Domenico Iacopetta, Jessica Ceramella, Annaluisa Mariconda, Camillo Rosano, Domenica Scumaci, Carmela Saturnino, Pasquale Longo, Maria Stefania Sinicropi
Summary: TNBC is a heterogeneous group of malignancies with poor prognosis and aggressive nature, necessitating the development of new treatment strategies. Diagnosis and subtyping are essential for individualized treatment options. Chemotherapy, immune checkpoint inhibitors, targeted therapy, drug repurposing, nutraceuticals, and nanomedicines are among the various approaches being explored for TNBC treatment.
APPLIED SCIENCES-BASEL
(2022)
Article
Oncology
Alberto Izzotti, Enzo Fracchia, Camillo Rosano, Antonio Comite, Liliana Belgioia, Salvatore Sciacca, Zumama Khalid, Matteo Congiu, Cristina Colarossi, Giusi Blanco, Antonio Santoro, Massimo Chiara, Alessandra Pulliero
Summary: Ozonized oils can effectively decrease the risk of cancer relapses by damaging cancer cells and triggering apoptosis. Administering ozonized oil orally can significantly decrease blood antioxidants in cancer patients, resulting in improved survival rate and decreased relapses.
Article
Chemistry, Medicinal
Jessica Ceramella, Annaluisa Mariconda, Marco Sirignano, Domenico Iacopetta, Camillo Rosano, Alessia Catalano, Carmela Saturnino, Maria Stefania Sinicropi, Pasquale Longo
Summary: Metal complexes based on N-heterocyclic carbenes (NHCs) have been extensively studied in the past decade for their wide applications in material sciences and medicinal chemistry. The research focus has been on gold-based complexes for the development of new anticancer compounds. This study reports the design, synthesis, and good anticancer activity of silver and gold complexes with NHC ligands. Some of these complexes showed activity against breast cancer cell lines. New Au-NHC complexes were prepared to improve solubility and biological activity. Some of these compounds demonstrated interesting anticancer activity and inhibited key cellular processes in breast cancer cells.
Article
Biochemistry & Molecular Biology
Maurizio Viale, Giovanni Lentini, Rosaria Gangemi, Patrizio Castagnola, Gualtiero Milani, Silvia Ravera, Nadia Bertola, Antonio Carrieri, Maria Maddalena Cavalluzzi
Summary: This study investigated the potential of the anti-ischemic drug Lube S as an enhancer of anticancer chemotherapy. The results showed that Lube S can effectively improve the antitumor activity of doxorubicin through various mechanisms, including the inhibition of MDR1 gene expression and increased accumulation of doxorubicin in resistant cells.
Article
Oncology
Elia Bari, Francesca Ferrera, Tiziana Altosole, Sara Perteghella, Pierluigi Mauri, Rossana Rossi, Giulia Passignani, Luca Mastracci, Martina Galati, Giuseppina Iliana Astone, Maddalena Mastrogiacomo, Patrizio Castagnola, Daniela Fenoglio, Dario Di Silvestre, Maria Luisa Torre, Gilberto Filaci
Summary: By using silk fibroin nanoparticles as carriers, researchers found that they can promote the uptake of non-tumor antigens by tumor cells, thus generating an immune response against the tumor, which can enhance the effectiveness of immunotherapy.
JOURNAL FOR IMMUNOTHERAPY OF CANCER
(2023)
Article
Oncology
Adriana Agnese Amaro, Rosaria Gangemi, Laura Emionite, Patrizio Castagnola, Gilberto Filaci, Martine. J. J. Jager, Enrica Teresa Tanda, Francesco Spagnolo, Matteo Mascherini, Ulrich Pfeffer, Michela Croce
Summary: It has been found that driver mutations GNAQ and GNA11 activate MAP kinase and YAP/TAZ pathways, and MEK inhibitors do not effectively block UM progression. Combined treatment of trametinib and different drugs targeting YAP/TAZ can overcome resistance. The combined treatment of trametinib and cerivastatin can inhibit the growth of BAP1 mutated and chromosome 3 monosomic uveal melanoma cell lines in vitro and in vivo.
Article
Pharmacology & Pharmacy
Noemi Bognanni, Maurizio Viale, Luana La Piana, Simone Strano, Rosaria Gangemi, Cinzia Lombardo, Maria Teresa Cambria, Graziella Vecchio
Summary: Nanoparticles based on cyclodextrins have been synthesized with a hyaluronic acid backbone under green conditions for the delivery of doxorubicin. The hyaluronan-cyclodextrin conjugates increased the water solubility of doxorubicin and improved its antiproliferative activity in cancer cells. The system based on hyaluronan with a molecular weight of 45 kDa showed the highest effectiveness as a drug carrier and significantly reduced the IC50 value of doxorubicin by about 56%.
Article
Chemistry, Medicinal
Roberta Panebianco, Maurizio Viale, Fabrizio Loiacono, Valeria Lanza, Danilo Milardi, Graziella Vecchio
Summary: Metal terpyridine complexes have attracted significant interest in various fields, and the biological activity of terpyridine and its metal complexes has received considerable attention. To improve their water solubility and target them in cancer cells, we synthesized new terpyridine derivatives of trehalose and glucose. The glucose derivative and its copper(II) and iron(II) complexes exhibited antiproliferative activity, while the trehalose residue reduced the cytotoxicity. Additionally, we evaluated the ability of the parent terpyridine ligands and their copper complexes to inhibit proteasome activity as an antineoplastic mechanism.
Article
Chemistry, Medicinal
Jessica Ceramella, Domenico Iacopetta, Anna Caruso, Annaluisa Mariconda, Anthi Petrou, Athina Geronikaki, Camillo Rosano, Carmela Saturnino, Alessia Catalano, Pasquale Longo, Maria Stefania Sinicropi
Summary: Carbazoles have been extensively studied for their various biological properties, including their potential as antibacterial, antimalarial, antioxidant, antidiabetic, neuroprotective, and anticancer agents. This study focused on the anticancer activity of a series of carbazole derivatives against breast cancer cell lines. Compounds 3 and 4 showed the highest activity against the triple negative MDA-MB-231 cell line without affecting normal cells. Further investigations revealed that these compounds selectively inhibited human topoisomerase I and disrupted the actin system, leading to apoptosis. Therefore, compounds 3 and 4 hold promise for the development of multi-targeted therapy for triple negative breast cancer.
Article
Chemistry, Medicinal
Gabriele Carullo, Sarah Mazzotta, Jessica Ceramella, Domenico Iacopetta, Anna Ramunno, Camillo Rosano, Antonella Brizzi, Giuseppe Campiani, Francesca Aiello, Maria S. Sinicropi
Summary: Topoisomerases play a significant role in cancer development and progression in the human body. In particular, the inhibition of topoI has been found to be an effective strategy in controlling cancer cell proliferation. Pyrrole-based compounds have emerged as promising anticancer agents, especially for breast cancer therapy and topoI inhibition. A small library of 1-(2-aminophenyl)pyrrole-based amides (7a-f) has been developed, showing potential as new anticancer agents through their ability to induce apoptosis in MDA-MB-231 cells. Enzymatic assays and docking simulations revealed the inhibitory activity and potential binding site for these compounds.
ARCHIV DER PHARMAZIE
(2023)
Review
Virology
Alessia Catalano, Domenico Iacopetta, Jessica Ceramella, Michele Pellegrino, Federica Giuzio, Maria Marra, Camillo Rosano, Carmela Saturnino, Maria Stefania Sinicropi, Stefano Aquaro
Summary: Antibacterial resistance is a growing problem in public health, and the COVID-19 pandemic has exacerbated this issue. Antibiotic misuse and improper access have increased during the pandemic, potentially amplifying the future antibacterial resistance pandemic. Infections caused by multidrug-resistant, extensively drug-resistant, difficult-to-treat drug-resistant, carbapenem-resistant, and pan-drug-resistant bacteria continue to rise. This review highlights the current state of antibacterial resistance worldwide, focusing on important pathogens such as Enterobacterales, Acinetobacter baumannii, and Klebsiella pneumoniae and their resistance to common antibiotics.
Article
Chemistry, Medicinal
Maria Stefania Sinicropi, Jessica Ceramella, Patrice Vanelle, Domenico Iacopetta, Camillo Rosano, Omar Khoumeri, Shawkat Abdelmohsen, Wafaa Abdelhady, Hussein El-Kashef
Summary: Cancer is a complex disease and developing new compounds for cancer treatments is urgently needed. In recent years, the design and synthesis of innovative hybrid molecules have gained interest, with promising results in inhibiting cancer cells. The tested hybrid compounds containing trimethoxybenzene, thiazolidinedione and thiazole showed good efficacy against breast cancer cells, with compound 7e being the most effective. Docking simulations indicated that these compounds may target human Topoisomerases I and II, and enzymatic assays confirmed their inhibitory activity. Compound 7e was found to induce apoptosis in MCF-7 cells. These findings support further research in designing and synthesizing analogues for anticancer purposes.
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)
