Article
Biochemistry & Molecular Biology
Maria Schroder, Maria Petrova, Zlatina Vlahova, Georgi M. Dobrikov, Ivaylo Slavchev, Evdokia Pasheva, Iva Ugrinova
Summary: The successful design of antitumour drugs often involves combining different biologically active subunits to affect multiple cellular regulatory pathways, leading to higher efficacy. In this study, two ferrocene derivatives, DK-164 and CC-78, were tested for their cytotoxic potential on lung cancer cell lines. DK-164 showed selective cytotoxicity towards cancer cells, while CC-78 exhibited higher cytotoxicity without selectivity. The different cellular mechanisms induced by these compounds in lung cancer cells provide insights into the specific functions of functional groups in ferrocene compounds and can guide the design of new antitumour drugs.
Article
Biochemistry & Molecular Biology
Jeyce Kelle Ferreira de Andrade, Alexandre Jose da Silva Goes, Vanessa Xavier Barbosa, Mariza Severina de Lima Silva, Mariana Aragao Matos Donato, Christina Alves Peixoto, Gardenia Carmen Gadelha Militao, Teresinha Goncalves da Silva
Summary: Thiosemicarbazones derived from beta-lapachone showed potent cytotoxic effects on leukemia cells, with BV3 being the most selective compound, exhibiting high toxicity to tumor cells and low toxicity to normal cells. These compounds have the potential to be promising candidates for anticancer drugs.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Review
Biochemistry & Molecular Biology
Sandra Lucia Teniente, Adriana Carolina Flores-Gallegos, Sandra Cecilia Esparza-Gonzalez, Lizeth Guadalupe Campos-Muzquiz, Sendar Daniel Nery-Flores, Raul Rodriguez-Herrera
Summary: Polyphenols are bioactive phytochemicals with various beneficial activities, including antioxidant, anti-inflammatory, immunomodulatory, and antiviral effects. Extracts from natural sources, such as pomegranate peel extract (PPE), containing polyphenols have shown potential in cancer prevention and treatment. The review summarizes recent scientific reports on the anticancer activity of polyphenols found in PPE, including their mechanisms of action in cervical cancer models.
Article
Biochemistry & Molecular Biology
Shilpa Raina, Vikas Sharma, Zahid Nabi Sheikh, Navneet Kour, Shashank K. Singh, Ali Zari, Talal A. Zari, Hesham F. Alharby, Khalid Rehman Hakeem
Summary: This study aimed to evaluate the in vitro anticancer potential of different components (bark, leaves, pulp, and seeds) of Cordia dichotoma. The results showed that the bark of the plant exhibited in vitro cytotoxicity against A-549 human lung cancer cells, induced chromatin condensation, confirmed cell death through ROS generation, and significantly reduced colony formation in the lung cancer cell line. Additionally, HPLC and GCMS analyses identified several bioactive molecules, including some compounds reported for the first time from the bark.
Article
Pharmacology & Pharmacy
Sahar M. AlMotwaa, Waad A. Al-Otaibi
Summary: The synthesized nanoemulsion containing Pulicaria crispa essential oil and gemcitabine showed a synergistic effect in inhibiting cancer cell growth and inducing apoptosis. This formulation may reduce the dose of gemcitabine and eliminate its associated side effects.
Article
Biochemistry & Molecular Biology
Yong-Feng Guan, Xiu-Juan Liu, Xin-Ying Yuan, Wen-Bo Liu, Yin-Ru Li, Guang-Xi Yu, Xin-Yi Tian, Yan-Bing Zhang, Jian Song, Wen Li, Sai-Yang Zhang
Summary: In this study, quinoline-chalcone derivatives were designed and synthesized by linking chalcone fragment to the quinoline scaffold, resulting in compound 12e showing promising inhibitory activity against multiple cancer cell lines. Mechanism studies indicated that compound 12e may exert its anticancer effects through various pathways.
Article
Biochemistry & Molecular Biology
Farid Qoorchi Moheb Seraj, Niloofar Heravi-Faz, Arash Soltani, Seyed Sajad Ahmadi, Fatemeh Shahbeiki, Amir Talebpour, Amir R. Afshari, Gordon A. Ferns, Afsane Bahrami
Summary: Thymol exhibited potential cytotoxic activities on U-87 cells, possibly through increased apoptosis, generation of reactive oxygen species, and cell cycle arrest. Combination therapy of thymol and temozolomide synergistically enhanced cytotoxic effects.
MOLECULAR BIOLOGY REPORTS
(2022)
Article
Biochemistry & Molecular Biology
Mohammed Al-Hayali, Aimie Garces, Michael Stocks, Hilary Collins, Tracey D. Bradshaw
Summary: Thymoquinone (TQ) has demonstrated anti-cancer activity, possibly through the generation of ROS and induction of aneuploidy. Early depletion of GSH can substantially enhance TQ's anti-cancer activity. Structural modification of TQ by benzylamine substitution did not improve its anti-cancer potency.
Article
Biochemistry & Molecular Biology
Irina Tolmacheva, Yulia Beloglazova, Mikhail Nazarov, Olga Gagarskikh, Victoria Grishko
Summary: Multidrug resistance (MDR) is a common occurrence in cancer treatment, where cancer cells become resistant to chemotherapy drugs due to overexpression of ATP-binding cassette efflux transporters, including P-glycoprotein (P-gp). A new semi-synthetic derivative, MK, was found to have the highest cytotoxicity against cancer cells, but it was not identified as a P-gp inhibitor or substrate. Further studies suggest that the cytotoxic effect of MK on cancer cells may be induced through the ROS-mediated mitochondrial pathway.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Plant Sciences
Hyesu Jeon, Diem Thi Ngoc Huynh, Naehwan Baek, Thuy Le Lam Nguyen, Kyung-Sun Heo
Summary: The study showed that G-Rg2 has significant anticancer effects on MCF-7 breast cancer cells by increasing ROS-AMPK signaling pathway and inhibiting ERK1/2 and Akt activation-mediated cell proliferation and cell cycle progression.
Article
Chemistry, Inorganic & Nuclear
Archana Ranjan, Deepu Sharma, Avinash K. Srivastava, Ajit Varma, Magani S. K. Jayadev, Raj K. Joshi
Summary: Ferrocene-based compounds have gained importance in cancer treatment due to their lower toxicity and cost-effective synthesis. In this study, thianes containing ferrocene were synthesized and their synergistic effect with thiol was observed in suppressing tumor growth. These compounds showed significant anticancer effects by inducing apoptosis and inhibiting cell migration. The ferrocene-based compounds have the potential to serve as a platform for the development of new anticancer agents, replacing rare metal compounds.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Jin-yi Liu, Wei-qi Fu, Xiang-jin Zheng, Wan Li, Li-wen Ren, Jin-hua Wang, Cui Yang, Guan-hua Du
Summary: Avasimibe demonstrated potent anticancer effects on human glioblastoma cells by inhibiting proliferation, inducing apoptosis, and regulating multiple signaling pathways. The drug showed promising potential as a chemotherapy treatment for glioblastoma.
ACTA PHARMACOLOGICA SINICA
(2021)
Article
Medicine, Research & Experimental
Shabeeba M. Ashraf, Susobhan Mahanty, Krishnan Rathinasamy
Summary: Securinine effectively inhibits the proliferation of cervical, breast, and lung cancer cells while inducing minimal toxicity in non-malignant HEK cells. It disrupts microtubule organization in both interphase and mitotic phases, as well as inhibits tubulin assembly. Additionally, securinine induces a mitochondrial-dependent ROS response in cancer cells and leads to apoptosis through a p53-dependent pathway in MCF-7 cells.
Article
Biochemistry & Molecular Biology
Alberto M. Parra-Perez, Amalia Perez-Jimenez, Isabel Gris-Cardenas, Gloria C. Bonel-Perez, Luis M. Carrasco-Diaz, Khalida Mokhtari, Leticia Garcia-Salguero, Jose A. Lupianez, Eva E. Rufino-Palomares
Summary: Hydroxytyrosol (HT), the main polyphenol in olive oil, has been found to possess antioxidant, anti-inflammatory, antimicrobial, cardioprotective, and anticancer properties. This study evaluated the anticancer potential of HT in acute human leukemia cells and the anti-inflammatory potential in murine macrophages. The results showed that HT exhibited antiproliferative effects and induced cell cycle arrest in leukemia cells. It also acted as an anti-inflammatory agent by reducing inflammation markers in stimulated macrophages. These findings suggest that HT could be a natural drug for the treatment of liquid cancers such as leukemias, myelomas, and lymphomas.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Inorganic & Nuclear
Joanna Skiba, Aleksandra Kowalczyk, Damian Trzybinski, Krzysztof Wozniak, Valerije Vrcek, Magdalena Gapinska, Konrad Kowalski
Summary: This paper reports a Yb(OTf)(3)-mediated etherification reaction to obtain R,R and S,R isomers of ferrocenyl glycol nucleic acid (Fc-GNA) nucleosides from their stereo-defined (S,R) precursor. The mechanism of the reaction is explained by density functional theory calculations, and the obtained compounds show reversible oxidation of the ferrocenyl portion. Anticancer activity studies reveal that the (S,R) nucleoside exhibits the highest activity against cancer cells HeLa and Ishikawa, inducing apoptosis in HeLa cells at a concentration of IC50=66.0 μM after 72 hours of treatment.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ewelina Namiecinska, Magdalena Grazul, Beata Sadowska, Marzena Wieckowska-Szakiel, Pawel Hikisz, Beata Pasternak, Elzbieta Budzisz
Summary: This paper evaluates the antimicrobial potential of arene-ruthenium(II) complexes and their salts as alternatives to antibiotics. The complexes were found to have synergistic effects with certain antibiotics against bacteria, and their bactericidal effect was associated with cell lysis and DNA cutting.
Article
Materials Science, Multidisciplinary
Marsel Z. Shafikov, Alfiya F. Suleymanova, Roger J. Kutta, Alexander Gorski, Aleksandra Kowalczyk, Magdalena Gapinska, Konrad Kowalski, Rafal Czerwieniec
Summary: In this study, the photophysical properties of transition metal complexes were fine-tuned by targeted design of a N<^>C-C<^>N type ligand. The mononuclear complex Pt-1 exhibited red phosphorescence, while the dinuclear complex Pt-2 showed near infrared phosphorescence. The phosphorescence of the complexes was quenched in the presence of molecular oxygen, generating singlet oxygen molecules. Pt-1 had a unique dual emission ability, which was beneficial for cellular imaging.
JOURNAL OF MATERIALS CHEMISTRY C
(2022)
Article
Materials Science, Multidisciplinary
Marsel Z. Shafikov, Craig Hodgson, Aleksander Gorski, Aleksandra Kowalczyk, Magdalena Gapinska, Konrad Kowalski, Rafal Czerwieniec, Valery N. Kozhevnikov
Summary: Annulation of the additional aromatic pi-system to the ligand is an effective method of influencing the luminescence of metal complexes. The new dinuclear complex di-Ir shows drastically improved efficiency of phosphorescence compared to the previously reported complex Ir-2. The two complexes, mono-Ir and di-Ir, are promising materials for optical oxygen sensing and applications associated with singlet oxygen generation.
JOURNAL OF MATERIALS CHEMISTRY C
(2022)
Article
Biochemistry & Molecular Biology
Aleksandra Kowalczyk, Michal Piotrowicz, Magdalena Gapinska, Damian Trzybinski, Krzysztof Wozniak, Taryn M. Golding, Tameryn Stringer, Gregory S. Smith, Rafal Czerwieniec, Konrad Kowalski
Summary: The knowledge regarding the chemistry and biological activity of glycol nucleic acid (GNA) components is limited. The synthesized phenanthrenyl GNA nucleoside and gemcitabine exhibit similar mechanisms of anticancer activity in HeLa cancer cells. Additionally, these compounds also show some activity in antiplasmodial assays.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Joanna Skiba, Aleksandra Kowalczyk, Aleksander Gorski, Natalia Dutkiewicz, Magdalena Gapinska, Jozef Strozek, Krzysztof Wozniak, Damian Trzybinski, Konrad Kowalski
Summary: The synthesis of luminescent dinucleoside phosphate analogs with a [Re-2(mu-Cl)(2)(CO)(6)(mu-pyridazine)] click linker as a replacement for the natural phosphate group is reported. These compounds exhibited orange emission and showed no toxicity to human cancer cells in vitro. Additionally, they showed moderate antibacterial activity against Staphylococcus aureus and Escherichia coli strains.
DALTON TRANSACTIONS
(2023)
Article
Biochemistry & Molecular Biology
Damian Jacenik, Pawel Hikisz, Ellen J. Beswick, Jakub Fichna
Summary: Among the various adhesion G protein-coupled receptors, ADGRF5 stands out with its unique domains in the N-terminal tail that play a critical role in cell-cell and cell-matrix interactions, as well as cell adhesion. Although the biology of ADGRF5 is still not fully understood, accumulating evidence suggests its fundamental importance in both health and disease. Recent studies have highlighted its potential diagnostic value in osteoporosis and cancers, and ongoing research indicates its relevance to other diseases as well. This article provides a comprehensive overview of the current understanding of ADGRF5 in human disease physiology and pathophysiology, emphasizing its potential as a novel therapeutic target in various areas.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
(2023)
Review
Chemistry, Inorganic & Nuclear
Konrad Kowalski
Summary: Cancer is a leading cause of death worldwide. This review emphasizes the significance of metal-catalyzed azide-alkyne cycloaddition reactions in synthesizing ferrocenyl-x-1,2,3-triazolyl-R compounds with anticancer activity. The review discusses over 160 ferrocenyl-triazoles and their classification into four categories based on their chemical properties. The study demonstrates that copper-catalyzed azide-alkyne cycloaddition reactions are particularly important in yielding the highest number of ferrocenyl-x-1,2,3-triazolyl compounds with anticancer activity. Oxidative stress and reactive oxygen species generation are identified as common mechanisms through which the ferrocenyl moiety contributes to the anticancer activity of 1,2,3-triazolyl derivatives. The review contains 23 figures, 24 schemes, and 208 references.(c) 2022 Elsevier B.V. All rights reserved.
COORDINATION CHEMISTRY REVIEWS
(2023)
Article
Chemistry, Inorganic & Nuclear
Sara La Manna, Valentina Roviello, Fabiana Napolitano, Anna Maria Malfitano, Vittoria Monaco, Antonello Merlino, Maria Monti, Konrad Kowalski, Lukasz Szczupak, Daniela Marasco
Summary: Three photoactivable metal-CORMs have been found to modulate the self-aggregation mechanism of the peptide covering the second helix of the C-terminal domain of nucleophosmin 1 in different ways, with two acting as aggregating agents and one as an anti-aggregating agent. This highlights the importance of ligand systems in the development of metal-based drugs with potential application as antiamyloidogenic agents.
INORGANIC CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Pawel Hikisz, Damian Jacenik
Summary: Acrolein, a highly reactive alpha,beta-unsaturated aldehyde, is involved in the pathogenesis of many diseases, including neurodegenerative diseases, cardiovascular and respiratory diseases, diabetes mellitus, and various types of cancers. It is mainly derived from environmental pollution, tobacco smoke, and our daily diet. The intake of acrolein through diet is a major public health concern. This review focuses on the molecular mechanisms of acrolein in digestive system-related diseases such as diabetes, alcoholic liver disease, and intestinal cancer.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Pawel Hikisz, Ewelina Namiecinska, Piotr Paneth, Elzbieta Budzisz
Summary: This study aims to investigate the biological aspects and anticancer activity of arene-ruthenium(II) complexes. Additional testing was conducted to better understand the potential mechanism of antitumor activity, including membrane permeability studies, ROS/RNS assays, and DNA analysis. Lipophilicity and molecular docking studies were also conducted. The presented data may have practical implications in cancer treatment.
Editorial Material
Pharmacology & Pharmacy
Chiara Riganti, Konrad Kowalski, Joanna Kopecka
FRONTIERS IN PHARMACOLOGY
(2023)
Review
Cell Biology
Pawel Hikisz, Damian Jacenik
Summary: Acrolein, a highly reactive unsaturated aldehyde, is a widespread environmental pollutant that poses serious threats to human health and life. It is implicated in the development of various diseases, including multiple sclerosis, neurodegenerative diseases, cardiovascular and respiratory diseases, diabetes mellitus, and even cancer. Both traditional tobacco smokers and e-cigarette users are at high risk of exposure to acrolein, which is considered one of the most toxic and harmful components of cigarette smoke. Chronic exposure to acrolein through cigarette smoke is linked to the development of asthma, acute lung injury, chronic obstructive pulmonary disease (COPD), and respiratory cancers.
Article
Biochemistry & Molecular Biology
Lukasz Gwozdzinski, Joanna Bernasinska-Slomczewska, Pawel Hikisz, Anna Wiktorowska-Owczarek, Edward Kowalczyk, Anna Pieniazek
Summary: In this study, the properties of human varicose vein endothelial cells (HVVEC) and human umbilical vein endothelial cells (HUVEC) were compared. Three bioactive compounds, diosmin, escin, and bromelain, were tested on the cells. The drugs showed different effects on reactive oxygen species and nitric oxide generation in the cells. The study revealed a potential mechanism of action for VV therapy drugs on HVVEC cells.
Article
Biochemistry & Molecular Biology
Lucie Paulus, Manuel Gallardo-Villagran, Claire Carrion, Catherine Ouk, Frederique Martin, Bruno Therrien, David Yannick Leger, Bertrand Liagre
Summary: Prostate cancer is a major health issue and the second most common cancer in men. Photodynamic therapy (PDT) is a non-invasive method that uses photosensitizers and light to induce cell death with minimal side effects. However, some photosensitizers used in PDT have low solubility in biological media, requiring functionalization or vectorization for effective internalization. This study used arene-ruthenium cages to deliver photosensitizers to prostate cancer cells. The results showed that most of the compounds induced cytotoxic effects on prostate cancer cells, with confirmed internalization in the cytoplasm. The presence of metals in the photosensitizers decreased the effectiveness of PDT, and in some cases, completely eliminated its effect.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Konrad Kowalski
Summary: Xeno nucleic acids (XNA) are an important class of hypermodified nucleic acids with potential applications in bioorganic chemistry and synthetic biology. Glycol nucleic acid (GNA) is the simplest known XNA, constructed from a three-carbon 1,2-propanediol backbone. This review focuses on the synthetic methods and chemical transformations of GNA nucleosides, as well as highlighting their properties and biological activity.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
