Article
Biochemistry & Molecular Biology
Juliusz Maksymilian Walczak, Dorota Iwaszkiewicz-Grzes, Michalina Ziomkowska, Magdalena Sliwka-Kaszynska, Mateusz Dasko, Piotr Trzonkowski, Grzegorz Cholewinski
Summary: In this study, 18 new amide derivatives and selected heterocyclic amines were synthesized as potential immunosuppressive agents. The most promising activity was observed in a benzoxazole analogue.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Microbiology
Claire V. Hoffmann, Gilles Nevez, Marie-Christine Moal, Dorothee Quinio, Nathan Le Nan, Nicolas Papon, Jean-Philippe Bouchara, Yannick Le Meur, Solene Le Gal
Summary: MPA may exert selective pressure on specific P. jirovecii strains circulating in SOT recipients.
Article
Oncology
Agnieszka Siebert, Milena Deptula, Miroslawa Cichorek, Anna Ronowska, Grzegorz Cholewinski, Janusz Rachon
Summary: This study investigated the anticancer potential of amino acid and peptide derivatives of Mycophenolic Acid (MPA) against selected cancer cell lines in vitro. The results demonstrated that D and L-threonine derivatives as methyl esters showed the highest activity, possibly due to better cell membrane penetration.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Hong-Wei Jia, Hua-Li Yang, Zhi-Ling Xiong, Ming-Hui Deng, Tong Wang, Yang Liu, Maosheng Cheng
Summary: In this study, 38 acrylamide derivatives were designed and synthesized, and these compounds exhibited effective IMPDH inhibitory activity and played a significant role in cancer intervention.
BIOORGANIC CHEMISTRY
(2022)
Article
Microbiology
Takayuki Hishiki, Takeshi Morita, Daisuke Akazawa, Hirofumi Ohashi, Eun-Sil Park, Michiyo Kataoka, Junki Mifune, Kaho Shionoya, Kana Tsuchimoto, Shinjiro Ojima, Aa Haeruman Azam, Shogo Nakajima, Madoka Kawahara, Tomoki Yoshikawa, Masayuki Shimojima, Kotaro Kiga, Ken Maeda, Tadaki Suzuki, Hideki Ebihara, Yoshimasa Takahashi, Koichi Watashi
Summary: Mpox is a zoonotic disease caused by mpox virus infection, and a global outbreak occurred in May 2022. The smallpox vaccine has been approved for clinical use against mpox, and gemcitabine, trifluridine, and mycophenolic acid have shown inhibitory effects on mpox virus propagation. IMP dehydrogenase has been identified as a potential target for the development of anti-mpox virus agents.
MICROBIOLOGY SPECTRUM
(2023)
Article
Biochemistry & Molecular Biology
Olga Michalak, Marcin Cybulski, Wojciech Szymanowski, Agnieszka Gornowicz, Marek Kubiszewski, Kinga Ostrowska, Piotr Krzeczynski, Krzysztof Bielawski, Bartosz Trzaskowski, Anna Bielawska
Summary: A series of new derivatives of ursolic acid (UA) were designed and synthesized by substituting various amino acids (AAs) or dipeptides (DP) at the C-3 position of the steroid skeleton. These conjugates exhibited cytotoxic activity against hormone-dependent and triple-negative breast cancer cells. Mechanistic studies revealed the activation of apoptotic pathways for some compounds and the induction of autophagy for others. Additionally, the synthesized compounds showed potential as anticancer agents based on their ADME properties and molecular docking to the estrogen receptor.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Physical
Thaissa S. Beck, Mara de Mattos, Carlos R. T. Jortieke, Jean C. B. Vieira, Camila M. Verdi, Roberto C. V. Santos, Michele R. Sagrillo, Aline Rossato, Larissa da Silva Silveira, Clarissa P. Frizzo
Summary: Amino acid-based ionic liquids exhibit specific properties in thermal stability, heat capacity, antimicrobial activity, and cytotoxicity. It was found in the study that amino acid-based anions can reduce the thermal stability of mono and dicationic AAILs, and AAILs with more carbon chains have lower glass transition temperature.
JOURNAL OF MOLECULAR LIQUIDS
(2022)
Article
Biochemistry & Molecular Biology
Ricardo Ballinas-Indili, Maria Ines Nicolas-Vazquez, Joel Martinez, Maria Teresa Ramirez-Apan, Cecilio Alvarez-Toledano, Alfredo Toscano, Maricarmen Hernandez-Rodriguez, Elvia Mera Jimenez, Rene Miranda Ruvalcaba
Summary: A series of novel compounds 3a-p were synthesized to aid in the prevention of multidrug resistance in tumors and reduce toxicity. Compounds 3a and 3b exhibited strong antineoplastic activity and could be considered as suitable drug candidates.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Oncology
Mariana N. Costa, Roberto N. Silva
Summary: Cancer cells have higher proliferation rates and increased demand for amino acids compared to normal cells, which has been exploited for the development of anticancer drugs like L-asparaginase. Additionally, L-lysine alpha-oxidase, an enzyme of L-amino acid oxidase family, has been studied as a potential antineoplastic agent.
SEMINARS IN CANCER BIOLOGY
(2022)
Article
Oncology
Samir M. Awad, Mosaad S. Mohamed, Marwa Abd El-Fattah Khodair, Rania H. Abd El-Hameed
Summary: The study focused on synthesizing new benzo[h]chromene derivatives and testing their anti-cancer activities. Compound 1c showed the highest anti-cancer activity among all tested compounds and may require further investigation for potential development as a new anti-cancer agent.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Lidia A. Baltina, Hsueh-Chou Lai, Ya-Chi Liu, Su-Hua Huang, Mann-Jen Hour, Lia A. Baltina, Tagir R. Nugumanov, Sophia S. Borisevich, Leonard M. Khalilov, Svetlana F. Petrova, Sergey L. Khursan, Cheng-Wen Lin
Summary: This study focused on synthesizing a series of nitrogen and sulfur-containing derivatives of Glycyrrhetinic acid as potential inhibitors of Zika virus. Among the compounds tested, four active compounds were identified as effective in inhibiting Zika virus replication, with one compound showing the highest activity. Time-of-addition assays indicated the importance of specific functional groups in inhibiting different stages of the viral life cycle, and molecular docking analysis revealed potential interactions with viral protease enzymes. These findings suggest promising leads for developing new antiviral agents against Zika virus infection.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Gulnara Giniyatullina, Anastasiya Petrova, Akhat G. Mustafin, Zulfia R. Zileeva, Ulyana Sh Kuzmina, Yulia V. Vakhitova, Oxana B. Kazakova
Summary: A series of betulonic acid N-methylpiperazinyl amide derivatives were synthesized and evaluated for their cytotoxic activity against cancer cell lines, with some compounds showing higher activity than the standard drug doxorubicin. Compound 11 was found to promote apoptosis induction, while compound 14 exhibited cytostatic and cytotoxic activity dependent on the cell line. Compounds 11 and 14 are promising for future antitumor drug development.
Article
Agricultural Engineering
Q. H. Zhang, N. Xua
Summary: During oil and gas exploitation, the corrosion of carbon steel pipes leads to significant economic loss, casualties, environmental pollution, and resource waste. Developing highly efficient and stable corrosion inhibitors is crucial for protecting carbon steel in this industry. L-cysteine is commonly found in plants but has low inhibitive efficiency, so chemical modification is used to enhance its effectiveness. In this study, two synthetic amino acid derivatives, namely PTCA and TTCA, were investigated as corrosion inhibitors for carbon steel in a CO2-containing environment. Electrochemical experiments, surface techniques, and theoretical calculations were conducted to evaluate the anti-corrosion property and inhibitive mechanism of these derivatives. The results showed that PTCA and TTCA exhibited high corrosion inhibition efficiencies at a concentration of 0.8 mM: PTCA (99.1%) and TTCA (99.3%). Theoretical calculations revealed that PTCA and TTCA adsorb onto the steel surface by forming Fe-O bonds. TTCA exhibited stronger adsorption and a more negative adsorption energy, leading to its superior inhibitive performance compared to PTCA.
INDUSTRIAL CROPS AND PRODUCTS
(2023)
Article
Chemistry, Medicinal
Alaaeldin M. F. Galal, Hanaa S. Mohamed, Marwa M. Abdel-Aziz, Atef G. Hanna
Summary: This study focused on the development and synthesis of sulfonyl-alpha-l-amino acids coupled with the anisamide scaffold for their anti-Helicobacter pylori and IMPDH inhibitory activities. Among the synthesized derivatives, compounds 6 and 10 exhibited promising inhibitory activities against the HpIMPDH enzyme, with IC50 values of 2.42 and 2.56 µM, respectively. Additionally, the compounds showed less activity and higher safety against hIMPDH2 compared to the reference drugs, indicating a potential selectivity towards HpIMPDH.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Organic
Takayuki Kodama, Ikuo Sasaki, Hideyuki Sugimura
Summary: A highly regioselective method was developed for the preparation of pyridazine derivatives via the aza-Diels-Alder reaction of 1,2,3-triazines with 1-propynylamines under neutral conditions. This methodology allowed direct access to a wide range of 6-aryl-pyridazin-3-amines in high yields with good functional group compatibility. Key features of this strategy included a broad substrate scope and simple, metal-free, and neutral reaction conditions.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Rheumatology
Maria Skrzypkowska, Mariusz Stasiak, Justyna Sakowska, Joanna Chmiel, Agata Maciejewska, Adam Bucinski, Bartosz Slominski, Piotr Trzonkowski, Piotr Luczkiewicz
Summary: The study evaluated the concentrations of specific cytokines and chemokines in patients with rheumatoid arthritis and osteoarthritis. The results showed significant differences in the concentrations of various cytokines and chemokines in the blood and synovial fluid of rheumatoid arthritis patients, even in those with low disease activity. These abnormalities may serve as indicators of disease progression.
RHEUMATOLOGY INTERNATIONAL
(2022)
Article
Multidisciplinary Sciences
Karolina Piekarska, Zuzanna Urban-Wojciuk, Malgorzta Kurkowiak, Iwona Pelikant-Malecka, Adriana Schumacher, Justyna Sakowska, Jan Henryk Spodnik, Lukasz Arcimowicz, Hanna Zielinska, Boguslaw Tymoniuk, Alicja Renkielska, Janusz Siebert, Ewa Slominska, Piotr Trzonkowski, Ted Hupp, Natalia Maria Marek-Trzonkowska
Summary: Transfer of mitochondria from mesenchymal stem cells to allogeneic Treg cells enhances the immunosuppressive functions of Treg cells, providing potential for the development of cell-based immunotherapies.
NATURE COMMUNICATIONS
(2022)
Article
Endocrinology & Metabolism
Maciej Zielinski, Magdalena Zalinska, Dorota Iwaszkiewicz-Grzes, Mateusz Gliwinski, Matylda Hennig, Anna Jazwinska-Curyllo, Halla Kaminska, Justyna Sakowska, Anna Woloszyn-Durkiewicz, Radoslaw Owczuk, Wojciech Mlynarski, Przemyslawa Jarosz-Chobot, Artur Bossowski, Agnieszka Szadkowska, Janusz Siebert, Malgorzata Mysliwiec, Natalia Marek-Trzonkowska, Piotr Trzonkowski
Summary: This study explored the efficacy and safety of combined treatment with Tregs and rituximab in pediatric patients with T1DM. Results showed that the combined therapy was consistently superior to monotherapy in terms of C-peptide levels and the maintenance of remission, with a higher rate of adverse events.
DIABETES OBESITY & METABOLISM
(2022)
Article
Immunology
Hanna Zielinska, Maciej Zielinski, Anna Debska-Zielkowska, Anna Dukat-Mazurek, Grazyna Moszkowska, Dorota Lewandowska, Alicja Debska-Slizien, Piotr Trzonkowski
Summary: This study found that simultaneous testing of C1q and SAB can provide in-depth analysis of alloantibodies before transplantation. There is a strong correlation between SAB and C1q for most HLA loci, except HLA-DP. Additionally, an unusual laboratory phenotype was identified, with positive C1q results but no corresponding SAB specificity.
TRANSPLANTATION PROCEEDINGS
(2022)
Review
Immunology
Justyna Sakowska, Lukasz Arcimowicz, Martyna Jankowiak, Ines Papak, Aleksandra Markiewicz, Katarzyna Dziubek, Malgorzata Kurkowiak, Sachin Kote, Karolina Kazmierczak-Siedlecka, Karol Polom, Natalia Marek-Trzonkowska, Piotr Trzonkowski
Summary: Autoimmune diseases and cancer have traditionally been seen as separate fields of research, but recent studies have shown that studying autoimmune diseases can be beneficial in the development of anti-cancer drugs. This review discusses the role of regulatory cell populations, effector molecules, genetic predisposition, and environmental factors in the loss of self-tolerance in autoimmunity and tolerance induction in cancer.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Immunology
Katarzyna Stefanska, Martyna Tomaszewicz, Joanna Debska-Zielkowska, Dorota Zamkowska, Karolina Piekarska, Justyna Sakowska, Maciej Studzinski, Boguslaw Tymoniuk, Przemyslaw Adamski, Joanna Jassem-Bobowicz, Piotr Wydra, Katarzyna Leszczynska, Renata Swiatkowska-Stodulska, Sebastian Kwiatkowski, Krzysztof Preis, Piotr Trzonkowski, Natalia Marek-Trzonkowska, Maciej Zielinski
Summary: The activity of natural killer (NK) cells is important for the tolerance of the fetus during pregnancy, and complications such as hypertensive disorders may be associated with this immune compartment. This study found that patients with hypertensive disorders had a higher number of ligands related to inhibitory receptors within the KIRs receptors, while the healthy group maintained balance through various receptors.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Immunology
Magdalena Piotrowska, Maciej Zielinski, Leszek Tylicki, Bogdan Biedunkiewicz, Alicja Kubanek, Zuzanna Slizien, Karolina Polewska, Piotr Tylicki, Marta Muchlado, Justyna Sakowska, Marcin Renke, Adam Sudol, Malgorzata Dabrowska, Monika Lichodziejewska-Niemierko, Tomasz Smiatacz, Alicja Debska-Slizien, Piotr Trzonkowski
Summary: Patients with end-stage renal disease and kidney transplant recipients have a weakened immune response to the COVID-19 vaccine, and two doses of the Pfizer vaccine are ineffective. Further research and clinical guidelines are needed.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Juliusz Maksymilian Walczak, Dorota Iwaszkiewicz-Grzes, Michalina Ziomkowska, Magdalena Sliwka-Kaszynska, Mateusz Dasko, Piotr Trzonkowski, Grzegorz Cholewinski
Summary: In this study, 18 new amide derivatives and selected heterocyclic amines were synthesized as potential immunosuppressive agents. The most promising activity was observed in a benzoxazole analogue.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Geriatrics & Gerontology
Michal Cezary Czarnogorski, Justyna Sakowska, Mateusz Maziewski, Maciej Zielinski, Agnieszka Piekarska, Igor Obuchowski, Mikolaj Mlynski, Magdalena Dutka, Alicja Sadowska-Klasa, Ewa Zarzycka, Maria Bieniaszewska, Piotr Trzonkowski, Jacek M. Witkowski, Andrzej Hellmann, Katarzyna Ruckemann-Dziurdzinska, Jan M. Zaucha
Summary: This study compared the ageing characteristics between recipients and donors of allogeneic hematopoietic cell transplant (allo-HCT) and found that the rate of ageing in long-term allo-HCT recipients is not accelerated, except for some molecular features in the recipients' lymphocytes (mainly CD8(+)) that are characteristic of physiological ageing. However, a history of lower infection numbers in HCT recipients is associated with an increased percentage of NK cells.
Review
Biochemistry & Molecular Biology
Dorota Garwolinska, Agata Kot-Wasik, Weronika Hewelt-Belka
Summary: Metabolomics is widely used in various fields such as clinical diagnostics, disease investigation, therapy prediction, treatment efficiency monitoring, drug discovery, and sample composition analysis. The study design, including careful selection of conditions and consideration of pre-analytical variability, is crucial for robust and reliable results. This study provides key information on pre-analytical variables affecting metabolomics studies of biological fluids, serving as a practical review and identifying factors that introduce artificial data variation.
Article
Biochemistry & Molecular Biology
Marlena Typiak, Piotr Trzonkowski, Monika Skotarczak, Anna Dubaniewicz
Summary: Sarcoidosis (SA) is a granulomatous disorder that affects the lungs, resembling tuberculosis (TB) in clinical characteristics but with different treatment approaches. By studying the phagocytic activity of monocytes in the blood of SA and TB patients using flow cytometry, we found higher phagocytic activity in SA patients and an increased frequency of Fc?RIII (CD16) receptors but a decreased frequency of CR1 (CD35) receptors compared to TB patients. This study provides insights into the pathomechanisms and differential diagnosis of SA and TB.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Immunology
Martyna Tomaszewicz, Anna Ronowska, Maciej Zielinski, Agnieszka Jankowska-Kulawy, Piotr Trzonkowski
Summary: CD4(+)CD25(high)FoxP3(+) regulatory T cells (Tregs) are a subset of lymphocytes that can suppress the immune system through direct interactions with other cells and the secretion of suppressive compounds. Modulating the metabolic program of Tregs may improve or weaken their stability and function, making it a crucial tool in managing infections and autoimmunity.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Immunology
Justyna Sakowska, Paulina Glasner, Anna Dukat-Mazurek, Anna Rydz, Maciej Zielinski, Irena Pellowska, Wojciech Biernat, Leopold Glasner, Katarzyna Michalska-Ma Lecka, Piotr Trzonkowski
Summary: The risk of graft failure increases significantly for repeated corneal transplantations due to alloimmunization and the development of memory T and B cells. The rejection is mainly mediated by local T cells, particularly the accumulation of effector memory CD4+ and CD8+ T cells. Additionally, the presence of CD4+ and CD8+ Tregs expressing Foxp3 and Helios may be insufficient for graft acceptance.
TRANSPLANT IMMUNOLOGY
(2023)
Meeting Abstract
Immunology
Justyna Sakowska, Paulina Glasner, Anna Rydz, Anna Dukat-Mazurek, Maciej Zielinski, Piotr Trzonkowski, Leopold Glasner
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)
