Article
Chemistry, Physical
Andrii Pyrih, Mariusz Jaskolski, Andrzej K. Gzella, Roman Lesyk
Summary: A synthetic method for 4-arylamino-5-(2-pyrazoline-1-yl)-methylidene-1,3-thiazoline-2-ones with good yields was described. The prepared compounds were characterized by IR, NMR, and X-ray crystal structure analysis, and their anticancer activity was tested.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Kamila Buzun, Anna Kryshchyshyn-Dylevych, Julia Senkiv, Olexandra Roman, Andrzej Gzella, Krzysztof Bielawski, Anna Bielawska, Roman Lesyk
Summary: A series of novel 5-[(Z,2Z)-2-chloro-3-(4-nitrophenyl)-2-propenylidene]-thiazolidinones were synthesized, with compound 2h showing the highest level of antimitotic activity against various cancer cell lines. Hit compounds were found to have low toxicity towards normal human blood lymphocytes and a fairly wide therapeutic range. The significance of specific substituents in the 4-thiazolidinone derivatives for anticancer cytotoxicity levels was established.
Article
Biochemistry & Molecular Biology
Agnieszka Gornowicz, Roman Lesyk, Robert Czarnomysy, Serhii Holota, Yulia Shepeta, Bozena Poplawska, Magdalena Podolak, Wojciech Szymanowski, Krzysztof Bielawski, Anna Bielawska
Summary: Combining chemotherapy with immunotherapy is a promising strategy in treating gastric cancer with confirmed HER2 expression. Novel 4-thiazolidinone derivatives and anti-HER2 antibodies show potential in increasing the sensitivity of gastric cancer cells to treatment. The molecular mechanism of action involves apoptosis induction and decreased inflammation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Physical
Andrii Pyrih, Andrzej Lapinski, Sylwia Zieba, Adam Mizera, Roman Lesyk, Andrzej K. Gzella, Mariusz Jaskolski
Summary: In this article, we reported the recent findings of our systematic studies on the effects of phenyl-ring substituents on proton tautomerism and stereoisomerism in 4-phenylamino-1,3-thiazol-2(5H)-one derivatives. Through synthesis, spectral analysis, and crystal studies, we found that these compounds exist solely in the amino tautomeric form and exhibit a specific arrangement.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
Article
Chemistry, Organic
Mohamed R. Elmorsy, Mariam Eltoukhi, Ahmed A. Fadda, Ehab Abdel-Latif, Miral A. Abdelmoaz
Summary: This research focuses on the synthesis of carbazole-thiazolidinone derivatives and their cytotoxicity against three different cell lines. The compounds 3b and 5c show the most effective antitumor activity against the tested cell lines.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Chemistry, Organic
Adisak Thanetchaiyakup, Suparerk Borwornpinyo, Hassayaporn Rattanarat, Phongthon Kanjanasirirat, Kedchin Jearawuttanakul, Sawinee Seemakhan, Nutthawat Chuanopparat, Paiboon Ngernmeesri
Summary: A new synthesis method has been developed for substituted indolo[1,2-a]quinolines with high yields, which exhibit activity against breast cancer and colorectal cancer cells.
TETRAHEDRON LETTERS
(2021)
Article
Chemistry, Physical
Irfan Sahin, Fatma Betul Ozgeris, Muhammet Kose, Ebubekir Bakan, Ferhan Tumer
Summary: This study synthesized six 1,2,3-triazole derivatives and investigated their antioxidant and anticancer activities. The results showed that some of the compounds exhibited significant anticancer activity.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Inorganic & Nuclear
Samahe Sadjadi, Sara Tarighi, Ali Afshar Ebrahimi
Summary: Two novel composites, composed of MIL-101 and ZSM-5 zeolites with different SiO2/Al2O3 ratios, were synthesized via surface functionalization of ZSM-5 zeolites and subsequent hydrothermal treatment with MIL-101 precursors. These composites demonstrated higher catalytic activity than their individual components in Knoevenagel condensation reaction, indicating the synergism between ZSM-5 and MIL-101. Additionally, the composites showed broad substrate scope, facile catalyst recovery, and high recyclability.
INORGANIC CHEMISTRY COMMUNICATIONS
(2023)
Article
Thermodynamics
Sandra Ramos-Inza, Eneko Almagro, Maria Font, Ignacio Encio, Daniel Plano, Carmen Sanmartin, Rafael Sirera, Elena Lizarraga
Summary: In this study, the stability, thermal characterization, and polymorphic forms of thirty new nonsteroidal anti-inflammatory drug derivatives containing selenium were analyzed. The compounds exhibited thermal stability and no significant differences were found among polymorphic forms, indicating their suitability for further drug development.
JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY
(2023)
Article
Chemistry, Organic
Pravin S. Kulkarni, Sanjay N. Karale, Amol U. Khandebharad, Brijmohan R. Agrawal, Swapnil R. Sarda
Summary: A series of newer derivatives containing 2,4-thiazolidinedione and 2-aryl-4-thiazolidinone moieties were synthesized and tested for their antimicrobial and cytotoxic activities. Some compounds exhibited equipotent antibacterial activity against different strains without cytotoxicity.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Article
Chemistry, Physical
Diana Becerra, Jaime Portilla, Hugo Rojas, Mario A. Macias, Juan-Carlos Castillo
Summary: A regioselective synthesis of two 1-(arylsulfonyl)-1H-1,2,4-triazol-5-amines was described, and the resulting compounds were characterized by various techniques. The compounds exhibited unique molecular structures and packing arrangements. In vitro experiments showed that they possessed promising anticancer activity.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
Article
Chemistry, Organic
Jagseer Singh, Pooja A. Chawla, Rohit Bhatia, Shamsher Singh
Summary: The study synthesized and screened fifteen 2,5-disubstituted-4thiazolidinones with potential anti-inflammatory and antioxidant activities. The compounds showed activities close to standard drugs and could target degenerative disorders associated with inflammation and free radical generation.
LETTERS IN ORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Salvatore Princiotto, Loana Musso, Fabrizio Manetti, Valentina Marcellini, Giovanni Maga, Emmanuele Crespan, Cecilia Perini, Nadia Zaffaroni, Giovanni Luca Beretta, Sabrina Dallavalle
Summary: Inhibition of c-Src is a widely studied approach in cancer treatment and this study focused on synthesizing and evaluating the inhibitory potency and cytotoxic activity of various functionalized indolinones. The researchers found that compounds with an amino group had increased affinity towards the ATP-binding site of c-Src, while bulkier derivatizations improved interactions within the enzymatic pocket. These findings provide an early stage towards the development of easily functionalized indolinones as potential c-Src inhibitors.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
S. Sisira, K. S. Hithisha, J. Syama Sankar, N. Nazirin, R. K. Vimalraj, M. Kalaimathi
Summary: In this study, CuONPs were synthesized using plant extracts and characterized using various techniques. The results showed that CuONPs exhibited significant anticancer activity against MM2 cell lines, indicating their potential for further cancer research and drug discovery.
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Adam A. A. Sulaiman, Ali Alhoshani, Saeed Ahmad, Abdul Malik Puthan Peedikakkal, Ahmed K. Abogosh, Meshal Alghanem, Mohamed A. Mahmoud, W. A. Alanazi, Noura Alasmael, Muhammad Monim-ul-Mehboob, Anvarhusein A. Isab
Summary: Four new phosphanegold(I) complexes were synthesized and characterized, showing excellent cytotoxicity against human cancer cell lines, with one complex inducing apoptosis in A549 cells in a concentration-dependent manner.
INORGANICA CHIMICA ACTA
(2021)
Article
Hematology
Christian Pecquet, Nicolas Papadopoulos, Thomas Balligand, Ilyas Chachoua, Amandine Tisserand, Audrey Nedelec, Didier Vertommen, Anita Roy, Caroline Marty, Harini Nivarthi, Mira El-Khoury, Eva Hug, Andrea Majoros, Erica Xu, Oleh Zagrijtschuk, Tudor E. Fertig, Daciana S. Marta, Heinz Gisslinger, Bettina Gisslinger, Martin Schalling, Ilaria Casetti, Elisa Rumi, Daniela Pietra, Chiara Cavalloni, Luca Arcaini, Mario Cazzola, Norio Komatsu, Yoshihiko Kihara, Yoshitaka Sunami, Yoko Edahiro, Marito Araki, Roman Lesyk, Veronika Buxhofer-Ausch, Sonja Heibl, Florence Pasquier, Violaine Havelange, Isabell Plo, William Vainchenker, Robert Kralovics, Stefan N. Constantinescu
Summary: Mutant CALR proteins bind to and activate the TpoR in cells, driving the development of myeloproliferative neoplasms. These mutant CALR proteins can be found in patient plasma complexed with sTFR1, which increases their stability. They can specifically interact with TpoR on target cells and promote thrombopoietin-independent colony formation.
Article
Chemistry, Medicinal
Yevhenii Novodvorskyi, Roman Lesyk, Igor Komarov, Dmitry Lega, Iryna Zhuravel, Oleh Moskalenko, Volodymyr Sukhoveev, Anatolii Demchenko
Summary: Yellow fever disease is a public health concern in the tropics, and there is currently a lack of effective treatment. Researchers synthesized a series of new compounds and tested their inhibitory activity against yellow fever virus. Four compounds with strong inhibitory activity were identified, which showed good toxicity profile, making them potential candidates for further evaluation in the treatment of yellow fever virus infection.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Andrii Pyrih, Andrzej Lapinski, Sylwia Ziebab, Roman Lesyk, Mariusz Jaskolski, Andrzej K. Gzella
Summary: New compounds, 5-dimethylaminomethylidene-4-phenylamino-1,3-thiazol-2(5H)-one and 5-methoxycarbonylmethylidene-4-phenylamino-1,3-thiazol-2(5H)-one, were synthesized and studied. Their crystal structure, chemical environment, and intermolecular interactions were analyzed using various methods, including X-ray diffraction, NMR, and FT-IR spectroscopy. The compounds exhibited amine tautomeric form in both solution and solid state, and the molecular interactions were investigated with a focus on stereoisomerism and proton tautomerism. The conformational analysis revealed the preferred coplanar arrangement of the thiazolin-2-one and phenyl systems.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Medicinal
Iryna Ivasechko, Andrii Lozynskyi, Julia Senkiv, Piotr Roszczenko, Yuliia Kozak, Nataliya Finiuk, Olga Klyuchivska, Nataliya Kashchak, Nazar Manko, Zvenyslava Maslyak, Danylo Lesyk, Andriy Karkhut, Svyatoslav Polovkovych, Robert Czarnomysy, Olga Szewczyk, Andriy Kozytskiy, Olexandr Karpenko, Dmytro Khyluk, Andrzej Gzella, Krzysztof Bielawski, Anna Bielawska, Petr Dzubak, Sona Gurska, Marian Hajduch, Rostyslav Stoika, Roman Lesyk
Summary: A series of 11-substituted 9-hydroxy-3,5,10,11-tetrahydro-2H-benzo[6,7]thiochromeno[2,3-d][1,3]thiazole-2,5,10-triones were synthesized and their structures were confirmed through spectral data and X-ray diffraction analysis. These compounds showed potential anticancer activity, particularly compound 3.10 which exhibited a cytotoxic effect similar to doxorubicin but was less toxic to normal cells. In vivo testing on mice showed that compound 3.10 had no acute toxic effects on their blood parameters, indicating its potential as a bio-tolerant anticancer drug.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Agnieszka Gornowicz, Roman Lesyk, Robert Czarnomysy, Serhii Holota, Yulia Shepeta, Bozena Poplawska, Magdalena Podolak, Wojciech Szymanowski, Krzysztof Bielawski, Anna Bielawska
Summary: Combining chemotherapy with immunotherapy is a promising strategy in treating gastric cancer with confirmed HER2 expression. Novel 4-thiazolidinone derivatives and anti-HER2 antibodies show potential in increasing the sensitivity of gastric cancer cells to treatment. The molecular mechanism of action involves apoptosis induction and decreased inflammation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Organic
Yiliang Chen, Wenwen Pan, Xiaolong Ding, Liang Zhang, Qinfei Xia, Qi Wang, Qian Chen, Qinghe Gao, Jufen Yan, Roman Lesyk, Zilong Tang, Xinya Han
Summary: A series of novel nitrobenzoxadiazole-piperazine hybrids were designed, synthesized, and evaluated for their anticancer activities. The hybrids 3u, 3v, and 3w with a chloromethyl substitution exhibited the most potent anticancer effects. Compound 3u triggered apoptosis in cancer cell lines through hydrolyzing of PARP and effectively inhibited colony formation. Compound 3u shows potential as a promising lead compound for discovering novel antitumor agents.
Review
Chemistry, Multidisciplinary
Stepan Sysak, Beata Czarczynska-Goslinska, Piotr Szyk, Tomasz Koczorowski, Dariusz T. Mlynarczyk, Wojciech Szczolko, Roman Lesyk, Tomasz Goslinski
Summary: Flavonoids are widely found in plants and have various medical applications. Combining flavonoids with nanocarriers can improve their bioavailability and create systems with wider functionalities. The conjugates of flavonoid-metal nanoparticles have unique physicochemical and biological properties, including improved selectivity towards target sites. Furthermore, flavonoids can also play a role in the initial step of metal nanomaterial preparation.
Article
Chemistry, Multidisciplinary
Andrii Pyrih, Andrzej Lapinski, Sylwia Zieba, Adam Mizera, Roman Lesyk, Mariusz Jaskolski, Andrzej K. Gzella
Summary: Three new derivatives of 5-dimethylaminomethylidene-4-phenylamino-1,3-thiazol-2(5H)-one were synthesized and their prototropic tautomerism was studied. The compounds were found to exist solely in the amino tautomeric form in both solid and liquid phases. The electronic effects, molecular conformation, and intermolecular interactions in the crystals were analyzed.
ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE CRYSTAL ENGINEERING AND MATERIALS
(2023)
Article
Chemistry, Multidisciplinary
Andrii Pyrih, Andrzej Lapinski, Sylwia Zieba, Adam Mizera, Roman Lesyk, Andrzej K. Gzella, Mariusz Jaskolski
Summary: In this study, two derivatives were synthesized to investigate the structural changes associated with proton tautomerism of the amidine system. The results showed that the studied compounds exist in the amine tautomeric form in both solid and liquid states.
ACTA CRYSTALLOGRAPHICA SECTION C-STRUCTURAL CHEMISTRY
(2023)
Review
Cell Biology
Olga Klaudia Szewczyk-Roszczenko, Piotr Roszczenko, Anna Shmakova, Nataliya Finiuk, Serhii Holota, Roman Lesyk, Anna Bielawska, Yegor Vassetzky, Krzysztof Bielawski
Summary: Endocytosis is a major cellular communication process that can be hijacked by pathogens and involved in oncogenic transformation. This review explores different approaches to inhibit endocytosis, discusses chemical inhibitors, and explores potential clinical applications.
Article
Pharmacology & Pharmacy
Sergii Demchenko, Roman Lesyk, Oleh Yadlovskyi, Serhii Holota, Sergii Yarmoluk, Sergii Tsyhankov, Anatolii Demchenko
Summary: Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used but searching for and creating new NSAIDs continues to be a challenge due to risks associated with their use. This study focuses on triazole-azepine hybrid molecules as potential NSAIDs. In silico evaluation using SwissADME and in vivo screening in mice were conducted, resulting in identification of derivatives with greater activity compared to reference drugs. Preliminary SAR analysis was performed based on screening results.
SCIENTIA PHARMACEUTICA
(2023)
Article
Pharmacology & Pharmacy
Yulian Konechnyi, Andrii Lozynskyi, Iryna Ivasechko, Tetiana Dumych, Solomiya Paryzhak, Oksana Hrushka, Ulyana Partyka, Iryna Pasichnyuk, Dmytro Khylyuk, Roman Lesyk
Summary: In this study, a previously studied compound was screened for antimicrobial, antifungal, anti-allergic, and antitumor activities. It was found to have slight antimicrobial and antitumor activity, as well as anti-inflammatory and anti-allergic activities. Molecular docking confirmed its good bonding with specific targets and it was identified as a potential PPAR? modulator, which is important in allergy, cancer, and cardiovascular diseases pathogenesis.
SCIENTIA PHARMACEUTICA
(2023)
Article
Pharmacology & Pharmacy
Yuliia Kremin, Lilia Lesyk, Roman Lesyk, Oksana Levytska, Bohdan Hromovyk
Summary: As members of a public trust profession, pharmacists are the most accessible medical team members. Therefore, every pharmacist must know the scope of their professional roles and professional functions. The study aimed to detail the major roles into a pooled set of functions.
SCIENTIA PHARMACEUTICA
(2023)
Article
Biochemistry & Molecular Biology
Anna Kryshchyshyn-Dylevych, Danylo Kaminskyy, Roman Lesyk
Summary: This study synthesized and screened a class of novel thiopyranothiazole molecules with broad pharmacological profiles against various viruses. The results showed that some derivatives exhibited strong antiviral activity against Influenza Virus type A, indicating the potential of thiopyranothiazoles as antiviral agents.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Article
Chemistry, Physical
Andrii Pyrih, Andrzej Lapinski, Sylwia Zieba, Adam Mizera, Roman Lesyk, Andrzej K. Gzella, Mariusz Jaskolski
Summary: In this article, we reported the recent findings of our systematic studies on the effects of phenyl-ring substituents on proton tautomerism and stereoisomerism in 4-phenylamino-1,3-thiazol-2(5H)-one derivatives. Through synthesis, spectral analysis, and crystal studies, we found that these compounds exist solely in the amino tautomeric form and exhibit a specific arrangement.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
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)
