Article
Pharmacology & Pharmacy
Magda F. Mohamed, Nada S. Ibrahim, Amna A. Saddiq, Omar A. Almaghrabi, Maha E. Al-Hazemi, Hamdi M. Hassaneen, Ismail A. Abdelhamid
Summary: A new series of chalcones has been developed for potential use in treating lung cancer. Spectral tools were used to confirm the existence of the new series, and MTT assay and molecular docking studies were conducted to evaluate their cytotoxic and apoptotic effects on lung cancer cells.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Arif Khan, Fatima Naaz, Rafia Basit, Deepak Das, Piyush Bisht, Majeed Shaikh, Bilal Ahmad Lone, Yuba Raj Pokharel, Qazi Naveed Ahmed, Shazia Parveen, Intzar Ali, Shashank Kumar Singh, Gousia Chashoo, Syed Shafi
Summary: A series of novel 1,2,3-triazole derivatives of capsaicin, including a new natural product hybrid capsaicinoid, were synthesized. Most of the synthesized compounds showed antiproliferative activity against various cancer cell lines, with lung cancer cell lines being the most sensitive. Compound 18f demonstrated the best antiproliferative activity and acted through inducing cell apoptosis and altering mitochondrial membrane potential.
Article
Biochemistry & Molecular Biology
Zuleima Blanco, Esteban Fernandez-Moreira, Michael R. Mijares, Carmen Celis, Gricelis Martinez, Juan B. De Sanctis, Sona Gurska, Petr Dzubak, Marian Hajduch, Ali Mijoba, Yael Garcia, Xenon Serrano, Nahum Herrera, Jhonny Correa-Abril, Yonathan Parra, Jorge Angel, Hegira Ramirez, Jaime E. Charris
Summary: This research reports 16 synthetic chalcone derivatives with potential therapeutic activities against parasites and cancer cells.
Article
Biochemistry & Molecular Biology
Aliaa M. Mohassab, Heba A. Hassan, Dalia Abdelhamid, Ahmed M. Gouda, Bahaa G. M. Youssif, Hiroshi Tateishi, Mikako Fujita, Masami Otsuka, Mohamed Abdel-Aziz
Summary: A series of new quinoline/chalcone hybrids containing 1,2,4-triazole moiety were designed and synthesized in this study, showing moderate to good activity against various cancer cell lines. Some of these compounds exhibited promising antiproliferative activities and displayed high binding affinities in inhibiting EGFR and BRAF(V600E) kinases.
BIOORGANIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Fatemeh Zomorodi Anbaji, Seyed Jalal Zargar, Saeed Tavakoli
Summary: This study aimed to isolate and evaluate the antineoplastic potential of grandivittin (GRA) in human lung cancer A549 cells. The results showed that GRA induced apoptosis in a dose- and time-dependent manner and decreased cell viability. The expression of apoptotic genes (caspase 3, caspase 9, Bax, P53) was upregulated, while Bcl2 was downregulated after GRA treatment. Therefore, GRA may be a potential new therapeutic agent for the treatment of lung cancer.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2023)
Article
Chemistry, Physical
Hannah Clara, Johanan Christian Prasana, D. Reuben Jonathan, V. Vishwanathan
Summary: The novel third-order nonlinear organic single crystal DMBH exhibits excellent properties such as optical characteristics, thermal stability, molecular structure, and laser damage threshold, making it suitable for nonlinear optical applications. The experimental and theoretical studies confirm its superior performance compared to urea and other chalcone derivatives.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Physical
J. Christina Jebapriya, D. Reuben Jonathan, Shivaraj R. Maidur, Prabhu Nallamuthu, Parutagouda Shankaragouda Patil, Johanan Christian Prasana
Summary: CPDAPP, a novel chalcone derivative, exhibits significant optical properties and shows promise for nonlinear optical applications.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Physical
Mairton C. Romeu, Paulo T. C. Freire, Alejandro P. Ayala, Antonio C. H. Barreto, Larissa S. Oliveira, Mateus R. de Oliveira, Paulo N. Bandeira, Helcio S. dos Santos, Alexandre M. R. Teixeira, Daniel L. M. Vasconcelos
Summary: Dihydrochalcones, characterized by the reduction of unsaturated carbons, are promising structures in medicinal chemistry. In this study, a dihydrochalcone compound, DIHYDROCHAL, was synthesized and characterized using various techniques. The crystal structure of DIHYDROCHAL was found to be monoclinic with molecules arranged in layers. Theoretical quantum chemistry calculations provided insights into its structural, vibrational, and electronic properties.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biology
Guang-Yan Zhang, Wei-Yong Chen, Xiao-Bo Li, Hua Ke, Xue-Lin Zhou
Summary: The study demonstrated that scutellarin significantly inhibited cell viability and increased apoptosis in A549 lung cancer cells. Scutellarin promoted intracellular ROS production, TGF-beta 1/smad2 signaling pathway activation, and cleaved caspase-3 expression, which could be partly reversed by Tempo treatment. Moreover, blocking the TGF-beta 1/smad2 pathway with SB431542 inhibited scutellarin-induced intracellular ROS production and cleaved caspase-3 expression.
OPEN LIFE SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Henoc del Rosario, Ester Saavedra, Ignacio Brouard, Daniel Gonzalez-Santana, Celina Garcia, Elena Spinola-Lasso, Carlos Tabraue, Jose Quintana, Francisco Estevez
Summary: Synthetic flavonoids with new substitution patterns show potential as anticancer drugs. In this study, twelve chalcones were synthesized and their antiproliferative effects on human tumour cells were evaluated. The most cytotoxic chalcones contained a furoyl substituent linked by an ester or an amide through the 2'-hydroxy or the 2'-amino group of the chalcone skeleton. The synthetic chalcone 2'-furoyloxy-4-methoxychalcone (FMC) displayed higher potency than the antineoplastic agent etoposide and had less toxicity on normal blood cells. The mechanism of action involved cell cycle arrest, induction of apoptosis, and inhibition of tubulin polymerization, and depended on the generation of reactive oxygen species.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Physical
Mohamed Hisham, Heba A. Hassan, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Alaa M. Hayallah, Mohamed Abdel-Aziz
Summary: A new series of quinazoline-4-one/chalcone hybrids, 7-26, were synthesized and tested as EGFR inhibitors with antiproliferative activity. Three compounds showed the greatest antiproliferative activity and were the most potent EGFR inhibitors. These three compounds improved the levels of active caspase-3, 8, and 9, induced cytochrome c and Bax levels, and down regulated Bcl_2 levels. The most active inhibitors docked well inside EGFR active sites.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Review
Neurosciences
Aziz Unnisa, Nigel H. H. Greig, Mohammad Amjad Kamal
Summary: Traumatic brain injury (TBI) is a major cause of death and morbidity, and is the focus of translational research. Apoptosis is important in the pathophysiology of TBI, and inhibiting it may improve functional recovery. Caspases, such as Caspase-3 and Caspase-9, are key mediators of cell death due to apoptosis in TBI. Understanding these apoptotic pathways and finding ways to inhibit Caspases may have significant treatment implications for TBI.
CURRENT NEUROPHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Jing Chen, Zhenghuan Rao, Qinqin Li, Tao Jiang, Yuan Chen, Xia Gu, Mengyue Miao, Daifeng Hu, Hui Zhou, Alexander Tobias Teichmann, Youzhe Yang
Summary: The study demonstrates the beneficial effects of FK-morph on a surgically induced endometriosis rat model. FK-morph effectively reduces the volumes and adhesion scores of implants, downregulates inflammatory cytokines and chemokines levels, mediates cell apoptosis of endometriosis foci, and attenuates angiogenesis by decreasing the expression of VEGF. The underlying mechanism involves blocking the activation of the PI3K/Akt and NF-xB signaling pathways.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Meigui Zhang, Jing Li, Ruixia Ma, Jiahui Xi, Lili Xi, Baoxin Zhang, Jing Tian, Zhongtian Bai
Summary: In this study, it was found that TMOCC inhibits proliferation and promotes apoptosis in liver cancer cells by suppressing the RAS-ERK and AKT/FOXO3a signaling pathways. Additionally, potential target proteins such as ERK1, PARP-1, and BAX were identified. These findings suggest that TMOCC could be a promising multi-target compound for liver cancer treatment.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Biochemistry & Molecular Biology
Vera Belousova, Oxana Svitich, Elena Timokhina, Irina Ignatko, Irina Bogomazova, Svetlana Pesegova, Tatiana Silaeva, Tatiana Kuzmina, Oxana Skorobogatova
Summary: This article presents the hypothesis that premature placenta apoptosis could be a potential cause of preterm birth, supported by evaluating gene expression. The study found that during pregnancy, the expression of apoptosis-related genes in the placenta is low, but the expression of the apoptosis inhibitor XIAP is high. However, at the onset of preterm labor, the expression of apoptosis-related genes increases significantly, potentially initiating preterm birth.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Hossameldin A. Aziz, Gamal A. I. Moustafa, Gamal El-Din A. Abuo-Rahma, Safwat M. Rabea, Glenn Hauk, Vagolu S. Krishna, Dharmarajan Sriram, James M. Berger, Samar H. Abbas
Summary: A new series of nitric oxide-donating fluoroquinolone/oximes were synthesized, showing higher activity in antitubercular and antibacterial evaluations. Mycobacterial DNA cleavage and molecular modeling were used to explain the bioactivity observed. Oximes3c-e were highly potent against Klebsiella pneumoniae, while ketone2c and oxime4c were more active against Staphylococcus aureus than ciprofloxacin.
ARCHIV DER PHARMAZIE
(2021)
Article
Biochemistry & Molecular Biology
Hamada H. H. Mohammed, Samar H. Abbas, Alaa M. Hayallah, Gamal El-Din A. Abuo-Rahma, Yaser A. Mostafa
Summary: A novel series of urea-linked ciprofloxacin-chalcone hybrids 3a-j showed significant antiproliferative activities against colon cancer and leukemia cells, making them potential candidates for further optimization as antitumor agents.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Aliaa M. Mohassab, Heba A. Hassan, Dalia Abdelhamid, Ahmed M. Gouda, Bahaa G. M. Youssif, Hiroshi Tateishi, Mikako Fujita, Masami Otsuka, Mohamed Abdel-Aziz
Summary: A series of new quinoline/chalcone hybrids containing 1,2,4-triazole moiety were designed and synthesized in this study, showing moderate to good activity against various cancer cell lines. Some of these compounds exhibited promising antiproliferative activities and displayed high binding affinities in inhibiting EGFR and BRAF(V600E) kinases.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Muhamad Mustafa, Gamal El-Din A. Abuo-Rahma, Amer Ali Abd El-Hafeez, Esam R. Ahmed, Dalia Abdelhamid, Pradipta Ghosh, Alaa M. Hayallah
Summary: Small molecule inhibitors of focal adhesion kinase have shown promising therapeutic potential in cancer treatment. Among the 1,2,4-triazole derivatives tested, compounds 3c and 3d demonstrated the strongest antiproliferative activity, with 3d being identified as a potent preclinical candidate for cancer treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Abdelfattah Hassan, Mohamed Badr, Heba A. Hassan, Dalia Abdelhamid, Gamal El-Din A. Abuo-Rahma
Summary: A new series of synthesized compounds showed high anticancer activity, with one dihalogenated derivative exhibiting the best cytotoxicity. Some compounds exhibited VEGFR-2 inhibitory activity similar to sorafenib, indicating potential antiproliferative effects.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Hamada H. H. Mohammed, Amer Ali Abd El-Hafeez, Kareem Ebeid, Aml Mekkawy, Mohammed A. S. Abourehab, Emad Wafa, Suhaila O. Alhaj-Suliman, Aliasger K. Salem, Pradipta Ghosh, Gamal El-Din A. Abuo-Rahma, Alaa M. Hayallah, Samar H. Abbas
Summary: The novel ciprofloxacin hybrids demonstrated remarkable anti-proliferative activity against colon cancer cells by inhibiting topoisomerase and tubulin polymerization, suggesting their potential as novel anticancer agents. Their mechanism of action involves DNA damage and cell cycle arrest through the ATR/CHK1/Cdc25C pathway.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Hamada H. H. Mohammed, Doaa Mohamed Elroby Ali, Mohamed Badr, Ahmed G. K. Habib, Abobakr Mohamed Mahmoud, Sarah M. Farhan, Shimaa Salah Hassan Abd El Gany, Soad A. Mohamad, Alaa M. Hayallah, Samar H. Abbas, Gamal El-Din A. Abuo-Rahma
Summary: A series of N-4 piperazinyl ciprofloxacin derivatives were synthesized and showed broad antibacterial and antifungal activities. Some of the derivatives also exhibited inhibitory activity against DNA gyrase.
MOLECULAR DIVERSITY
(2023)
Article
Chemistry, Medicinal
Fatma Fouad Hagar, Samar H. Abbas, Dalia Abdelhamid, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Mohamed Abdel-Aziz
Summary: A series of new 1,3,4-oxadiazole-chalcone/benzimidazole hybrids were synthesized and investigated for their antiproliferative activities. Compounds 9g-i and their oxygen isosteres, 10f-h, exhibited promising antiproliferative activities with IC50 values ranging from 0.80 to 2.27 μM.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Multidisciplinary
Hend A. A. Ezelarab, Heba A. A. Hassan, Gamal El-Din A. Abuo-Rahma, Samar H. H. Abbas
Summary: A series of Ciprofloxacin-Piperazine C-7 linked quinoline derivatives were synthesized and evaluated for their antimicrobial, antifungal, and anti-proliferative activities. Compound 6a, 6b, and 8a demonstrated promising anticancer, antifungal, and antibacterial properties, indicating their potential as lead compounds for drug discovery.
JOURNAL OF THE IRANIAN CHEMICAL SOCIETY
(2023)
Article
Biochemistry & Molecular Biology
Hend A. A. Ezelarab, Taha F. S. Ali, Samar H. Abbas, Ahmed M. Sayed, Eman A. M. Beshr, Heba A. Hassan
Summary: New 3-substituted oxindole derivatives were synthesized and evaluated as antiproliferative agents. Among the tested compounds, compounds 6f and 6g showed remarkable antiproliferative activity against leukemia and breast cancer cell lines. Compound 6f exhibited the most promising antiproliferative activity against MCF-7 (human breast cancer), and inhibited receptor tyrosine EGFR and tubulin polymerization.
MOLECULAR DIVERSITY
(2023)
Review
Chemistry, Medicinal
Mostafa M. Badran, Samar H. Abbas, Mikako Fujita, Mohamed Abdel-Aziz
Summary: Histone deacetylase (HDAC) inhibitors, particularly those based on the pyrimidine scaffold, have shown great potential as bioactive agents against tumors and neurodegenerative disorders. In this article, we provide a comprehensive overview of the successful utilization of pyrimidine and its derivatives in the development of HDAC inhibitors. We also discuss the perspectives and strategies that may guide medicinal chemists in designing more effective chemotherapeutic agents with potential clinical applications in the future.
ARCHIV DER PHARMAZIE
(2023)
Review
Chemistry, Multidisciplinary
Hend A. A. Ezelarab, Taha F. S. Ali, Samar H. H. Abbas, Heba A. A. Hassan, Eman A. M. Beshr
Summary: FLT3 mutations are common in AML patients and are associated with poor clinical response. Several FLT3 inhibitors have been developed, but the overall survival rate in AML patients is still low. This review summarizes the indole-based FLT3 inhibitors and their chemotypes, mechanism of action, and interaction mode. It provides insights for future exploration of new therapies for FLT3-related AML.
Article
Chemistry, Multidisciplinary
Fatma Fouad Hagar, Samar H. Abbas, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Ahmed M. Sayed, Dalia Abdelhamid, Mohamed Abdel-Aziz
Summary: This study successfully demonstrated the potential of new compounds in cancer treatment and induction of apoptosis. The compounds showed inhibitory effects on cell proliferation, EGFR, and BRAF(V600E), and induced apoptosis in cancer cells.
Review
Chemistry, Multidisciplinary
Mostafa A. Mansour, Asmaa M. AboulMagd, Samar H. Abbas, Hamdy M. Abdel-Rahman, Mohamed Abdel-Aziz
Summary: Lung cancer is the second most common cause of morbidity and mortality among cancer types worldwide, with non-small cell lung cancer (NSCLC) representing the majority of most cases. EGFR TKIs are widely used as targeted therapy for NSCLC, but their efficacy is compromised by acquired mutations, including C797S. The development of next-generation EGFR TKIs that selectively inhibit EGFR triple mutations is of urgent medical need. This review discusses the design of fourth-generation EGFR TKIs, their binding interactions, clinical difficulties, and potential outcomes of treating patients with C797S mutation.
Review
Chemistry, Organic
Abdelfattah Hassan, Heba A. Hassan, Dalia Abdelhamid, Gamal El-Din A. Abuo-Rahma
Summary: In this literature review, various methods of synthesizing antimicrobial thiazole derivatives published in the past decade are comprehensively discussed, with a focus on those exhibiting antibacterial, antimycobacterial, and/or antifungal activity. The diversity of thiazole-derived antimicrobial agents is highlighted through categorization into chemical classes, showcasing the common methods of thiazole ring closure and the antimicrobial activity of the most potent derivatives.
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)