Review
Biochemistry & Molecular Biology
Hina Shamshad, Rowaida Bakri, Agha Zeeshan Mirza
Summary: Parasitic diseases have significant impact on global health and economy. Targeting three main enzymes through hybrid approaches shows promise in treating these diseases and can play a significant role in the future.
MOLECULAR BIOLOGY REPORTS
(2022)
Article
Biochemistry & Molecular Biology
Saira Khatoon, Aiman Aroosh, Arshad Islam, Saima Kalsoom, Faisal Ahmad, Shahid Hameed, Sumra Wajid Abbasi, Masoom Yasinzai, Muhammad Moazzam Naseer
Summary: Novel coumarin-incorporated isatin hydrazones were synthesized and evaluated as potent antileishmanial agents, with three compounds showing high activity and biocompatibility in vitro experiments against Leishmania tropica.
BIOORGANIC CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Shefali Chowdhary, Shalini, Amandeep Arora, Vipan Kumar
Summary: Isatin is recognized as an attractive therapeutic fragment in drug design and development, particularly for developing new anticancer scaffolds. It also has potential in treating Neglected Tropical Diseases (NTDs).
Review
Chemistry, Analytical
Tais Aparecida Reis Cordeiro, Mayra Asevedo Campos de Resende, Simone Cristina dos Santos Moraes, Diego Leoni Franco, Arnaldo Cesar Pereira, Lucas Franco Ferreira
Summary: Neglected tropical diseases are a group of infectious and parasitic diseases prevalent in tropical and subtropical regions, with limited access to proper healthcare. The development of low-cost biosensors for fast diagnosis in these areas is crucial for better treatment and eradication. While progress has been made in the past decade, challenges remain in early detection of neglected tropical diseases using biosensors.
Article
Chemistry, Medicinal
Atamjit Singh, Harneetpal Kaur, Saroj Arora, Preet Mohinder Singh Bedi
Summary: Novel hydrazine-linked morpholinated isatin-quinoline hybrids were designed, synthesized, and evaluated as potent and safer anti-breast cancer agents, showing high inhibitory potential against hormone-positive breast cancer cells with selective action and mitotic arrest at the G(2)/M phase, suggesting AS-4 as a potential lead compound for further development.
ARCHIV DER PHARMAZIE
(2022)
Review
Rheumatology
Rasmi Ranjan Sahoo, Anupam Wakhlu, Vikas Agarwal
Summary: Dealing with rheumatic diseases in tropical countries is complex due to limited healthcare infrastructure, lack of diagnostic and therapeutic facilities, impact of dominant prevalent diseases, and challenges in differentiating from infectious and non-infectious disease mimics. Several tropical diseases present with musculoskeletal and rheumatic manifestations, leading to delayed diagnosis or misdiagnosis and poor patient outcomes.
CLINICAL RHEUMATOLOGY
(2022)
Review
Pharmacology & Pharmacy
Rachel H. Clare, Steven R. Hall, Rohit N. Patel, Nicholas R. Casewell
Summary: Snakebite envenoming causes up to 138,000 deaths annually, making it the deadliest neglected tropical disease. Current treatment with biologic antivenoms is outdated and expensive, but there is great potential in developing small molecule drugs to inhibit venom toxins. Strategies successful in treating other NTDs could be utilized to facilitate the development of next-generation snakebite treatments.
TRENDS IN PHARMACOLOGICAL SCIENCES
(2021)
Article
Immunology
Martin Walker, Jonathan I. D. Hamley, Philip Milton, Frederic Monnot, Sally Kinrade, Sabine Specht, Belen Pedrique, Maria-Gloria Basanez
Summary: Drug-based interventions are crucial in addressing major diseases, with a growing consensus on the need for new therapeutic options in some cases. In this field, minimizing wastage of money and resources is essential.
CLINICAL INFECTIOUS DISEASES
(2021)
Article
Immunology
Hollie-Ann Hatherell, Hope Simpson, Rebecca F. Baggaley, T. Deirdre Hollingsworth, Rachel L. Pullan
Summary: The WHO's 2030 road map for neglected tropical diseases highlights the importance of strengthened, institutionalized post-elimination surveillance, but lacks practical guidance on implementation. Nationally representative survey programs, such as DHS, may provide a platform for integrating disease surveillance within national health systems, with a focus on maximizing utility and addressing priorities for further data collection and characterization.
CLINICAL INFECTIOUS DISEASES
(2021)
Article
Infectious Diseases
Wendemagegn Enbiale, Alemayehu Bekele, Nigus Manaye, Fikre Seife, Zeyede Kebede, Filmon Gebremeskel, Johan van Griensven
Summary: Subcutaneous mycoses are endemic in Ethiopia, with cases reported throughout the country, especially in the northern regions. The lack of research and surveillance programs for these diseases highlights the need for routine programs and systems to identify and record cases.
PLOS NEGLECTED TROPICAL DISEASES
(2023)
Review
Pharmacology & Pharmacy
Leonardo L. G. Ferreira, Josue de Moraes, Adriano D. Andricopulo
Summary: Neglected tropical diseases, such as leishmaniasis and schistosomiasis, continue to be a public health challenge in developing countries. However, advancements in drug discovery using modern strategies have shown promise in addressing these diseases by combining medicinal chemistry and parasite biology.
DRUG DISCOVERY TODAY
(2022)
Article
Immunology
Amanda Minter, Lorenzo Pellis, Graham F. Medley, T. Deirdre Hollingsworth
Summary: As countries strive to meet WHO goals for reducing morbidity and eliminating disease transmission, they will need to plan for the next stages of surveillance and control in low prevalence settings. Going beyond simple predictions of treatment program effectiveness, more nuanced intervention choices informed by quantitative analyses will be necessary for sustainable gains in the long term. Identifying policy goals and finding the right balance between intervention and surveillance constraints will be key challenges in achieving multiple aims such as minimizing morbidity and costs simultaneously.
CLINICAL INFECTIOUS DISEASES
(2021)
Review
Infectious Diseases
Theresa W. Gyorkos, Helene Carabin, Maneesh Phillip, Leshawn Benedict, Amy Davis, Janet Hatcher Roberts, Kishor M. Wasan, Momar Ndao, Alison Krentel
Summary: Canadian researchers have published over 160 publications per year on neglected tropical diseases between 2010 and 2019, covering all 20 NTDs. The most commonly studied diseases were leishmaniasis, dengue fever, chikungunya, Chagas disease, soil-transmitted helminthiases, and rabies.
PLOS NEGLECTED TROPICAL DISEASES
(2021)
Review
Chemistry, Medicinal
Igor Jose dos Santos Nascimento, Misael de Azevedo Teotonio Cavalcanti, Ricardo Olimpio de Moura
Summary: Neglected tropical diseases (NTDs) are a group of infectious diseases that mainly affect impoverished populations in tropical countries. They cause many deaths worldwide and require substantial investments in public health to treat and control them. Protozoan diseases such as Chagas disease, sleeping sickness, and Leishmaniasis, as well as the big three diseases (AIDS, tuberculosis, and malaria), are endemic in tropical countries. However, there is still a gap in treatment, emphasizing the need for new alternatives.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Medicine, General & Internal
Juan Garcia-Bernalt Diego, Pedro Fernandez-Soto, Antonio Muro
Summary: Neglected Tropical Diseases (NTDs), particularly those caused by parasites, continue to be a major public health issue in tropical and subtropical regions, affecting 10% of the global population. Isothermal nucleic acid amplification techniques, especially loop-mediated isothermal amplification (LAMP), have emerged as an affordable alternative to PCR for molecular diagnostics in parasite-caused NTDs.
Article
Biochemistry & Molecular Biology
Tarfah Al-Warhi, Ahmed A. Al-Karmalawy, Ayman Abo Elmaaty, Maha A. Alshubramy, Marwa Abdel-Motaal, Taghreed A. Majrashi, Medhat Asem, Ahmed Nabil, Wagdy M. Eldehna, Marwa Sharaky
Summary: In this study, a set of pyridine and pyrimidine derivatives were evaluated for their effects on cell cycle and apoptosis. Compounds 8 and 14 exhibited outstanding effects on various cancer cell lines and showed antioxidant and EGFR kinase inhibitory potential.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Hosam M. El-Seadawy, Kamilia Abo A. El-Seoud, Mona El-Aasr, Haytham O. Tawfik, Wagdy M. Eldehna, Amany E. Ragab
Summary: This study investigated the biological activities of Zamia floridana leaves extract and its fractions, and found that the n-butanol fraction exhibited inhibitory activity against Toxoplasma gondii and cytotoxic effects on MCF-7 and HCT-116 cancer cells. Six compounds, including three biflavonoids and two phenolic acid derivatives, were isolated from the n-butanol fraction.
Article
Biochemistry & Molecular Biology
Heba A. S. El-Nashar, Ahmed M. Sayed, Hany A. M. El-Sherief, Mostafa E. Rateb, Lina Akil, Ibrahim Khadra, Taghreed A. Majrashi, Sara T. Al-Rashood, Faizah A. Binjubair, Mahmoud A. El Hassab, Wagdy M. Eldehna, Usama Ramadan Abdelmohsen, Nada M. Mostafa
Summary: This study investigated the metabolic profile and anti-trypanosomal effect of the methanol extract of Thunbergia grandifolia leaves. Fifteen compounds of different classes were identified using LC-HRESIMS. The extract showed a strong inhibitory activity against T. brucei TC 221 and two compounds were identified as potential targets. Both compounds showed acceptable drug-like properties.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Mohammed A. F. Elewa, Wagdy M. Eldehna, Ahmed M. E. Hamdan, Samraa H. Abd El-kawi, Asmaa M. El-Kalaawy, Taghreed A. Majrashi, Reham F. Barghash, Hatem A. Abdel-Aziz, Khalid S. Hashem, Mohammed M. H. Al-Gayyar
Summary: This study evaluated the antitumor activity of WRH-2412 in rats with hepatocellular carcinoma (HCC) by affecting the TGF-beta/beta-catenin/alpha-SMA pathway. The results showed that WRH-2412 significantly increased the rats' survival rate and decreased serum alpha-fetoprotein levels. It also reduced the expression of TGF-beta, beta-catenin, SMAD4, fascin, and alpha-SMA in the liver, while increasing the expression of E-cadherin.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Ibrahim H. Eissa, Reda G. Yousef, Hazem Elkady, Aisha A. Alsfouk, Dalal Z. Husein, Ibrahim M. Ibrahim, Nehal El-Deeb, Ahmed M. Kenawy, Wagdy M. Eldehna, Eslam B. Elkaeed, Ahmed M. Metwaly
Summary: A new theobromine-derived EGFR inhibitor with essential structural characteristics to interact with EGFR's pocket was developed. Through DFT studies, the optimized chemical structure and molecular orbital of the compound were analyzed. Molecular docking and dynamics simulations confirmed the effective bonding and inhibition of the compound to EGFR protein. In vitro experiments showed promising anticancer potential against triple-negative breast cancer cell lines, as well as inhibitory effects on other cancer cell lines, and the ability to induce apoptosis.
MOLECULAR DIVERSITY
(2023)
Article
Biochemistry & Molecular Biology
Shaza H. H. Aly, Ahmed M. M. Elissawy, Abdulla M. A. Mahmoud, Fatma Sa'eed El-Tokhy, Sherif S. Abdel Mageed, Hadia Almahli, Sara T. T. Al-Rashood, Faizah A. A. Binjubair, Mahmoud A. El Hassab, Wagdy M. M. Eldehna, Abd El-Nasser B. Singab
Summary: In this study, flavonoid-rich fractions of Glycyrrhiza glabra roots and Sophora japonica leaves were prepared and their compositions were analyzed. The wound healing potential of these fractions was evaluated, and it was found that the topical application of the fractions significantly increased wound healing and reduced oxidative stress. Molecular docking studies also revealed that the major compounds in the fractions could efficiently bind to proteins related to wound healing. Therefore, Glycyrrhiza glabra roots and Sophora japonica leaves may serve as a rich source of bioactive metabolites with antioxidant, anti-inflammatory, and wound healing properties.
Article
Biochemistry & Molecular Biology
Tarfah Al-Warhi, Hadia Almahli, Raed M. Maklad, Zainab M. Elsayed, Mahmoud A. El Hassab, Ohoud J. Alotaibi, Nada Aljaeed, Rezk R. Ayyad, Hazem A. Ghabour, Wagdy M. Eldehna, Mohamed K. El-Ashrey
Summary: In this study, two small molecule series based on the 1-benzyl-5-bromoindolin-2-one scaffold were developed and evaluated for their anticancer activity. The derivatives 7c and 7d showed the best anticancer activity against breast cancer cells. They also demonstrated good inhibitory activity against VEGFR-2. Molecular docking and dynamic simulations were performed to explore the binding mode of 7d within the VEGFR-2 active site.
Article
Chemistry, Medicinal
Moataz A. Shaldam, Ahmed F. Khalil, Hadia Almahli, Maiy Y. Jaballah, Andrea Angeli, Eman F. Khaleel, Rehab Mustafa Badi, Eslam B. Elkaeed, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Summary: New 5-cyano-6-oxo-pyridine-based sulfonamides were designed and synthesized to potentially inhibit both EGFR and CA, with anticancer properties. The inhibitory effects on EGFR were observed, while the inhibitory effects on CA were affected by the neighboring methoxy group.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Heba A. Elsebaie, Eman A. El-Bastawissy, Kamel M. Elberembally, Eman F. Khaleel, Rehab Mustafa Badi, Moataz A. Shaldam, Wagdy M. Eldehna, Haytham O. Tawfik, Tarek F. El-Moselhy
Summary: The current study discovered 15 new thieno[2,3-d]pyrimidine derivatives with potential anticancer action and further validated the inhibitory ability of some compounds on specific cell lines, as well as their role in cell cycle and apoptosis. The biological activities of the most potent compound were also explained through computational methods.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Wagdy M. Eldehna, Eslam E. Mohammed, Ghada H. Al-Ansary, Emanuela Berrino, Mostafa M. Elbadawi, Tamer M. Ibrahim, Maiy Y. Jaballah, Sara T. Al-Rashood, Faizah A. Binjubair, Meltem Celik, Alessio Nocentini, Fawzy A. Elbarbry, Fikrettin Sahin, Hatem A. Abdel-Aziz, Claudiu T. Supuran, Mohamed Fares
Summary: SLC-0111 is a selective hCA IX inhibitor used for the treatment of hypoxic malignancies. In this study, novel structural analogues were designed and synthesized, and their anticancer activity was evaluated.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Moataz A. Shaldam, Denisa Hendrychov, Radwan El-Haggar, Veronika Voj, Taghreed A. Majrashi, Eslam B. Elkaeed, Nicolas Masurier, Vladimir Krystof, Haytham O. Tawfik, Wagdy M. Eldehna
Summary: A study reports the development of novel derivatives of pyrimido[1,2-a]benzimidazole as potential anti-AML agents. Compound 5h exhibited effective anti-tumor activity at low micromolar concentration, particularly against leukemia. Furthermore, compounds 5e-h showed single-digit micromolar activity against acute leukemia cell lines. Pyrimido[1,2-a]benzimidazoles 5e and 5h significantly inhibited BMX kinase.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Samaa Saied, Moataz Shaldam, Mostafa M. Elbadawi, Simone Giovannuzzi, Alessio Nocentini, Hadia Almahli, Rofaida Salem, Tamer M. Ibrahim, Claudiu T. Supuran, Wagdy M. Eldehna
Summary: In this study, a series of novel indolinone-based benzenesulfonamides were designed and synthesized as potential dual inhibitors for cancer-associated hCA IX/XII and VEGFR-2. The synthesized sulfonamides displayed varying degrees of inhibitory effect against hCA isoforms I, II, IX, and XII. The most effective and selective hCA IX and XII inhibitors 8g, 8j, and 15b were further tested for their inhibitory and antiproliferative impact against VEGFR-2 overexpressing breast cancer cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Ahmed E. Elsawi, Mostafa M. Elbadawi, Alessio Nocentini, Hadia Almahli, Simone Giovannuzzi, Moataz Shaldam, Rofaida Salem, Tamer M. Ibrahim, Hatem A. Abdel-Aziz, Claudiu T. Supuran, Wagdy M. Eldehna
Summary: Currently, dual targeting by a single small molecule is considered an effective strategy for cancer treatment. In this study, novel SLC-0111 analogues with dual inhibitory activities against CA IX/XII and VEGFR-2 were designed and synthesized. The inhibitory activities of these compounds were evaluated against a panel of hCAs, cancer cell lines, and breast cancer cell lines.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Abdullah A. Elgazar, Ramadan A. El-Domany, Wagdy M. Eldehna, Farid A. Badria
Summary: In this study, new compounds based on AKBA were developed for managing drug-induced liver injury. These compounds exhibited superior anti-inflammatory activity and hepatoprotective potential, and their action mechanisms were explored through molecular docking and network pharmacology analysis.
Article
Chemistry, Medicinal
Tarfah Al-Warhi, Nermeen M. Rashad, Hadia Almahli, Marwa M. Abdel-Aziz, Zainab M. Elsayed, Mai I. Shahin, Wagdy M. Eldehna
Summary: In this study, new benzo[b]thiophene-based hybrids were designed and synthesized as potential candidates for the management of multidrug-resistant/extensively drug-resistant Mycobacterium tuberculosis. The compounds showed promising antimycobacterial activity against drug-sensitive and resistant strains, while having acceptable cytotoxicity.
ARCHIV DER PHARMAZIE
(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)