Article
Chemistry, Medicinal
Prisca Lagardere, Cyril Fersing, Nicolas Masurier, Vincent Lisowski
Summary: This review presents the anti-infective properties of thienopyrimidines and their three isomers. The structure-activity relationship and synthetic pathways of these compounds are analyzed and summarized. Ligand-receptor interactions are also modeled.
Article
Microbiology
Jeremy Ardanuy, Robert Johnson, Carly Dillen, Louis Taylor, Holly Hammond, Stuart Weston, Matthew Frieman
Summary: Pyronaridine triphosphate has demonstrated efficacy in inhibiting SARS-CoV-2 infection and reducing lung inflammation in both cellular and animal models. It can be combined with current COVID-19 treatments to further inhibit viral infections. Pyronaridine represents a promising therapeutic option for COVID-19 and future coronavirus outbreaks.
Review
Biochemistry & Molecular Biology
Afnan, Ammara Saleem, Muhammad Furqan Akhtar, Ali Sharif, Bushra Akhtar, Rida Siddique, Ghulam Md Ashraf, Badrah S. Alghamdi, Saif A. Alharthy
Summary: Phenolic acids are a prevalent class of bioactive chemicals found in plants, with various bioactivities such as anticancer, anti-inflammatory, and cardioprotective effects. Their strong antioxidant properties and modulation of oxidative stress and signal transduction pathways contribute to their therapeutic potential. Further research is needed to fully understand their mechanisms of action and evaluate their efficacy in human disease therapy.
Review
Chemistry, Medicinal
Menna Tallah M. Sayed, Rasha A. A. Hassan, Peter A. A. Halim, Afaf K. K. El-Ansary
Summary: Thienopyrimidine derivatives occupy a special place in fused pyrimidine compounds due to their structural analogs of purines. They have significant biological activities and are widely used in medicinal chemistry. This review discusses various synthetic methods for preparing heterocyclic thienopyrimidine derivatives and highlights recent research on their anticancer effects through enzyme and pathway inhibition in the past 9 years.
MEDICINAL CHEMISTRY RESEARCH
(2023)
Article
Chemistry, Physical
Satyaveni Malasala, Anusha Polomoni, Md. Naiyaz Ahmad, Manjulika Shukla, Grace Kaul, Arunav Dasgupta, Sidharth Chopra, Srinivas Nanduri
Summary: TrmD, a tRNA-(N(1)G37) methyltransferase, is essential for the growth of various bacteria including Staphylococcus aureus, Pseudomonas aeruginosa, Mycobacterium tuberculosis, and Mycobacterium abscessus. In this study, a library of around 200 structurally diverse thienopyrimidines was designed, synthesized, and evaluated for their inhibitory activities against multiple pathogens. Several compounds showed promising inhibitory effects against M. tuberculosis and S. aureus, with compound 18f demonstrating selectivity against the latter. Further studies were conducted to understand the mechanism of action and physico-chemical properties of the selected compounds.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Review
Biochemistry & Molecular Biology
Hesham R. El-Seedi, Nermeen Yosri, Bishoy El-Aarag, Shaymaa H. Mahmoud, Ahmed Zayed, Ming Du, Aamer Saeed, Syed G. Musharraf, Islam M. El-Garawani, Mohamed R. Habib, Haroon Elrasheid Tahir, Momtaz M. Hegab, Xiaobo Zou, Zhiming Guo, Thomas Efferth, Shaden A. M. Khalifa
Summary: Cardiotonic steroids are hormones found in the blood of amphibians and toads, as well as in natural products like plants, herbs, and marines. They have effects against congestive heart failure and atrial fibrillation, and are divided into two groups: cardenolides and bufadienolides. This review focuses on their chemistry, antiviral, and anticancer activities, particularly in combating chronic health problems caused by cancer, viruses, and inflammations. Various cardiotonic steroids from toad venom have been isolated and shown to exhibit superior activities. Identification of these compounds and their bioactivities has been achieved using molecular and biotechnological techniques.
Article
Nanoscience & Nanotechnology
Ning Li, He-Kuan Luo, Adrielle Xianwen Chen, Jeremy Pang Kern Tan, Chuan Yang, Melgious Jin Yan Ang, Huaqiang Zeng, Yi Yan Yang
Summary: This study introduces a novel class of supramolecules with highly potent antimicrobial activities. These supramolecules exhibit high antimicrobial potency against various bacteria and fungus, with negligible toxicity to mammalian cells.
ACS APPLIED MATERIALS & INTERFACES
(2022)
Article
Biochemistry & Molecular Biology
Lukasz Swiatek, Elwira Sieniawska, Kouadio Ibrahime Sinan, Gokhan Zengin, Anastazja Boguszewska, Benita Hryc, Kouadio Bene, Malgorzata Polz-Dacewicz, Stefano Dall'Acqua
Summary: This study investigated the chemical profiles and biological properties of Justicia secunda extracts obtained using different solvents. Over 50 compounds, including flavonoids, phenolic acids, and alkaloids, were identified using LC-MS. The methanol and water extracts showed higher phenolic and flavonoid contents and stronger antioxidant abilities. The dichloromethane and ethyl acetate extracts exhibited greater activity against alpha-amylase and alpha-glucosidase. The aqueous extracts demonstrated selective anticancer properties and the methanolic extract decreased the infectious titer and viral load of human herpesvirus type-1. Overall, J. secunda could be used as a multifunctional bioactive raw material for managing diseases related to oxidative stress.
Review
Biochemistry & Molecular Biology
Panagiotis Zagaliotis, Anthi Petrou, George A. Mystridis, Athina Geronikaki, Ioannis S. Vizirianakis, Thomas J. Walsh
Summary: The development of broad-spectrum antiviral agents is difficult, as the key molecules and pathways differ greatly between viruses. The COVID-19 pandemic has highlighted the limited effectiveness of current antiviral agents. Clinical protocols for COVID-19 treatment currently focus on inhibiting inflammation or the cytopathic effect of the virus. There is a need for expanded oral antiviral agents with dual antiviral and anti-inflammatory activity for early treatment of COVID-19 in high-risk patients.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Celina Osakowicz, Lauren Fletcher, Jeff L. Caswell, Julang Li
Summary: PG-1, an antimicrobial peptide, demonstrates protective effects against pathogen-induced colitis by reducing tissue pathology, preventing weight loss, alleviating clinical symptoms, and enhancing bacterial clearance. Additionally, it modulates the expression of inflammatory mediators to resolve inflammation and restore intestinal homeostasis, with mature PG-1 showing greater efficacy than its pro-form ProPG-1. This study is the first to show the protective effects of PG-1 on infectious colitis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Biochemistry & Molecular Biology
Antonella Di Sotto, Mehdi Valipour, Aala Azari, Silvia Di Giacomo, Hamid Irannejad
Summary: Tylophorine and lycorine, two potential antiviral agents derived from plants, show broad-spectrum antiviral properties and anti-inflammatory effects. They may help combat respiratory viral infections, mitigate the oncogenic effects of viruses, and contribute to cancer research. However, further research is needed to address pharmacologic development issues.
Article
Chemistry, Multidisciplinary
Mujtaba Hussain, Abdul Salam, Muhammad Fahad Arain, Azeem Ullah, Anh-Tuan Dao, Hai Vu-Manh, Duy-Nam Phan, Aamir Shabbir Ansari, Muhammad Qamar Khan, Zafar Javed, Ick-Soo Kim
Summary: Antimicrobial viroblock/polyacrylonitrile nanofiber webs fabricated using the electrospinning method showed promising potential for utilization in anti-viral masks, with 2 wt% VB/PAN nanofibers demonstrating the highest antibacterial properties and excellent cell viability.
APPLIED SCIENCES-BASEL
(2021)
Review
Polymer Science
Muhammad Azeem, Muhammad Hanif, Khalid Mahmood, Nabeela Ameer, Fazal Rahman Sajid Chughtai, Usman Abid
Summary: Flavonoids, such as quercetin, are powerful natural antioxidants and cytotoxic compounds found in many fruits and vegetables. A recent review highlighted the various roles of quercetin in the medical field, including antioxidant, antimicrobial, antidiabetic, anticancerous, and anti-inflammatory effects. The review also discussed the use of quercetin complexes in drug delivery systems and therapeutic interventions.
Review
Chemistry, Medicinal
Javier Avila-Roman, Sara Garcia-Gil, Azahara Rodriguez-Luna, Virginia Motilva, Elena Talero
Summary: Acute inflammation is a key part of the immune system's response, but uncontrolled acute inflammation may lead to chronic inflammation and the development of diseases like cancer. Microalgal carotenoids are considered rich sources of bioactive molecules, with beneficial effects for health, including anti-inflammatory and anticancer activities.
Article
Biochemistry & Molecular Biology
Nesrin Korkmaz, Dursun Kisa, Ozlem Kaplan, Nazan Goksen Tosun, Aykut Ozgur, Rizvan Imamoglu, Ahmet Karadag
Summary: This study investigated the biological activity of the silver coordination compound K-22. The results showed that K-22 has selective inhibitory effects on cancer cell proliferation and also stimulates apoptosis. Additionally, K-22 exhibits antimicrobial activity against various microorganisms and inhibitory potential against the BChE enzyme, which is important in Alzheimer's disease progression. Overall, K-22 shows strong potential for medical use due to its anticancer, antibacterial, antifungal, and anti-Alzheimer properties.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Biochemistry & Molecular Biology
Eslam M. H. Ali, Mohammed S. Abdel-Maksoud, Rasha Mohamed Hassan, Karim I. Mersal, Usama M. Ammar, Choi Se-In, Han He-Soo, Hee-Kwon Kim, Anna Lee, Kyung-Tae Lee, Chang-Hyun Oh
Summary: In this study, drug repurposing strategies were used to reposition a series of inhibitors to target P38α kinase, leading to the identification of compounds with anti-inflammatory activity by effectively inhibiting the production of inflammatory cytokines. The most potent inhibitor, compound 11d, exhibited satisfactory inhibitory activity against the production of PGE2 and NO in LPS-stimulated macrophages.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Eslam M. H. Ali, Rania Farag A. El-Telbany, Mohammed S. Abdel-Maksoud, Usama M. Ammar, Karim Mersal, Seyed-Omar Zaraei, Mohammed El-Gamal, Se-In Choi, Kyung-Tae Lee, Hee-Kwon Kim, Kwan Hyi Lee, Chang-Hyun Oh
Summary: The newly synthesized (imidazol-5-yl)pyrimidine compounds exhibited dual inhibitory activity against BRAF(V600E) and p38 alpha kinases, as well as antiproliferative and TNF-alpha inhibitory activities. Compound 20h showed the highest inhibitory activity among the tested compounds.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Mohammed S. Abdel-Maksoud, Mohammed El-Gamal, Bong S. Lee, Mahmoud M. Gamal El-Din, Hong R. Jeon, Dow Kwon, Usama M. Ammar, Karim Mersal, Eslam M. H. Ali, Kyung-Tae Lee, Kyung Ho Yoo, Dong Keun Han, Jae Kyun Lee, Garam Kim, Hong Seok Choi, Young Jik Kwon, Kwan Hyi Lee, Chang Hyun Oh
Summary: In this study, a series of new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives with a terminal sulfonamide moiety were synthesized and their pan-RAF inhibitory effect was investigated. Compounds 27c and 38a showed the highest antiproliferative activity against cancer cells and were able to inhibit phosphorylation of MEK and ERK. Compound 38a was further tested for its in vivo activity against melanoma, and both cellular and animal activities were reported.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Karim I. Mersal, Mohammed S. Abdel-Maksoud, Eslam M. H. Ali, Usama M. Ammar, Seyed-Omar Zaraei, Jae-Min Kim, Su-Yeon Kim, Kyung-Tae Lee, Kwan Hyi Lee, Si-Won Kim, Hyun-Mee Park, Mi-Jung Ji, Chang-Hyun Oh
Summary: In this study, a new series of compounds were designed and synthesized with potential cytotoxic and anti-inflammatory effects. Compounds 8d and 9k showed the highest inhibitory effect on NO production, PGE(2) inhibition, and cytokines inhibition. Additionally, compounds 8d and 9k exhibited high binding affinity to the COX-2 active site, similar to the native ligand celecoxib.
MEDICINAL CHEMISTRY RESEARCH
(2021)
Article
Chemistry, Medicinal
Rasha M. Hassan, Islam H. Ali, Mohammed S. Abdel-Maksoud, Heba M. I. Abdallah, Ahmed M. El Kerdawy, Francesca Sciandra, Iman A. Y. Ghannam
Summary: Compound 9q demonstrated potent antihyperlipidemic and antioxidant activities, lowering blood lipid levels and enhancing antioxidant capacity, with improvements in aortic architecture and hepatic steatosis.
ARCHIV DER PHARMAZIE
(2022)
Article
Biochemistry & Molecular Biology
Mohammed S. Abdel-Maksoud, Rasha Mohamed Hassan, Aida Abdel-Sattar El-Azzouny, Mohamed Nabil Aboul-Enein, Chang-Hyun Oh
Summary: In this study, a novel series of anticancer and anti-inflammatory compounds were designed and synthesized, with compound 11c showing the highest anticancer activity and compound 11n demonstrating the most potent anti-inflammatory effects. These compounds were further analyzed for their biological targets and structure-activity relationships, indicating potential clinical applications.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Seyed-Omar Zaraei, Rawan M. Sbenati, Nour N. Alach, Hanan S. Anbar, Randa El-Gamal, Hamadeh Tarazi, Mahmoud K. Shehata, Mohammed S. Abdel-Maksoud, Chang-Hyun Oh, Mohammed El-Gamal
Summary: This article reports on novel imidazothiazole derivatives as first-in-class potent and selective ErbB4 (HER4) inhibitors. The compounds showed promising antiproliferative activity with high selectivity towards cancer cell lines, indicating potential therapeutic value.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Mohammed S. Abdel-Maksoud, Ahmed A. B. Mohamed, Rasha M. Hassan, Mohamed A. Abdelgawad, Garri Chilingaryan, Samy Selim, Mohamed S. Abdel-Bakky, Mohammad M. Al-Sanea
Summary: A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives were designed and synthesized based on established V600EBRAF inhibitors. Among them, 12e, 12i, and 12l showed the strongest inhibitory activity against V600EBRAF, with 12l having the lowest IC50 of 0.49 μM. Further studies revealed that 12e exhibited significant growth inhibition against multiple cancer cell lines and warrants further investigation into its effect on cell cycle progression. Additionally, virtual docking studies provided insights into the binding modes of vemurafenib and the synthesized compounds.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Eslam M. H. Ali, Karim Mersal, Usama M. Ammar, Seyed-Omar Zaraei, Mohammed S. Abdel-Maksoud, Mohammed El-Gamal, Md Mamunul Haque, Tanuza Das, Eunice EunKyeong Kim, Jun-Seok Lee, Kwan Hyi Lee, Hee-Kwon Kim, Chang-Hyun Oh
Summary: In this article, a new series of 4-(imidazol-5-yl)pyridines with improved anticancer activity and selective B-RAF(V600E)/p38 alpha kinase inhibitory activity was designed and evaluated. Compound 10c exhibited the highest potency among the tested compounds, with nano-molar activity against most cancer cell lines and incredible activity against melanoma. It also induced cell cycle arrest, apoptosis, and autophagy in multiple cancer cell lines.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Infectious Diseases
Ruqaiyyah Siddiqui, Mohammed El-Gamal, Anania Boghossian, Balsam Qubais Saeed, Chang-Hyun Oh, Mohammed S. Abdel-Maksoud, Ahmad M. Alharbi, Hasan Alfahemi, Naveed Ahmed Khan
Summary: The synthesized compounds exhibited significant anti-amoebic effects against brain-eating amoebae, showing promise as effective treatments for these infections.
Article
Infectious Diseases
Noor Akbar, Mohammed El-Gamal, Balsam Qubais Saeed, Chang-Hyun Oh, Mohammed S. Abdel-Maksoud, Naveed Ahmed Khan, Ahmad M. Alharbi, Hasan Alfahemi, Ruqaiyyah Siddiqui
Summary: This study found that compounds 1m and 1zb exhibited excellent anti-amoebic effects against Acanthamoeba. These compounds significantly inhibited the proliferation of Acanthamoeba trophozoites and blocked the encystation and excystation processes. They also showed minimal cytotoxic effects on host cells and reduced amoeba-mediated host cell death.
Article
Chemistry, Medicinal
Afnan Shahin, Seyed-Omar Zaraei, Bilal O. AlKubaisi, Saif Ullah, Hanan S. Anbar, Randa El-Gamal, Varsha Menon, Mohammed S. Abdel-Maksoud, Chang-Hyun Oh, Raafat El-Awady, Nicolly Espindola Gelsleichter, Julie Pelletier, Jean Sevigny, Jamshed Iqbal, Taleb H. Al-Tel, Mohammed El-Gamal
Summary: A series of adamantyl carboxamide derivatives containing sulfonate or sulfonamide moiety were designed and evaluated for their antiproliferative activity against NCI-60 cancer cell lines panel. Compounds 1e and 1i exhibited potent and broad-spectrum inhibition against multiple cancer subtypes while showing safety towards normal cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Mohammed Farrag El-Behairy, Walaa Hamada Abd-Allah, Mohamed M. M. Khalifa, Mohamed S. S. Nafie, Mohamed A. A. Saleh, Mohammed S. S. Abdel-Maksoud, Tarfah Al-Warhi, Wagdy M. M. Eldehna, Ahmed A. A. Al-Karmalawy
Summary: Based on the rigidification principle and doxorubicin's pharmacophoric features, two novel series of dibenzo[b,f]azepines (14 candidates) were designed and synthesised. The anti-proliferative activity and topoisomerase II inhibition ability of the promising candidates (5a-g) were evaluated, with 5e identified as the most active congener. Moreover, 5e exhibited cytotoxicity against leukaemia SR cells, arrested the cell cycle at the G1 phase, increased apoptosis ratio, and showed inhibition of tumor proliferation and volume decrease in in vivo studies.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Ahmed Elkamhawy, Eslam M. H. Ali, Kyeong Lee
Summary: Lymphocyte-specific protein tyrosine kinase (Lck), a non-receptor Src family kinase, plays a crucial role in regulating cellular processes and T-cell functions. Alterations in Lck expression and activity can lead to various diseases, prompting research efforts to develop new Lck inhibitors and explore their binding modes within the active site of Lck for potential therapeutic applications.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)