Article
Chemistry, Medicinal
Khaled El-Adl, Helmy Sakr, Sanadelaslam S. A. El-Hddad, Abdel-Ghany A. El-Helby, Mohamed Nasser, Hamada S. Abulkhair
Summary: The study evaluated the anticancer activity of novel thiazolidine-2,4-diones against several cancer cell lines, with some derivatives showing high inhibitory effects on HCT-116, HepG2, and MCF-7 cells. Some derivatives also displayed potential inhibitory effects against VEGFR-2. These compounds demonstrated promising characteristics as potential anticancer drug candidates.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Medicinal
Khaled El-Adl, Abdel-Ghany A. El-Helby, Helmy Sakr, Rezk R. Ayyad, Hazem A. Mahdy, Mohamed Nasser, Hamada S. Abulkhair, Sanadelaslam S. A. El-Hddad
Summary: The study found that compounds 18, 12, 17, and 16 have strong anticancer activity against HepG2, HCT116, and MCF-7 cancer cells, with MCF-7 being the most sensitive to these new derivatives; the inhibitory activity of these compounds is comparable to classic anticancer drugs such as doxorubicin and sorafenib.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Multidisciplinary
Hazem Elkady, Osama A. El-Dardir, Alaa Elwan, Mohammed S. Taghour, Hazem A. Mahdy, Mohammed A. Dahab, Eslam B. Elkaeed, Bshra A. Alsfouk, Ibrahim M. Ibrahim, Dalal Z. Husein, Elsayed E. Hafez, Amira M. G. Darwish, Ahmed M. Metwaly, Ibrahim H. Eissa
Summary: In this study, novel VEGFR-2-targeting thiazolidine-2,4-dione derivatives were designed and synthesized. The compounds demonstrated potent anti-VEGFR-2 activity and inhibited the growth of three different cancer cell types. Compound 15 showed the best anti-VEGFR-2 potency and exhibited remarkable anti-proliferative activities against the tested cancer cell lines. Computational methods were used to analyze the molecular characteristics of the VEGFR-2-15 complex, and ADMET and toxicity experiments were conducted to evaluate the therapeutic potential of the synthesized compounds. The findings suggest that compound 15 may serve as an effective anticancer lead compound.
Article
Chemistry, Medicinal
Mohamed A. Abdelgawad, Khaled El-Adl, Sanadelaslam S. A. El-Hddad, Mostafa M. Elhady, Nashwa M. Saleh, Mohamed M. Khalifa, Fathalla Khedr, Mohamed Alswah, AbdElAziz A. Nayl, Mohammed M. Ghoneim, Nour E. A. Abd El-Sattar
Summary: Newly designed thiazolidine-2,4-dione derivatives were synthesized and evaluated for their anticancer activities. Some of the derivatives exhibited potent activities against HepG2 tumor cells. Additionally, these derivatives showed inhibitory effects on VEGFR-2 and had varying affinities and insulin-secreting activities towards PPAR gamma.
Article
Chemistry, Medicinal
Noura S. Hanafy, Nada A. A. M. Aziz, Sanadelaslam S. A. El-Hddad, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Amal F. Dawood, Samy Mohamady, Khaled El-Adl, Sahar Ahmed
Summary: Novel thiazolidine-2,4-diones were developed and evaluated as dual inhibitors of EGFR(T790M) and VEGFR-2 against multiple cancer cell lines. Compounds 6a, 6b, and 6c demonstrated significant activity against HCT116, MCF-7, A549, and HepG2 cells. Although not as potent as sorafenib, they exhibited higher efficacy than erlotinib. These compounds also showed promising effects on VEGFR-2 and EGFR(T790M), with 6b and 6c being the most effective derivatives. Additionally, compounds 6a, 6b, and 6c exhibited favorable in silico computed ADMET profiles.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Asmaa M. Sayed, Fatma A. Taher, Mohammad R. K. Abdel-Samad, Mohamed S. A. El-Gaby, Khaled El-Adl, Nashwa M. Saleh
Summary: A novel series of sulfonamide derivatives containing hydrazone were synthesized and evaluated for their anticancer activities. Some compounds showed high sensitivity in HepG2 cells and good inhibitory activity against VEGFR-2.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Khaled El-Adl, Mohamed K. Ibrahim, Fathalla Khedr, Hamada S. Abulkhair, Ibrahim H. Eissa
Summary: The study designed and synthesized 20 new N-substituted-4-phenylphthalazin-1-amine derivatives, among which compound 7f showed the most potent anticancer and anti-angiogenesis activities with IC50 values significantly lower than existing drugs. Other compounds also exhibited good inhibitory activity.
ARCHIV DER PHARMAZIE
(2022)
Article
Biochemistry & Molecular Biology
Musherah M. Alshammari, Raoudha Soury, Khalaf M. Alenezi, Md. Mushtque, M. Moshahid Alam Rizvi, Ashanul Haque
Summary: A new pyrazole-tethered thiazolidine-2,4-dione derivative was synthesized and its structure was confirmed by spectroscopic techniques. Density functional theory calculations were used to determine the molecular features. In vitro cytotoxicity studies showed higher activity and lower toxicity of the compound against breast cancer cell line.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Medicinal
Nashwa M. Saleh, Adel A-H Abdel-Rahman, Asmaa M. Omar, Mohamed M. Khalifa, Khaled El-Adl
Summary: Novel pyridine-derived compounds were synthesized and evaluated for their anticancer activities targeting the VEGFR-2 enzyme. Compounds 10, 9, 8, and 15 showed potent inhibitory effects on HepG2 and MCF-7 cells, with compound 10 exhibiting higher activity than the standard drugs sorafenib and doxorubicin.
ARCHIV DER PHARMAZIE
(2021)
Article
Biochemistry & Molecular Biology
Mohamed H. Hekal, Paula S. Farag, Magdy M. Hemdan, Wael M. El-Sayed
Summary: This study synthesized a series of N-(1,3,4-thiadiazol-2yl)furan-2-carboxamide derivatives and found higher yields and rates under microwave conditions compared to traditional methods. The antiproliferative activities of these compounds were assessed, showing promising results against three cancer cell lines and VEGFR-2 as a potential molecular target. Some compounds exhibited significant antiproliferative activity, with Compound 7 identified as the best inhibitor of VEGFR-2.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Musherah M. Alshammari, Raoudha Soury, Khalaf M. Alenezi, Md Mushtque, M. Moshahid Alam Rizvi, Ashanul Haque
Summary: A new pyrazole-tethered thiazolidine-2,4-dione derivative was synthesized and displayed higher activity and lower toxicity towards breast cancer cell line compared to its intermediate compound. The study also involved spectroscopic confirmation, theoretical calculations, in vitro cytotoxicity testing, and complementary docking and ADME studies.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Chemistry, Medicinal
Khaled El-Adl, Mohamed-Kamal Ibrahim, Fathalla Khedr, Hamada S. Abulkhair, Ibrahim H. Eissa
Summary: A series of novel VEGFR-2 inhibitors were designed, synthesized, and evaluated for their anticancer activities against various cancer cell lines. Among them, compound 7a showed the most potent anticancer and VEGFR-2 inhibitory effects, demonstrating promising potential for further development in cancer therapy. The results of cytotoxicity studies and inhibitory activities against VEGFR-2 were consistent with molecular modeling studies, indicating the efficacy and mechanism of action of the synthesized compounds.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Medicinal
Nada A. A. M. Aziz, Riham F. F. George, Khaled El-Adl, Walaa R. R. Mahmoud
Summary: In this study, 22 innovative thiazolidine-2,4-dione compounds were designed and evaluated for their anticancer activity against four human neoplasms. The results showed that compounds 14a and 14g exhibited the most active anticancer performance. Additionally, these compounds showed good inhibitory activity against VEGFR-2 and EGFR(T790M).
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Multidisciplinary
Meenakshi Duhan, Rahul Singh, Meena Devi, Jayant Sindhu, Parvin Kumar, Sudhir Kumar, Ramesh Kataria, Ashwani Kumar, Sohan Lal, Devender Singh
Summary: A series of 2,4-thiazolidinedione fused spiropyrrolidineoxindole and 1,2,3-triazole scaffolds were designed and synthesized for α-amylase inhibition. Compound 9b showed the highest inhibition with 88.05 +/- 2.51%, 76.65 +/- 2.19%, and 68.57 +/- 1.96% inhibition at 50, 25, and 12.5 mg mL(-1), respectively. Molecular docking and dynamic simulations confirmed the stability of the ligand-protein complexes.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Nawaf A. Alsaif, Mohammed A. Dahab, Mohammed M. Alanazi, Ahmad J. Obaidullah, Abdulrahman A. Al-Mehizia, Manal M. Alanazi, Saleh Aldawas, Hazem A. Mahdy, Hazem Elkady
Summary: A new series of [1,2,4]triazolo[4,3-a]quinoxalin-4(5H)-one and [1,2,4]triazolo[4,3-a]quinoxaline derivatives were designed, synthesized, and evaluated for their anti-proliferative activities against MCF-7 and HepG2 tumor cell lines. Compounds 25d, 25e, 25i, and 27e showed the highest activities against the cell lines, while also exhibiting potent VEGFR-2 inhibitory effects. Compound 25d was found to induce apoptosis in HepG2 cells and arrest their growth at the G2/M phase, with significant increases in apoptotic markers observed.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Eslam B. Elkaeed, Reda G. Yousef, Hazem Elkady, Ahmed B. M. Mehany, Bshra A. Alsfouk, Dalal Z. Husein, Ibrahim M. Ibrahim, Ahmed M. Metwaly, Ibrahim H. Eissa
Summary: A new naphthalene analog (compound 7) designed and synthesized demonstrated high inhibitory potential against VEGFR-2, with proper binding and energy compared to sorafenib in molecular docking studies. Various experiments confirmed the accurate interaction of compound 7 with VEGFR-2 and its drug-likeness.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Multidisciplinary Sciences
Ahmed A. Gaber, Mohamed Sobhy, Abdallah Turky, Wagdy M. Eldehna, Samiha A. El-Sebaey, Souad A. El-Metwally, Abeer M. El-Naggar, Ibrahim M. Ibrahim, Eslam B. Elkaeed, Ahmed M. Metwaly, Ibrahim H. Eissa
Summary: Fifteen derivatives of quinazoline were synthesized as DNA intercalators, and their cytotoxicity against HCT-116 and HepG2 cancer cell lines as well as their inhibitory effect on Topo II were evaluated. Compound 16 exhibited the highest cytotoxicity and Topo II inhibition, but had low cytotoxicity against Vero cells. Compounds 16, 17, and 18 showed significant DNA binding affinities. Compound 16 also displayed Topo II catalytic inhibitory effect at a concentration of 10 mu M. Further investigations revealed that compound 16 induced apoptosis in HCT-116 cells and arrested growth at the S and G2/M phases, accompanied by increased BAX level and decreased Bcl-2 level compared to control cells. In silico studies demonstrated the ability of the synthesized derivatives to bind to the DNA-Topo II complex.
Article
Immunology
Sara Shokry, Akram Hegazy, Ahmad M. Abbas, Islam Mostafa, Ibrahim H. Eissa, Ahmed M. Metwaly, Galal Yahya, Assem M. El-Shazly, Khaled M. Aboshanab, Ahmed Mostafa
Summary: This study investigated the anti-influenza activity of various plant-derived phytochemicals against highly pathogenic avian influenza A/H5N1 virus and seasonal low pathogenic human influenza A/H1N1 virus. Among 22 tested phytochemicals, the steroid compounds beta-sitosterol and beta-sitosterol-O-glucoside showed potent activity against the predefined influenza viruses. These steroids could affect multiple stages of the influenza virus replication cycle and have a significant viricidal effect.
Article
Biology
Ibrahim H. Eissa, Reda G. Yousef, Hazem Elkady, Aisha A. Alsfouk, Bshra A. Alsfouk, Dalal Z. Husein, Ibrahim M. Ibrahim, Eslam B. Elkaeed, Ahmed M. Metwaly
Summary: A new lead compound, T-1-PCPA, was designed as an antiangiogenic EGFR inhibitor that can bind with the catalytic pocket of EGFR protein. Through computational studies and experimental validation, it was confirmed that T-1-PCPA has a high level of reactivity and inhibitory effect on EGFR. T-1-PCPA showed potent inhibition against EGFR(WT) and malignant cell lines A549 and HCT-116, with comparable or better efficacy than erlotinib.
Article
Biology
Souad A. El-Metwally, Abdelrahman A. Abuelkhir, Hazem Elkady, Mohammed S. Taghour, Ibrahim M. Ibrahim, Dalal Z. Husein, Aisha A. Alsfouk, Ahlam Sultan, Ahmed Ismail, Samy Y. Elkhawaga, Eslam B. Elkaeed, Ahmed M. Metwaly, Ibrahim H. Eissa
Summary: New thieno[2,3-d]pyrimidine derivatives were designed, synthesized, and investigated for their potential anticancer activity by inhibiting the VEGFR-2 receptor. These derivatives showed strong in vitro abilities to inhibit VEGFR-2 and prevent cancer cell growth in MCF-7 and HepG2 cells. Compound 22 exhibited the most potent anti-VEGFR-2 activity with an IC50 value of 0.58μM and also showed good anti-proliferative activity against both cancer cell lines.
COMPUTATIONAL BIOLOGY AND CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Omnia R. Elbatrawy, Moshira A. El Deeb, Mohamed Hagras, Fatimah Agili, Maghawry Hegazy, Ahmed A. El-Husseiny, Mohamed A. Elkady, Ibrahim H. Eissa, Samar El-Kalyoubi
Summary: The study presents new active HDAC inhibitors through the design and synthesis of 16 thiouracil derivatives with deep biological and computational investigation. Compounds 7a, 7c, 7d, 7e, 8a and 8f showed the highest antiproliferative effects against MCF7, HepG2 and HCT116 cell lines. Compound 7e exhibited the highest activities against HDAC1 and HDAC4, and arrested the cell cycle of HCT116 cells at G0-G1 with significant apoptotic effect. The docking studies provided insights into the binding patterns of the synthesized compounds against HDAC1.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Eman A. Sobh, Mohammed A. Dahab, Eslam B. Elkaeed, Aisha A. Alsfouk, Ibrahim M. Ibrahim, Ahmed M. Metwaly, Ibrahim H. Eissa
Summary: This study aimed to discover new thieno[2,3-d]pyrimidine derivatives as EGFR tyrosine kinase inhibitors. Nine derivatives were designed, synthesized, and evaluated in vitro and in silico. Compound 7a showed significant inhibitory effects against both EGFR wild-type and EGFR(T790M), inducing apoptosis and arresting cell growth. Docking and molecular dynamics simulation confirmed the stable binding modes of the synthesized compounds. Compound 7a is a promising dual EGFR inhibitor for cancer treatment.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Hazem A. Mahdy, Hazem Elkady, Mohammed S. Taghour, Alaa Elwan, Mohammed A. Dahab, Mohamed A. Elkady, Elsayed G. E. Elsakka, Eslam B. Elkaeed, Bshra A. Alsfouk, Ibrahim M. Ibrahim, Ibrahim H. Eissa, Ahmed M. Metwaly
Summary: This study aimed to design and semi-synthesize new theobromine derivatives as potential VEGFR-2 inhibitors, and evaluate the synthesized compounds in vitro and in silico. The results showed that compound 5b exhibited excellent antiproliferative and VEGFR-2 inhibitory effects, with significant apoptotic activity. It modulated the immune response by increasing IL-2 and reducing TNF-α levels. Docking and molecular dynamics simulations revealed the compound's binding affinity with VEGFR-2. Furthermore, computational ADMET studies indicated the high potential of compound 5b for drug development.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Ashish K. Patel, Ujashkumar A. Shah, Jigar Y. Soni, Ahmed M. Metwaly, Eslam B. Elkaeed, Ibrahim H. Eissa, Divya M. Teli, Purvesh R. Patel, Bhavin H. Patel, Nikunj Valand, Manish B. Patel
Summary: A series of thiophene compounds were designed as potential EGFR inhibitors. The compound AP-A15 showed stable binding with EGFR and exhibited potent anticancer activity against MCF-7 cell line.
Article
Chemistry, Medicinal
Faez Ahmmed, Samiah Hamad Al-Mijalli, Emad M. Abdallah, Ibrahim H. Eissa, Ferdausi Ali, Ajmal R. Bhat, Joazaizulfazli Jamalis, Taibi Ben Hadda, Sarkar M. A. Kawsar
Summary: This study synthesized a series of galactoside-based molecules and evaluated their antimicrobial and antifungal activities. The synthesized analogs exhibited varying levels of antibacterial activity against different bacteria and showed potential as new antibacterial and antifungal agents with low cytotoxicity.
Article
Chemistry, Medicinal
Omnia R. R. Elbatrawy, Mohamed Hagras, Moshira A. A. El Deeb, Fatimah Agili, Maghawry Hegazy, Ahmed A. A. El-Husseiny, Mahmoud Mohamed Mokhtar, Samy Y. Y. Elkhawaga, Ibrahim H. H. Eissa, Samar El-Kalyoubi
Summary: In this study, new uracil and thiouracil derivatives were synthesized as HDAC inhibitors. Compound 5m showed promising cytotoxic and HDAC inhibitory activities, and had significant effects on cell cycle and apoptosis.
Article
Chemistry, Multidisciplinary
Ibrahim H. H. Eissa, Reda G. G. Yousef, Hazem Elkady, Eslam B. B. Elkaeed, Aisha A. A. Alsfouk, Dalal Z. Z. Husein, Ibrahim M. M. Ibrahim, Mostafa A. A. Elhendawy, Murrell Godfrey, Ahmed M. M. Metwaly
Summary: This study aimed to design theobromine derivatives that can inhibit VEGFR-2, a protein involved in cancer progression. The new compounds were tested in vitro against two cancer cell lines, MCF-7 and HepG2, and compound 15a showed the highest effectiveness. 15a demonstrated potent VEGFR-2 inhibitory activity and induced apoptosis in HepG2 cells, making it a promising lead compound for the development of a novel anticancer agent.
Article
Chemistry, Multidisciplinary
Abdulrahman M. Saleh, Hazem A. Mahdy, Mohamed Ayman El-Zahabi, Ahmed B. M. Mehany, Mohamed M. Khalifa, Ibrahim H. Eissa
Summary: A series of pyrimidine-5-carbonitrile derivatives with benzylidene and hydrazone moieties were synthesized as potential inhibitors of VEGFR-2. The synthesized compounds exhibited higher cytotoxic activities than sorafenib against colon cancer and breast cancer cell lines. Compound 11e showed excellent activities against both cell lines and had lower cytotoxicity against normal human fibroblast cells. Moreover, compound 11e was the most potent VEGFR-2 inhibitor and exhibited anticancer effects through cell cycle arrest, apoptosis induction, and modulation of cytokine levels. The molecular docking study revealed similar binding modes to sorafenib, and molecular dynamics simulations confirmed the stability of compound 11e in the active site.
Article
Chemistry, Multidisciplinary
Anas Ramadan Kotb, Abdallah E. Abdallah, Hazem Elkady, Ibrahim H. Eissa, Mohammed S. Taghour, Dina Abed Bakhotmah, Tamer M. Abdelghany, Mohamed Ayman El-Zahabi
Summary: A series of thalidomide analogs were synthesized as potential antitumor immunomodulatory agents, showing significant antiproliferative activities against three human cancer cell lines. These compounds were found to reduce the expression levels of proinflammatory cytokines and showed comparable efficacy to thalidomide.
Article
Chemistry, Multidisciplinary
Marwa Alsulaimany, Khaled El-Adl, Ahmed K. B. Aljohani, Hussam Y. Alharbi, Omar M. Alatawi, Majed S. Aljohani, Ahmed El-morsy, Sara A. Almadani, Abdulrahman A. Alsimaree, Samir A. Salama, Doaa E. Keshek, Abeer A. Mohamed
Summary: Fifteen new 1-alkyl-6-iodoquinazoline derivatives were designed and synthesized, and their anticancer activities were evaluated against multiple cancer cell lines. Compound 9c showed the highest activity and exhibited excellent dual inhibition of EGFR and VEGFR-2.
Correction
Biochemistry & Molecular Biology
Mohamed Marzouk, Shimaa M. Khalifa, Amal H. Ahmed, Ahmed M. Metwaly, Hala Sh. Mohammed, Hanan A. A. Taie
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Gerardo Andres Libreros-Zuniga, Danilo Pava e Pavao, Vinicius de Morais Barroso, Nathalya Cristina de Moraes Roso Mesquita, Saulo Fehelberg Pinto Braga, Glaucius Oliva, Rafaela Salgado Ferreira, Kelly Ishida, Marcio Vinicius Bertacine Dias
Summary: Tuberculosis is a major global cause of death, and the emergence of drug-resistant strains has increased the burden of this disease. New alternative therapies are constantly needed, and recent research has identified small molecules as potential inhibitors of Ldts in M. tuberculosis, which have antimycobacterial activity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xiao-Dong Wang, Yong-Si Liu, Ming-Hao Hu
Summary: In this study, a selffolded fluorescent probe was designed to selectively illuminate G4s by unfolding its intramolecular aggregation mediated by G4 binding. This probe showed more controllable background emission and promising ability to track G4 forming dynamics compared to previous disaggregation-induced emission (DIE) probes.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Xiang, Zhuo Yuan, Qichuan Deng, Linshen Xie, Dongke Yu, Jianyou Shi
Summary: This review provides a brief description of the diagnosis, pathogenesis, and potential therapeutic inhibitors for renal fibrosis. Currently, there are no clear therapeutic targets or drugs for renal fibrosis; however, some natural products may have potential efficacy for treating renal fibrosis.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Anna Nikitjuka, Bruna Rafaela Pereira Resende, Michael Smietana, Alessio Nocentini, Claudiu T. Supuran, Jean-Yves Winum
Summary: Boron-based compounds have been extensively studied in medicinal chemistry, playing a crucial role in designing small molecule drugs for various diseases. Boron is particularly valuable in developing inhibitors for metalloenzymes carbonic anhydrases, and it can modulate ligand recognition ability and selectivity. Recent advancements have led to the discovery of novel boron-based inhibitors that can inhibit carbonic anhydrases through a Lewis acid-base mechanism. Further research is needed to fully explore the potential of boron-based inhibitors and advance their clinical applications.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xinxin Liu, Lei Chen, Ze Chen
Summary: This study developed a nanostructured photosensitizer loaded with oxygen-throttling drug and demonstrated its enhanced cytotoxicity against tumor cells under hypoxic conditions. Animal experiments showed the enhanced tumor targeting capability of the photosensitizer and its inhibitory effect on tumor growth.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Shuai Jiang, Wen-Yan Li, Zai-Feng Yuan, Qin-Shi Zhao
Summary: This study isolated two new dimeric Lycopodium alkaloids and twelve previously undescribed Lycopodium alkaloids from Lycopodiastrum casuarinoides. The structures of these compounds were determined and their inhibitory activities on the Cav3.1 channel were evaluated.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yan Yang, Dong-Xiao Yan, Rui-Xue Rong, Bing-Ye Shi, Man Zhang, Jing Liu, Jie Xin, Tao Xu, Wen-Jie Ma, Xiao-Liu Li, Ke-Rang Wang
Summary: In this study, a series of nucleolar fluorescent probes based on naphthalimide derivatives were designed and synthesized, which could achieve clear nucleolar staining in living cells. The results showed that these probes exhibited good targeting to the cell nucleolus and could bind to RNA and enhance fluorescence. This has positive implications for the diagnosis and treatment of nucleolus-related diseases.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yongxi Dong, Fang Wang, Jinlan Wen, Yongqing Mao, Shanhui Zhang, Tiemei Long, Zhangxiang Yang, Lei Li, Jiquan Zhang, Li Dong, Gang Liu, Jianwei Xu
Summary: The hybrid molecules of Scutellarein and Tertramethylpyrazine show excellent neuroprotective and antiplatelet effects in the treatment of ischemic stroke. Compound 1e is particularly effective, enhancing cell membrane permeability and inhibiting cell uptake, as well as significantly reducing cerebral infarction volume.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Chen, Yuanyuan Ying, Jonathan Lalsiamthara, Yuheng Zhao, Saber Imani, Xin Li, Sijing Liu, Qingjing Wang
Summary: This paper examines the role and metabolic regulation of NAD+ in bacteria, highlighting its impact on physiology and virulence. It explores enzymes associated with NAD+ metabolism as potential targets for antibacterial drugs and vaccine candidates. Additionally, it scrutinizes the medical potential of NAD+ and provides insights for its application in biomedicine.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Jon Macicior, Daniel Fernandez, Silvia Ortega-Gutierrez
Summary: Hutchinson-Gilford progeria syndrome (HGPS), also known as progeria, is a rare genetic disease that causes premature aging and significantly reduces life expectancy. Currently, there is only one approved drug for treating progeria, but its efficacy is limited. Progerin levels are believed to be the most important biomarker related to disease severity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Fuko Hirano, Naoya Kondo, Yusuke Murata, Aya Sudani, Takashi Temma
Summary: Fluorinated alpha-methyl 3BPA derivatives showed improved water solubility, tumor targetability, and biodistribution compared to 3BPA and BPA, resulting in significantly improved tumor-to-normal tissue ratios.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Ying Shi, Jiaqin Tang, Shumeng Zhi, Ruiqi Jiang, Qing Huang, Lei Sun, Zhizhong Wang, Yanran Wu
Summary: Necroptosis is a type of cell death associated with various diseases. In this study, we identified a small molecule inhibitor, SY-1, that effectively blocks necroptosis by inhibiting the phosphorylation of RIP1/RIP3/MLKL pathway. SY-1 also showed protective effects against TNF-induced hypothermia and improved survival in mice with SIRS. These findings highlight the potential therapeutic applications of SY-1.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Andrea Bagan, Sonia Abas, Judith Pala-Pujadas, Alba Irisarri, Christian Grinan-Ferre, Merce Pallas, Itziar Muneta-Arrate, Carolina Muguruza, Luis F. Callado, Belen Perez, Elies Molins, Jose A. Morales-Garcia, Carmen Escolano
Summary: Recent studies have identified the modulation of imidazoline I-2 receptors (I-2-IR) by selective ligands as a potential strategy for treating neurodegenerative diseases. This study reports a family of bicyclic alpha-iminophosphonates that show high affinity and selectivity for I-2-IR and demonstrates their neuroprotective and anti-inflammatory effects in in vitro and in vivo models. The findings emphasize the importance of exploring structurally novel I-2-IR ligands for therapeutic strategies in neurodegeneration.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Qiuping Xiang, Tianbang Wu, Cheng Zhang, Chao Wang, Hongrui Xu, Qingqing Hu, Jiankang Hu, Guolong Luo, Xiaoxi Zhuang, Xishan Wu, Yan Zhang, Yong Xu
Summary: This study reports the discovery of a 1-(indolizin-3-yl)ethan-1-one derivative as a potent and selective CBP bromodomain inhibitor for AML drug development.
BIOORGANIC CHEMISTRY
(2024)
