Article
Biochemistry & Molecular Biology
Eman K. A. Abdelall, Lamees S. Aboelnaga, Randa M. Hassan, Phoebe F. Lamie
Summary: Novel chalcone 3a-c, pyrazoline 4a-i and pyridine 5a-c, 6a & b derivatives bearing methanesulfonamide moiety were synthesized and their structures were confirmed. In vitro and in vivo studies showed their COX-1/COX-2 inhibitory and anti-inflammatory activities. Histopathological and histochemical studies revealed the safety of the most active anti-inflammatory derivatives 4f-4i, especially 4h derivative, on gastric mucosa. Docking studies and physicochemical property predictions indicated good oral bio-availability for compounds 4f-i and 6b.
BIOORGANIC CHEMISTRY
(2023)
Review
Chemistry, Organic
Rajnish Kumar, Himanshu Singh, Avijit Mazumder, Salahuddin, Ranjeet Kumar Yadav
Summary: The pyrazoline moiety is widely used in pharmaceutical, agricultural, and industrial sectors, and its chemistry has been extensively studied. Various synthesis strategies have been developed, but researchers are continuously exploring greener and more economical methods.
CURRENT ORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Ioanna Kostopoulou, Antonia Diassakou, Eleni Kavetsou, Eftichia Kritsi, Panagiotis Zoumpoulakis, Eleni Pontiki, Dimitra Hadjipavlou-Litina, Anastasia Detsi
Summary: This study investigates the structure-activity relationship of quinolinone-chalcone and quinolinone-pyrazoline hybrids to discover potential antioxidant and anti-inflammatory agents. Four bioactive quinolinone-chalcone compounds were synthesized and chemically modified into fifteen new pyrazoline analogues. Among them, compounds 9b and 9m showed the best combined activity, with 9b exhibiting the most potent LOX inhibitory activity. Docking results revealed that pyrazoline analogue 9b had a high AutoDock Vina score and all tested derivatives interacted allosterically with the enzyme.
MOLECULAR DIVERSITY
(2021)
Review
Chemistry, Medicinal
T. M. Rangarajan, Bijo Mathew
Summary: Pyrazolines are five-membered heterocyclic compounds with two nitrogen atoms, serving as a privileged scaffold for diverse bioactive compounds. Synthesized from chalcones and hydrazine derivatives, they can greatly enhance physicochemical and pharmacological properties, particularly for CNS-related issues such as neurodegenerative disorders.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Multidisciplinary
Aditi Tiwari, Anjaneyulu Bendi, Anirudh Singh Bhathiwal
Summary: Chalcones are a group of aromatic ketones with enone moiety that exhibit a wide range of biological activities, and when synthesized into pyrazolines, their biological activity can be enhanced. This study reviews the chemistry of various chalcone-based pyrazolines and their derivatives up to 2021.
Article
Chemistry, Organic
Gajanan Kottapalle, Nagesh Deshmukh, Avinash Shinde
Summary: A new series of pyrazolines derivatives containing isoniazid moiety were synthesized and evaluated for their antitubercular activity. The presence of disubstituted halogen compound and electron-withdrawing group on the phenyl ring was found to be important for increasing the antitubercular activity.
LETTERS IN ORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Hesti Lina Wiraswati, M. Hasan Bashari, Nayla Majeda Alfarafisa, Ilma Fauziah Ma'ruf, Eti Nurwening Sholikhah, Tutik Dwi Wahyuningsih, Pamungkas Bagus Satriyo, Denny Mustofa, Denny Satria, Ema Damayanti
Summary: This study conducted virtual screening to predict the anticancer potential of chalcone and pyrazoline derivatives against breast cancer cells. The results showed that pyrazolines A, A1, A2, B, C2, D, and M have potential as anticancer agents. Further studies are needed to synthesize and evaluate their anticancer activity in vitro and in vivo.
JOURNAL OF PHARMACY & PHARMACOGNOSY RESEARCH
(2023)
Article
Chemistry, Organic
Hemantkumar N. Akolkar, Sujata G. Dengale, Keshav K. Deshmukh, Bhausaheb K. Karale, Nirmala R. Darekar, Vijay M. Khedkar, Mubarak H. Shaikh
Summary: Novel compounds targeting Malaria were synthesized based on computational docking data, and showed excellent anti-malarial activity. However, they did not exhibit significant antimicrobial activity.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Article
Biochemistry & Molecular Biology
Olga Troitskaya, Diana Novak, Anna Nushtaeva, Maria Savinkova, Mikhail Varlamov, Mikhail Ermakov, Vladimir Richter, Olga Koval
Summary: The study showed that MCF7 cells with high EGFR expression can quickly form spheroids enriched with cancer stem cells, which are characterized by lower drug resistance compared to normal MCF7 cells. These MCF7-EGFR spheroids serve as a useful cancer model for drug development, especially EGFR-targeted therapies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Chemistry, Multidisciplinary
Rajnish Kumar, Himanshu Singh, Avijit Mazumder, Salahuddin, Ranjeet Kumar Yadav
Summary: It has been confirmed that pyrazolines and their analogs have pharmacological activity. The pyrazoline moiety is present in several marketed molecules with a wide range of uses, establishing its importance in pharmaceutical, agricultural, and industrial sectors. Scientists are continuously exploring the chemistry of pyrazolines and their derivatives due to their broad-spectrum utility. Various synthesis strategies, such as chalcones, hydrazines, diazo compounds, and hydrazones, have been commonly used for the synthesis of pyrazoline and its analogs, but there are opportunities for other starting reagents to be employed.
TOPICS IN CURRENT CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Yangyang Feng, Qingmei Shi, Jing Lin, Erchong Chai, Xiang Zhang, Zhenli Liu, Lei Jiao, Yaobing Wang
Summary: In this study, a new type of rechargeable Zn-hydrazine battery was proposed and realized, which can efficiently generate separated hydrogen through temporarily decoupled electrochemical hydrazine splitting. The battery exhibits low energy input and high energy efficiency, as well as outstanding long-term stability for continuous hydrogen production on demand, showing great potential for practical application.
ADVANCED MATERIALS
(2022)
Article
Chemistry, Organic
Silja Hofmann, Martin Linden, Julian Neuner, Felix N. Weber, Siegfried R. Waldvogel
Summary: This article presents an electrochemically enabled approach for the sustainable synthesis of pyrazoles via oxidative aromatization of pyrazolines. It utilizes inexpensive sodium chloride as a redox mediator and supporting electrolyte in a biphasic system (aqueous/organic), and can be conducted using carbon-based electrodes in a simple electrolysis set-up. The method allows for simple work-up strategies such as extraction and crystallization, enabling its application on a technically relevant scale.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Martin Linden, Silja Hofmann, Antonia Herman, Nicole Ehler, Robin M. M. Baer, Siegfried R. R. Waldvogel
Summary: This study presents the first electrochemical approach for the direct synthesis of pyrazolines and pyrazoles from easily accessible hydrazones and dipolarophiles. The method allows for large-scale production and even conversion of highly sensitive alkenes. The use of a biphasic system with sodium iodide as a supporting electrolyte and mediator is cost-effective. Mechanistic insight is provided by the isolation of key intermediates, and the synthesis of a commercial herbicide safener further highlights the significance of this reaction.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Biochemistry & Molecular Biology
D. D. Novak, O. S. Troitskaya, A. A. Nushtaeva, M. Zhilnikova, V. A. Richter, M. I. Meschaninova, O. A. Koval
Summary: This study demonstrates the importance of EGFR in tumor formation and destruction, and suggests that N-cadherin is involved in the EGFR-dependent formation of MCF7-EGFR spheroids. Therefore, MCF7-EGFR spheroids can serve as a suitable model for studying aggressive hormone-positive breast tumors.
Article
Biochemistry & Molecular Biology
Shahabuddin, Avadhesh Kumar, Mehtab Parveen, Mahboob Alam
Summary: This study reports a simple and effective method for preparing 6 alpha-nitro-5 alpha-cholestano[7 alpha,5-cd] pyrazo-lines (4-7). In-silico study reveals significant interactions between the reactants and products with SARS-CoV-2 omicron protease.
Article
Biochemistry & Molecular Biology
Wagdy M. Eldehna, Sara T. Al-Rashood, Tarfah Al-Warhi, Razan O. Eskandrani, Amal Alharbi, Ahmed M. El Kerdawy
Summary: In this study, three series of oxindole-benzofuran hybrids were designed and synthesised as dual CDK2/GSK-3 beta inhibitors targeting breast cancer. The N-1 -unsubstituted oxindole derivatives showed potent cytotoxic activity, while the N-1-substituted derivatives exhibited moderate to weak activity on breast cancer cell lines. The most potent compounds caused cell cycle arrest in the G2/M phase by inhibiting CDK2/GSK-3 beta, as demonstrated by enzyme inhibition assays and molecular docking studies.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(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
Chemistry, Medicinal
Eman A. Abd El-Meguid, Ahmed M. Naglah, Gaber O. Moustafa, Hanem M. Awad, Ahmed M. El Kerdawy
Summary: A series of benzothiazole-based derivatives were synthesized and showed promising cytotoxic activities, as well as inhibitory activities against VEGFR-2 and EGFR. Some derivatives exhibited potent activity against resistant cell lines. QSAR study revealed the impact of molecular bulkiness and molecular partial charge distribution on the kinase inhibition potency in this series. Molecular docking study showed that the synthesized derivatives adopted the common binding pattern of type II PK inhibitors in VEGFR-2.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Medicinal
Heba T. Abdel-Mohsen, Ahmed M. El Kerdawy, Mohamed A. Omar, Andrea Petreni, Rasha M. Allam, Hoda El Diwani, Claudiu T. Supuran
Summary: A novel series of carbonic anhydrase inhibitors showed high potency and selectivity, displaying significant antiproliferative activity against cancer cells and suggesting CA II inhibition as a potential alternative therapeutic target for cancer treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Wagdy M. Eldehna, Raed M. Maklad, Hadia Almahli, Tarfah Al-Warhi, Eslam B. Elkaeed, Mohammed A. S. Abourehab, Hatem A. Abdel-Aziz, Ahmed M. El Kerdawy
Summary: In this study, a hybridisation strategy was used to design novel CDK2 type II inhibitors, which showed promising inhibitory activity and antiproliferative activity against cancer cell lines. The designed compounds have the potential to be used in cancer treatment with low toxicity to normal cells.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Tarfah Al-Warhi, Ahmed M. El Kerdawy, Mohamed A. Said, Amgad Albohy, Zainab M. Elsayed, Nada Aljaeed, Eslam B. Elkaeed, Wagdy M. Eldehna, Hatem A. Abdel-Aziz, Miral A. Abdelmoaz
Summary: In this study, various thiazolyl-pyrazoline derivatives were synthesized and evaluated for their anti-tumor activities. Compounds 7g and 7m showed the best activity against both lung cancer and breast cancer cells, with potential for EGFR inhibition.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Article
Chemistry, Medicinal
Yomna El-Gazzar, Heba R. Ghaiad, Ahmed M. El Kerdawy, Riham F. George, Hanan H. Georgey, Khairia M. Youssef, Hussein El-Subbagh
Summary: New 2-mercapto-quinazolin-4-one analogs were synthesized and tested for their in vitro anticancer activity, DHFR inhibition, and EGFR-TK inhibition. Compound 24 showed broad-spectrum anticancer activity, EGFR-TK inhibitory activity, and DHFR inhibitory potency.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Islam H. Ali, Heba T. Abdel-Mohsen, Marwa M. Mounier, Mahmoud T. Abo-Elfadl, Ahmed M. El Kerdawy, Iman A. Y. Ghannam
Summary: In this study, a series of conjugates of 2-arylbenzimidazole-thiopyrimidine and -thioquinazolin-4(3H)-ones were synthesized and tested for their anticancer and kinase inhibitory activities. Compounds 14c and 14g-i exhibited potent anticancer activity and RAF kinase inhibitory activity, suggesting their potential for cancer and tumor treatment.
BIOORGANIC CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Abdalla R. Mohamed, Ahmed M. El Kerdawy
Summary: This review highlights the importance of cellular signaling pathway components in controlling cell maturation stages and their potential as crucial targets for antitumor drugs. It discusses the diverse isoforms of these components that contribute to the resistance mechanisms developed by cancer cells. The article also presents molecular tracing of tumor resistance towards specific signaling pathways and suggests key interventions for the development of antitumor agents. Additionally, it explores the antitumor activities of kinase-targeting chemotherapies and their structural basis for protein kinase inhibitors, as well as the potential of multi-kinase inhibition approaches in overcoming cancer resistance.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Chemistry, Organic
Zinab M. Nofal, Kamelia M. Amin, Hanaa S. Mohamed, Ahmed M. El-Kerdawy, Magdy S. Aly, Basma S. Habib, Alaadin E. Sarhan
Summary: In this study, a novel series of 2-methyl-3-phenylquinazolin-4-one derivatives were synthesized and evaluated for their cytotoxic potential. Several compounds showed promising anticancer activity by inhibiting cell division and EGFR activity.
SYNTHETIC COMMUNICATIONS
(2022)
Article
Chemistry, Multidisciplinary
Marwa A. Fouad, Ahmed Serag, Enas H. Tolba, Manal A. El-Shal, Ahmed M. El Kerdawy
Summary: In this study, advanced firefly algorithm (FFA) and support vector regression (SVR) were used to construct quantitative structure-retention relationship (QSRR) models for predicting the retention behavior of quinolone and sulfonamide drugs in HPLC. pH value and acetonitrile composition in the mobile phase were studied to understand their effects on the retention behavior. The obtained QSRR models showed good performance in both internal and external validations, providing insights into the molecular features influencing retention behavior.
Article
Chemistry, Medicinal
Heba T. Abdel-Mohsen, Ahmed M. El Kerdawy, Andrea Petreni, Claudiu T. Supuran
Summary: Novel benzenesulfonamide derivatives were synthesized as carbonic anhydrase inhibitors, demonstrating potent inhibitory activity against multiple CA isoforms at the nanomolar range. The compounds displayed selectivity towards specific isoforms and adopted similar binding modes through molecular docking simulations.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Iman A. Y. Ghannam, Ahmed M. El Kerdawy, Marwa M. Mounier, Mahmoud T. Abo-elfadl, Islam H. Ali
Summary: Two series of diaryl urea derivatives were synthesized and tested for their cytotoxic activity against cancer cells and inhibitory activity against VEGFR-2 kinase. Some compounds exhibited potent cytotoxicity and inhibitory activity, as well as inducing apoptosis and inhibiting cancer cell migration. Molecular docking simulations and ADME property predictions were also performed.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Multidisciplinary
Iman A. Y. Ghannam, Ahmed M. El Kerdawy, Heba T. Abdel-Mohsen
Summary: A series of compounds were synthesized and evaluated for their cytotoxic activities against different cell lines and inhibitory activities against topoisomerases. Some compounds showed high toxicity against leukemia and breast cancer cell lines, and exhibited certain inhibitory effects on topoisomerases.
EGYPTIAN JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Eman M. Mohi El-Deen, Eman A. Abd El-Meguid, Usama Fathy, Eman A. Karam, Ahmed M. El Kerdawy
Summary: A new series of pyrazolo[3,4-b]pyridine compounds with potent antimicrobial activity and inhibition against methicillin-resistant Staphylococcus aureus (MRSA) and dihydrofolate reductase (DHFR) have been synthesized and evaluated.
EGYPTIAN JOURNAL OF CHEMISTRY
(2022)
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)