Article
Chemistry, Physical
Sumit Thakral, Devinder Kumar, Suman Rani, Ramesh Kataria, Poonam Sagar, Nitin Kumar Singhal
Summary: A library of 2'-aryl-2,5'-bibenzoxoles was synthesized and characterized. Compounds 8p, 8k, and 8t showed good cytotoxicity against cervical cancer cell lines.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Engineering, Environmental
Lijinhong Huang, Bin Xiao, Lihong Liu, Wenhao Li, Xiaoguang Duan, Wanfu Huang, Chunyan Fan, Yu Dong, Shaomin Liu
Summary: In this study, three-dimensional porous polymers were successfully prepared using benzimidazole and benzoxazole via a one-pot synthesis. The materials exhibited high surface areas and pore volumes, making them suitable for the adsorption and removal of heavy rare earth ions.
JOURNAL OF WATER PROCESS ENGINEERING
(2023)
Article
Food Science & Technology
Ebtehal K. Farrag, Wessam M. Aziz, Sylvia E. Shaker, Heba Shawky, Dalia B. Fayed
Summary: This study investigated the toxicological profile of BMPE in both in vitro and in vivo settings. The results showed that BMPE exhibited selective cytotoxicity against malignant cells and induced early cell apoptosis. In vivo experiments demonstrated that BMPE had tolerable toxicity at certain doses, and it also showed a modulatory effect on the oxidative-inflammatory response.
FOOD AND CHEMICAL TOXICOLOGY
(2023)
Article
Chemistry, Medicinal
Abigail C. Jackson, Tyler B. J. Pinter, Daniel C. Talley, Adnan Baker-Agha, Dhruvil Patel, Paul J. Smith, Katherine J. Franz
Summary: Metallo-beta-lactamases, such as NDM-1, utilize catalytic zinc ions in their active sites and have the ability to hydrolyze nearly all clinically available beta-lactam antibiotics. Inhibitors of metallo-beta-lactamases, which are urgently needed to combat antibacterial drug resistance, show promise in zinc-binding compounds. Evaluating 13 chelating agents containing benzimidazole and benzoxazole scaffolds as NDM-1 inhibitors revealed six compounds with potent inhibitory activity, suggesting potential for further development as NDM-1 inhibitors.
Article
Biochemistry & Molecular Biology
Sumit Thakral, Devinder Kumar, Samridhi Thakral, Vikramjeet Singh, A. Muni Nagesh, Sneha Verma, Deepak Pandey
Summary: Synthesized 2-halogenatedphenyl benzoxazole-5-carboxylic acids showed significant anti-inflammatory and cytotoxic activities, with compound 6b exhibiting comparable anti-inflammatory activity to standard drug ibuprofen and compound 6c showing superior cytotoxic activity to doxorubicin against human prostate carcinoma epithelial cell lines.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
Alicja Skrzypek, Monika Karpinska, Malgorzata Juszczak, Aneta Grabarska, Joanna Wietrzyk, Elzbieta Krajewska-Kulak, Marek Studzinski, Tadeusz Paszko, Joanna Matysiak
Summary: Benzoxazole and naphthoxazole fused systems, functionalized by the 2,4-dihydroxyphenyl moiety, showed potential activity in inhibiting AChE, anticancer effects, and antioxidant properties. Naphtho[1,2-d][1,3]oxazoles exhibited higher antiproliferative activity against human cancer cell lines compared to benzoxazoles, with one analog showing no toxicity to normal cells.
Article
Chemistry, Physical
Reddymasu Sireesha, Reddymasu Sreenivasulu, Choragudi Chandrasekhar, Surender Singh Jadav, Y. Pavani, Mandava Venkata Basaveswara Rao, Mannam Subbarao
Summary: A new series of benzimidazole/benzoxazole linked beta-carbolines were designed and synthesized, showing significant anti-cancer activity, especially against MCF-7 cell lines. These hybrid beta-carbolines also exhibited potential as kinase binders in molecular interaction analysis, suggesting promising future applications in cancer research.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Multidisciplinary Sciences
Mariam T. Sayed, Salwa A. Elsharabasy, Anhar Abdel-Aziem
Summary: Microbial infections are currently a widespread disease in hospitals and community health centres and are a major cause of death worldwide. Coumarin linked to thiazoles, pyridines and pyrazoles have been developed and evaluated for their antimicrobial properties against different microorganisms. Some of the prepared coumarins displayed high to moderate activity against the tested microorganisms with respect to the reference drugs, and compound 3 showed equal antimicrobial effect as Ciprofloxacin for Enterobacter cloacae. Compound 12 exhibited the most potent activity against Bacillus pumilis, while compounds 3, 4, and 12 showed remarkable activity against Streptococcus faecalis.
SCIENTIFIC REPORTS
(2023)
Article
Chemistry, Inorganic & Nuclear
Pragti, Sreshtha Nayek, Satyam Singh, Avinash Sonawane, Ivo Grabchev, Rakesh Ganguly, Suman Mukhopadhyay
Summary: In this study, three Ru(II) arene complexes with a bidentate benzimidazole-based ligand were synthesized and their antitumor activity was studied by varying the co-ligand X. The synthesized compounds showed good interactions with serum albumin proteins, had good drug stability and lipophilic character. They were found to bind with DNA and could induce apoptosis in cancer cells, as well as upregulate cleaved caspase-3 expression and downregulate BCLXL expression. These findings provide a new direction for the investigation of antitumor ruthenium-based metallodrugs using benzimidazole-based ligands.
DALTON TRANSACTIONS
(2023)
Article
Polymer Science
Haiquan Chen, Fengna Dai, Mengxia Wang, Chunhai Chen, Guangtao Qian, Youhai Yu
Summary: In this study, a pair of isomer diamines containing both benzimidazole and benzoxazole were successfully synthesized and used to prepare homopolyimides. The resulting polyimides exhibited outstanding thermal properties and ideal mechanical properties, making them suitable for flexible display substrate materials in the next generation.
JOURNAL OF POLYMER SCIENCE
(2021)
Article
Infectious Diseases
Christina Zalaru, Florea Dumitrascu, Constantin Draghici, Isabela Tarcomnicu, Maria Marinescu, George Mihai Nitulescu, Rodica Tatia, Lucia Moldovan, Marcela Popa, Mariana Carmen Chifiriuc
Summary: A new series of pyrazolo-benzimidazole hybrid Mannich bases were synthesized and characterized. In vitro cytotoxicity tests showed that the compounds were noncytotoxic at a certain concentration and exhibited high biocompatibility. The newly synthesized compounds demonstrated good antibacterial and antibiofilm activity against several bacterial strains.
Article
Chemistry, Medicinal
Hasan Kucukbay, Mustafa Uckun, Elif Apohan, Ozfer Yesilada
Summary: New benzimidazole derivatives were synthesized and tested for their cytotoxic properties against lung cancer cell line A549 and healthy lung epithelial cell line BEAS-2B. Compound 12 showed the highest cytotoxicity against A549 cells and comparable cytotoxicity to cisplatin against BEAS-2B cells. Additionally, compounds 7, 8, and 11 exhibited high antimicrobial activity against various microorganisms, with yeasts being particularly sensitive to these compounds.
ARCHIV DER PHARMAZIE
(2021)
Article
Biochemistry & Molecular Biology
Sravani Sana, Velma Ganga Reddy, T. Srinivasa Reddy, Ramya Tokala, Rahul Kumar, Suresh K. Bhargava, Nagula Shankaraiah
Summary: The study introduces a novel class of compounds with moderate to interesting cytotoxicity against various cancer cell lines, with compound 18i showing the highest potency and specificity towards A549 (lung cancer) cells. Flow cytometry analysis revealed that 18i induced G2/M phase cell cycle arrest, indicating potential anticancer activity. The most active compound, 18i, demonstrated enhanced microtubule disruption and significant antitumor effects through multiple mechanisms, including apoptosis induction, ROS generation, and inhibition of cellular migration.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Marta Redrado, Miriam Minana, Michael P. Coogan, M. Concepcion Gimeno, Vanesa Fernandez-Moreira
Summary: This study synthesized bioactive and luminescent cyclometallated iridium complexes with benzimidazole derivatives as auxiliary mimics of nucleotides. The complexes exhibited orange and green emission, with increased quantum yield under anaerobic conditions. The complexes also showed enhanced antiproliferative activity against lung cancer cells upon irradiation, making them potential candidates for photodynamic therapy.
Article
Chemistry, Physical
Umut Dogan, Ozge Ozcan, Gizem Alaca, Aydan Ari, Salih Gunnaz, H. Tansel Yalcin, Onur Sahin, Sevil Irisli
Summary: Three new Platinum complexes were synthesized and characterized, showing moderate cytotoxic activities against cancer cell lines and antimicrobial effects on both gram positive and gram negative bacteria.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Energy & Fuels
Imtiaz Ahmad, Waqas Ahmad, Syed Mohammad Sohail, Aftab Yasin
Summary: This study investigates the distillation behavior of neat and surfactants dispersed crude oils using boiling point curves/ASTM curves. The presence of surfactants increases the volatility of the crude oils, resulting in lighter products.
PETROLEUM SCIENCE AND TECHNOLOGY
(2023)
Article
Spectroscopy
Li Wang, Waqas Ahmad, Jizhong Wu, Xinnong Wang, Quansheng Chen, Qin Ouyang
Summary: A fluorescence nanosensor based on molecularly imprinted polymer modified upconversion nanoparticles was established for the selective and sensitive determination of carbendazim residues. The method showed good linearity, sensitivity, and stability in real food samples.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2023)
Article
Materials Science, Ceramics
Waqas Ahmad, Sofia Tahir, Adnan Ali, Khalid Mahmood
Summary: This paper investigates the impact of transition metal oxides (TMOs) on the front side passivation of c-Si PERC solar cells. Through simulation, three different configurations were compared, and the best thicknesses of TMO layers were selected. The reduction of front side losses was achieved.
CERAMICS INTERNATIONAL
(2023)
Article
Crystallography
Mohammad M. Al-Sanea, Olivier Blacque, Ahmed A. B. Mohamed, Edward R. T. Tiekink, Ali A. El-Emam
Summary: This is a triclinic compound with the chemical formula C18H17BrF3N3S. The unit cell parameters are a = 8.6380 Å, b = 14.5082 Å, c = 14.8000 Å, and the angles are alpha = 98.177°, beta = 97.015°, gamma = 91.111°. The crystal has a volume of 1820.89 Å3 and belongs to the space group P1 with 4 molecules in the unit cell. The crystal structure is well characterized.
ZEITSCHRIFT FUR KRISTALLOGRAPHIE-NEW CRYSTAL STRUCTURES
(2023)
Article
Engineering, Chemical
Waqas Ahmad, Waqas Farooq, Adnan Daud Khan, Shayan Tariq Jan, Michal Jasinski, Zbigniew Leonowicz, Radomir Gono, Jan Petrov
Summary: This study investigates the influence of C2N-based solar cells with Zn1-xMgxO buffer layers using numerical simulations. The results show that increasing the buffer layer Mg concentration reduces device performance, while increasing the absorber layer thickness improves efficiency. However, a doping density above a certain level degrades cell performance. Optimizing the buffer layer thickness and doping density, the C2N/Zn0.8125Mg0.1875O structure achieves the highest power conversion efficiency (PCE) of 19.01%.
Review
Materials Science, Multidisciplinary
Waqas Ahmad, Ayesha Khan Tareen, Karim Khan, Maaz Khan, Qasim Khan, Zhiming Wang, Muhammad Maqbool
Summary: Low dimensional materials are promising for electronic and optoelectronic devices due to their unique electronic structure and physiochemical properties. Mixed dimensional heterostructures (MDHs) combine different nanomaterials with various dimensionalities, offering great potential for a wide range of applications. Various dimensionalities of MDHs, especially 2D materials, enhance charge carrier mobilities, optical absorption, and response, making them ideal for developing next-generation optoelectronic devices.
APPLIED MATERIALS TODAY
(2023)
Article
Environmental Sciences
Amarjeet Singh, Maria Gracheva, Viktoria Kovacs Kis, Aron Keresztes, Mate Sagi-Kazar, Brigitta Muller, Fruzsina Pankaczi, Waqas Ahmad, Krisztina Kovacs, Zoltan May, Gyula Tolnai, Zoltan Homonnay, Ferenc Fodor, Zoltan Klencsar, Adam Solti
Summary: Nanoscale Fe-containing particles can penetrate the root apoplast. Close contact between FERRIC REDUCTASE OXIDASE (FRO) enzymes and Fe-containing particles is required for Fe mobilization. Haematite nanoparticles can be stacked in the middle lamella of the apoplast and release Fe through reduction process.
Article
Acoustics
Zhen Wang, Waqas Ahmad, Afang Zhu, Wenhui Geng, Wencui Kang, Qin Ouyang, Quansheng Chen
Summary: This study combined headspace solid phase microextraction-gas chromatography-mass spectrometry (HS-SPME-GC/MS) with multivariate analysis fusion metabonomics to investigate the metabolite profile changes in fermented kombucha tea. The correlation between the metabolites and the fermentation process was comprehensively explored. Ultrasound-assisted factors were also examined for optimizing the fermentation process. A total of 132 metabolites were detected in the fermented kombucha using HS-SPME-GC/MS. Multivariate statistical analysis revealed significant differences in the phenotype of metabolites during the fermentation, and 25 characteristic metabolites were identified as biomarkers. Leaf alcohol was identified as the characteristic volatile during the fermentation process. The findings of this research provide insights for enhancing the flavor and aroma of kombucha in future fermentation processes.
ULTRASONICS SONOCHEMISTRY
(2023)
Article
Environmental Sciences
Faiza Rehman, Waqas Ahmad, Nazish Parveen, Syed Khuram Zakir, Sanaullah Khan, Changseok Han
Summary: Fe2+/persulfate, Fe2+/peroxymonosulfate, and Fe2+/H2O2 were effective in the degradation of diclofenac sodium in water without UV-C light. The degradation efficiency varied depending on the oxidant used, with Fe2+/persulfate showing the highest decomposition of DCF sodium. The presence of various anions significantly affected the degradation efficiency, and the Fe2+/oxidant system showed promise in eliminating diclofenac sodium from the water environment.
Article
Green & Sustainable Science & Technology
Waqas Ahmad, Hikmat Ullah Khan, Tasswar Iqbal, Muhammad Attique Khan, Usman Tariq, Jae-hyuk Cha
Summary: With the rapid growth of user-generated content on social media, sentiment analysis has become a significant research area. In this manuscript, a technique combining variant algorithms in a parallel manner is proposed to extract advantageous informative features, and then perform sentiment classification. The proposed methodology, a combination of MC-CNN and MC-Bi-GRU, treats them equally in terms of input parameters and shares hidden layer information, making it distinctive and outperforming existing models.
Article
Pharmacology & Pharmacy
Omnia M. Hendawy, Mohammad M. Al-Sanea, Rehab Mohammed Elbargisy, Hidayat Ur Rahman, Hesham A. M. Gomaa, Ahmed A. B. Mohamed, Mohamed F. Ibrahim, Abdulsalam M. Kassem, Mohammed Elmowafy
Summary: The objective of this study was to fabricate, optimize, and assess olive oil/phytosomal nanocarriers for improved quercetin skin delivery. The optimized formulation, selected using a Box-Behnken design, showed better stability at ambient temperature and higher skin permeation of quercetin compared to the control. The optimized formulation also demonstrated alteration to skin barriers without remarkable toxicity aspects, indicating the potential of olive oil/phytosomal nanocarriers as carriers for quercetin.
Review
Plant Sciences
Ehab M. Mostafa, Arafa Musa, Hamdoon A. Mohammed, Abdulaziz Ibrahim Alzarea, Mohamed A. Abdelgawad, Mohammad M. Al-Sanea, Ahmed Ismail, Ameeduzzafar Zafar, Mohammed Elmowafy, Samy Selim, Riaz A. Khan
Summary: Plants of the Tylophora genus have been widely used in traditional medicine, especially in tropical and subtropical regions. These plants have shown diverse pharmacological activities, including anti-inflammatory, anti-tumor, anti-allergic, anti-microbial, hypoglycemic, and anti-oxidant effects. They have also exhibited diuretic, anti-asthmatic, and hepato-protective activities. The review provides information on the distribution, synonyms, chemical diversity, and biological activities of Tylophora plants.
Article
Chemistry, Medicinal
Nema S. Shaban, Abeer M. Radi, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Rasha Hamed Al-Serwi, Randa M. Hassan, Eman T. Mohammed, Rania A. Radi, Fatma M. Halfaya
Summary: Amphora coffeaeformis and nano-naringenin were found to have therapeutic effects on osteoarthritis by reducing oxidative stress and inflammation and increasing antioxidant capacity. Therefore, they can be considered as natural therapeutic agents for osteoarthritis.
Article
Chemistry, Medicinal
Syed Nasir Abbas Bukhari, Mohamed Abdelwahab Abdelgawad, Naveed Ahmed, Muhammad Wahab Amjad, Muhammad Ajaz Hussain, Mervat A. Elsherif, Hasan Ejaz, Nasser H. Alotaibi, Ignjat Filipovic, Nenad Jankovic
Summary: In this study, eight novel Meldrum's acid derivatives with various vanillic groups were synthesized and tested against cancer cell lines and microbes. Three of them showed excellent biological activity against E. coli, HeLa, and A549 cell lines. The O-alkyl substituted derivatives exhibited better antimicrobial and anticancer activities compared to the O-acyl ones. Compound 3i, with decyl substitution, demonstrated the highest activity against E. coli and cancer cell lines, with a selectivity index of 4.8 (HeLa). Molecular docking studies revealed that compound 3i had strong binding affinity to DNA, E. coli Gyrase B, and topoisomerase II beta, acting as a Michael acceptor for nucleophiles Lys and Ser. The topoisomerase II beta-LYS482-3i cluster showed the best E-b.
Article
Chemistry, Medicinal
Arafa Musa, Hamada S. Abulkhair, Ateyatallah Aljuhani, Nadjet Rezki, Mohamed A. Abdelgawad, Khaled Shalaby, Ahmed H. El-Ghorab, Mohamed R. Aouad
Summary: COVID-19 infection is a leading cause of human death. In this study, nineteen novel compounds were designed and synthesized to discover new medications for COVID-19. These compounds showed potent cellular anti-COVID-19 activity and inhibited viral replication with no or weak cytotoxic effect. In addition, the compounds were tested for their ability to block the primary protease of the SARS-CoV-2 virus and showed promising inhibitory activity. Molecular modeling studies and simulations were done to analyze the compounds' interactions and stability. The results suggest that these compounds have potential as potent medicines for SARS-CoV-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)