Article
Crystallography
Mezna Saleh Altowyan, Saied M. Soliman, Magda M. F. Ismail, Matti Haukka, Assem Barakat, Mohammed Salah Ayoup
Summary: The synthesis and characterization of new bioprecursor prodrugs of sulfadiazine have been established, and the crystal structure of the target compound has been obtained through X-ray analysis. The results showed that the interactions of H center dot center dot center dot H, O center dot center dot center dot H, and H center dot center dot center dot C contribute significantly to the crystal packing of the prodrug.
Review
Chemistry, Medicinal
Yuexuan Cheng, Chunhong Zhong, Shujing Yan, Chunli Chen, Xiaoli Gao
Summary: Prodrug strategy plays a critical role in innovative drug development. Structural modification is a straightforward and effective approach to develop prodrugs by improving drug defects and optimizing physical and chemical properties. Linking microenvironment-responsive groups to prototype drugs aids in enhancing drug targeting, while connecting prodrugs to suitable drug delivery systems enables improvements in drug loading, stability, bioavailability, and release control. This paper reviews lipidic, water-soluble, pH-responsive, redox-sensitive, and enzyme-activatable prodrugs based on structural modification.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Joomyung V. Jun, Yana D. Petri, Lucas W. Erickson, Ronald T. Raines
Summary: We have developed a versatile strategy for reversible modification of proteins using a tricomponent molecule. This molecule incorporates a diazo moiety for selective esterification of carboxyl groups, a pyridyl disulfide group for functionalization with thiolated ligands, and a self-immolative carbonate group for esterase-mediated cleavage. This strategy allows for the delivery of proteins into the cytosol of live mammalian cells, highlighting the advantages of bioreversible conjugation on carboxyl groups.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Chemistry, Medicinal
Claudia Schmidt, Tomer Babu, Hana Kostrhunova, Annika Timm, Uttara Basu, Ingo Ott, Valentina Gandin, Viktor Brabec, Dan Gibson
Summary: The multi-action Pt(IV) derivatives of cisplatin with combretastatin A4 (CA4) bioactive ligands show significantly higher cytotoxicity to cancer cells compared to cisplatin. In vivo tests demonstrate that the Pt(IV)-CA4 complexes inhibit tumor growth effectively, with the platinum moiety acting as a carrier triggered by reduction in cancer cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Simon Weising, Stefan Weber, Dominique Schols, Chris Meier
Summary: The study describes a triphosphate prodrug of 3'-fluoro-3'-deoxythymidine (FLT) with the aim of bypassing phosphorylation steps, increasing selectivity and stability, for potential use in HIV treatment.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biotechnology & Applied Microbiology
Pi-Wu Li, Jun Ma, Xiao-Feng Wei, Zi-Yang Zhang, Rui-Ming Wang, Jing Xiao, Jun-Qing Wang
Summary: Alkaline pectate lyase, BacPelA, was successfully modified to improve its catalytic activity, making it a promising candidate for applications in the textile, pulp, paper, and food industries.
Article
Biochemistry & Molecular Biology
Nupur S. Munjal, Rohit Shukla, Tiratha Raj Singh
Summary: Prodrugs are inactive drug molecules developed to improve pharmaceutical and pharmacokinetic properties. Paclitaxel, a potent anticancer drug, has low water solubility. Phosphate prodrugs can increase bioavailability by solving insolubility issues. In this study, twenty phosphate prodrugs of paclitaxel were evaluated, ten were selected for CYP3A4 docking studies, and three were found to be unstable compared to paclitaxel, indicating potential for increased bioavailability.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Medicinal
Crystall Swarbrick, Vasiliki Zogali, Kitti Wing Ki Chan, Dimitrios Kiousis, Chin Piaw Gwee, Sai Wang, Julien Lescar, Dahai Luo, Mark von Itzstein, Minos-Timotheos Matsoukas, George Panagiotakopoulos, Subhash G. Vasudevan, Gerasimos Rassias
Summary: The study presents a novel dengue protease inhibitor, SP-471, with high antiviral activity and no cellular toxicity, making it a promising candidate for dengue fever treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Xiao Jia, Dominique Schols, Chris Meier
Summary: This article describes the synthesis of two types of nucleotide prodrugs containing different nucleoside analogs and their effective inhibition against HIV-2 replication. The prodrugs exhibited high stability and antiviral activity in cell extracts.
Article
Chemistry, Applied
Ning Li, Min Han, Zhongzhong Xue, Panyue Liu, Lixia Ling, Ping Liu, Riguang Zhang, Baojun Wang
Summary: In this study, a catalyst with high activity and selectivity for the toluene methylation reaction via methanol was explored by modifying the structure of HZSM-5 zeolite and introducing Cu+ catalyst. The intrinsic activation energies and self-diffusion coefficients on BAS/Cu+-HZSM-5 zeolite were obtained through calculations and simulations. The results showed that BAS/Cu+-HZSM-5 had lower activation energy for methanol dissociation, smaller activation energy for xylene formation, and higher self-diffusion coefficient for PX, indicating its better catalytic performance and high PX selectivity.
MICROPOROUS AND MESOPOROUS MATERIALS
(2022)
Article
Chemistry, Multidisciplinary
Zhenchao Ma, Juanping Wu, Mengchi Sun, Bingyu Li, Xiang Yu
Summary: In this study, tumor redox stimulus-responsive nanoparticulate drug delivery systems were constructed using disulfide bonds as linkages. The results showed that disulfide bonds facilitated the breakage of polymers and the rapid release of drugs, unlike dicarbon bond-bridging polymers. These findings provide theoretical guidance for cancer therapy.
Article
Chemistry, Physical
Mykola Tasinkevych, Artem Ryabov
Summary: We studied the dynamics of a chemical nanoswimmer in a periodically rocked ratchet potential, and found that mechanochemical coupling can be utilized to control the motion of chemically active particles at the nanoscale.
JOURNAL OF MOLECULAR LIQUIDS
(2024)
Review
Agriculture, Multidisciplinary
Augusto Bene Tome Constantino, Edwin Elard Garcia-Rojas
Summary: Pseudocereals (amaranth, buckwheat, and quinoa) are gaining popularity as gluten-free crops due to their health benefits and high nutritional quality. However, the low solubility of their proteins in water limits their industrial applications. Various methods, including high-intensity ultrasound, heating, and conjugation, have been proposed to modify the physicochemical properties of these proteins and improve their solubility and functional properties.
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
(2022)
Article
Chemistry, Medicinal
Pooja V. D. Hegde, Michael D. Howe, Matthew Zimmerman, Helena L. M. Boshoff, Sachin Sharma, Brianna Remache, Ziyi D. Jia, Yan Pan, Anthony C. Baughn, Veronique Dartois, Courtney Aldrich
Summary: Tuberculosis is a deadly infectious disease with limited treatment options. Researchers have developed prodrugs and modified the structure of para-Aminosalicylic acid (PAS) to improve its oral bioavailability and reduce rapid clearance. These innovations have the potential to enhance the therapeutic effectiveness of PAS.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Oncology
Muhammad Abdur Rahim, Nasrullah Jan, Safiullah Khan, Hassan Shah, Asadullah Madni, Arshad Khan, Abdul Jabar, Shahzeb Khan, Abdelbary Elhissi, Zahid Hussain, Heather C. Aziz, Muhammad Sohail, Mirazam Khan, Hnin Ei Thu
Summary: This review focuses on improving the targeting of anticancer agents in the tumor microenvironment through stimuli-responsive drug delivery systems, discussing physical and chemical stimuli-responsive systems for active and passive targeting. Recent advancements in onco-targeted therapies have allowed for safe and effective tumor-specific localization, revolutionizing chemotherapy-based treatments with enhanced bioavailability and selective cytotoxicity.
