Pyrrole: A decisive scaffold for the development of therapeutic agents and structure-activity relationship
ChemMedChem. 2023 Nov 5:e202300447. doi: 10.1002/cmdc.202300447. Online ahead of print.ABSTRACTThe overview of pyrroles as distinct scaffolds with therapeutic potential and the significance of pyrrole derivatives for drug development are provided in this article. It lists instances of naturally occurring pyrrole-containing compounds and describes the sources of pyrroles in nature, including plants and microbes. It also explains the many conventional and modern synthetic methods used to produce pyrroles. The key topics are the biological characteristics, pharmacological behavior, and functional alterations displayed by pyrr...
Source: ChemMedChem - November 5, 2023 Category: Chemistry Authors: Bharathi Hassan Ganesh Anirudh G Raj Baladhandapani Aruchamy Pandurangan Nanjan Carmelo Drago Prasanna Ramani Source Type: research

Pyrrole: A decisive scaffold for the development of therapeutic agents and structure-activity relationship
ChemMedChem. 2023 Nov 5:e202300447. doi: 10.1002/cmdc.202300447. Online ahead of print.ABSTRACTThe overview of pyrroles as distinct scaffolds with therapeutic potential and the significance of pyrrole derivatives for drug development are provided in this article. It lists instances of naturally occurring pyrrole-containing compounds and describes the sources of pyrroles in nature, including plants and microbes. It also explains the many conventional and modern synthetic methods used to produce pyrroles. The key topics are the biological characteristics, pharmacological behavior, and functional alterations displayed by pyrr...
Source: ChemMedChem - November 5, 2023 Category: Chemistry Authors: Bharathi Hassan Ganesh Anirudh G Raj Baladhandapani Aruchamy Pandurangan Nanjan Carmelo Drago Prasanna Ramani Source Type: research

Pyrrole: A decisive scaffold for the development of therapeutic agents and structure-activity relationship
ChemMedChem. 2023 Nov 5:e202300447. doi: 10.1002/cmdc.202300447. Online ahead of print.ABSTRACTThe overview of pyrroles as distinct scaffolds with therapeutic potential and the significance of pyrrole derivatives for drug development are provided in this article. It lists instances of naturally occurring pyrrole-containing compounds and describes the sources of pyrroles in nature, including plants and microbes. It also explains the many conventional and modern synthetic methods used to produce pyrroles. The key topics are the biological characteristics, pharmacological behavior, and functional alterations displayed by pyrr...
Source: ChemMedChem - November 5, 2023 Category: Chemistry Authors: Bharathi Hassan Ganesh Anirudh G Raj Baladhandapani Aruchamy Pandurangan Nanjan Carmelo Drago Prasanna Ramani Source Type: research

Pyrrole: A decisive scaffold for the development of therapeutic agents and structure-activity relationship
ChemMedChem. 2023 Nov 5:e202300447. doi: 10.1002/cmdc.202300447. Online ahead of print.ABSTRACTThe overview of pyrroles as distinct scaffolds with therapeutic potential and the significance of pyrrole derivatives for drug development are provided in this article. It lists instances of naturally occurring pyrrole-containing compounds and describes the sources of pyrroles in nature, including plants and microbes. It also explains the many conventional and modern synthetic methods used to produce pyrroles. The key topics are the biological characteristics, pharmacological behavior, and functional alterations displayed by pyrr...
Source: ChemMedChem - November 5, 2023 Category: Chemistry Authors: Bharathi Hassan Ganesh Anirudh G Raj Baladhandapani Aruchamy Pandurangan Nanjan Carmelo Drago Prasanna Ramani Source Type: research

Synthesis and Biological Evaluation of Oxindole Sulfonamide Derivatives as Bruton's Tyrosine Kinase Inhibitors
This study focuses on the design and synthesis of new oxindole sulfonamide derivatives as promising inhibitors of BTK with negligible off-target effects. The most cytotoxic compounds with greater basicity were PID-4 (2.29 ± 0.52 µM), PID-6 (9.37 ± 2.47 µM), and PID-19 (2.64 ± 0.88 µM). These compounds caused a selective inhibition of Burkitt's lymphoma RAMOS cells without significant cytotoxicity in non-BTK cancerous and non-cancerous cell lines. Further, PID-4 showed promising activity in inhibiting BTK and downstream signalling cascades. As a potent inhibitor of Burkitt's lymphoma cells, PID-4 is a promising lead f...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Chandra Prakash Koraboina Venkatanarayana Chowdary Maddipati Narendran Annadurai So ňa Gurská Petr Dzubak Marian Hajduch Viswanath Das Rambabu Gundla Source Type: research

Recent Progress in Prompt Molecular Detection of Exosomes Using CRISPR/Cas and Microfluidic-Assisted Approaches Toward Smart Cancer Diagnosis and Analysis
ChemMedChem. 2023 Nov 2:e202300359. doi: 10.1002/cmdc.202300359. Online ahead of print.ABSTRACTNano exosomes are essential indicators of molecular mechanisms involved in interacting with cancer cells and the tumor environment. The nano exosomes, as nanostructures based on lipids and nucleic acids, provide a communication pathway for information transfer by transporting biomolecules from the target cell to other cells. Importantly, these extracellular vesicles are released into the blood flow by the most invading cells, i.e., cancer cells; thereby, they could be considered a promising specific biomarker for cancer diagnosis...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Seyyed Mojtaba Mousavi Seyyed Alireza Hashemi Masoomeh Yari Kalashgrani Vahid Rahmanian Mohsen Riazi Navid Omidifar Raed H Althomali Mohammed M Rahman Wei-Hung Chiang Ahmad Gholami Source Type: research

Synthesis and Biological Evaluation of Oxindole Sulfonamide Derivatives as Bruton's Tyrosine Kinase Inhibitors
This study focuses on the design and synthesis of new oxindole sulfonamide derivatives as promising inhibitors of BTK with negligible off-target effects. The most cytotoxic compounds with greater basicity were PID-4 (2.29 ± 0.52 µM), PID-6 (9.37 ± 2.47 µM), and PID-19 (2.64 ± 0.88 µM). These compounds caused a selective inhibition of Burkitt's lymphoma RAMOS cells without significant cytotoxicity in non-BTK cancerous and non-cancerous cell lines. Further, PID-4 showed promising activity in inhibiting BTK and downstream signalling cascades. As a potent inhibitor of Burkitt's lymphoma cells, PID-4 is a promising lead f...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Chandra Prakash Koraboina Venkatanarayana Chowdary Maddipati Narendran Annadurai So ňa Gurská Petr Dzubak Marian Hajduch Viswanath Das Rambabu Gundla Source Type: research

Recent Progress in Prompt Molecular Detection of Exosomes Using CRISPR/Cas and Microfluidic-Assisted Approaches Toward Smart Cancer Diagnosis and Analysis
ChemMedChem. 2023 Nov 2:e202300359. doi: 10.1002/cmdc.202300359. Online ahead of print.ABSTRACTNano exosomes are essential indicators of molecular mechanisms involved in interacting with cancer cells and the tumor environment. The nano exosomes, as nanostructures based on lipids and nucleic acids, provide a communication pathway for information transfer by transporting biomolecules from the target cell to other cells. Importantly, these extracellular vesicles are released into the blood flow by the most invading cells, i.e., cancer cells; thereby, they could be considered a promising specific biomarker for cancer diagnosis...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Seyyed Mojtaba Mousavi Seyyed Alireza Hashemi Masoomeh Yari Kalashgrani Vahid Rahmanian Mohsen Riazi Navid Omidifar Raed H Althomali Mohammed M Rahman Wei-Hung Chiang Ahmad Gholami Source Type: research

Synthesis and Biological Evaluation of Oxindole Sulfonamide Derivatives as Bruton's Tyrosine Kinase Inhibitors
This study focuses on the design and synthesis of new oxindole sulfonamide derivatives as promising inhibitors of BTK with negligible off-target effects. The most cytotoxic compounds with greater basicity were PID-4 (2.29 ± 0.52 µM), PID-6 (9.37 ± 2.47 µM), and PID-19 (2.64 ± 0.88 µM). These compounds caused a selective inhibition of Burkitt's lymphoma RAMOS cells without significant cytotoxicity in non-BTK cancerous and non-cancerous cell lines. Further, PID-4 showed promising activity in inhibiting BTK and downstream signalling cascades. As a potent inhibitor of Burkitt's lymphoma cells, PID-4 is a promising lead f...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Chandra Prakash Koraboina Venkatanarayana Chowdary Maddipati Narendran Annadurai So ňa Gurská Petr Dzubak Marian Hajduch Viswanath Das Rambabu Gundla Source Type: research

Recent Progress in Prompt Molecular Detection of Exosomes Using CRISPR/Cas and Microfluidic-Assisted Approaches Toward Smart Cancer Diagnosis and Analysis
ChemMedChem. 2023 Nov 2:e202300359. doi: 10.1002/cmdc.202300359. Online ahead of print.ABSTRACTNano exosomes are essential indicators of molecular mechanisms involved in interacting with cancer cells and the tumor environment. The nano exosomes, as nanostructures based on lipids and nucleic acids, provide a communication pathway for information transfer by transporting biomolecules from the target cell to other cells. Importantly, these extracellular vesicles are released into the blood flow by the most invading cells, i.e., cancer cells; thereby, they could be considered a promising specific biomarker for cancer diagnosis...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Seyyed Mojtaba Mousavi Seyyed Alireza Hashemi Masoomeh Yari Kalashgrani Vahid Rahmanian Mohsen Riazi Navid Omidifar Raed H Althomali Mohammed M Rahman Wei-Hung Chiang Ahmad Gholami Source Type: research

Synthesis and Biological Evaluation of Oxindole Sulfonamide Derivatives as Bruton's Tyrosine Kinase Inhibitors
This study focuses on the design and synthesis of new oxindole sulfonamide derivatives as promising inhibitors of BTK with negligible off-target effects. The most cytotoxic compounds with greater basicity were PID-4 (2.29 ± 0.52 µM), PID-6 (9.37 ± 2.47 µM), and PID-19 (2.64 ± 0.88 µM). These compounds caused a selective inhibition of Burkitt's lymphoma RAMOS cells without significant cytotoxicity in non-BTK cancerous and non-cancerous cell lines. Further, PID-4 showed promising activity in inhibiting BTK and downstream signalling cascades. As a potent inhibitor of Burkitt's lymphoma cells, PID-4 is a promising lead f...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Chandra Prakash Koraboina Venkatanarayana Chowdary Maddipati Narendran Annadurai So ňa Gurská Petr Dzubak Marian Hajduch Viswanath Das Rambabu Gundla Source Type: research

Recent Progress in Prompt Molecular Detection of Exosomes Using CRISPR/Cas and Microfluidic-Assisted Approaches Toward Smart Cancer Diagnosis and Analysis
ChemMedChem. 2023 Nov 2:e202300359. doi: 10.1002/cmdc.202300359. Online ahead of print.ABSTRACTNano exosomes are essential indicators of molecular mechanisms involved in interacting with cancer cells and the tumor environment. The nano exosomes, as nanostructures based on lipids and nucleic acids, provide a communication pathway for information transfer by transporting biomolecules from the target cell to other cells. Importantly, these extracellular vesicles are released into the blood flow by the most invading cells, i.e., cancer cells; thereby, they could be considered a promising specific biomarker for cancer diagnosis...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Seyyed Mojtaba Mousavi Seyyed Alireza Hashemi Masoomeh Yari Kalashgrani Vahid Rahmanian Mohsen Riazi Navid Omidifar Raed H Althomali Mohammed M Rahman Wei-Hung Chiang Ahmad Gholami Source Type: research

Kinetic Modeling of PROTAC-Induced Protein Degradation
ChemMedChem. 2023 Oct 31:e202300530. doi: 10.1002/cmdc.202300530. Online ahead of print.ABSTRACTKinetics of the PROTAC-induced protein degradation was modelled with the equilibrium approximation, accounting for the protein recovery rate with a time lag. The simulated kinetic curves resemble what is experimentally observed, and the physical formulas of the half-maximal degradation concentration (DC50) were derived from them. The equations reveal that DC50 is proportional to the dissociation constant of the ternary complex (Kd) and inversely proportional to the expression level of the E3 ligase and the effective ubiquitylati...
Source: ChemMedChem - October 31, 2023 Category: Chemistry Authors: Hongtao Zhao Frank Narjes Source Type: research

Kinetic Modeling of PROTAC-Induced Protein Degradation
ChemMedChem. 2023 Oct 31:e202300530. doi: 10.1002/cmdc.202300530. Online ahead of print.ABSTRACTKinetics of the PROTAC-induced protein degradation was modelled with the equilibrium approximation, accounting for the protein recovery rate with a time lag. The simulated kinetic curves resemble what is experimentally observed, and the physical formulas of the half-maximal degradation concentration (DC50) were derived from them. The equations reveal that DC50 is proportional to the dissociation constant of the ternary complex (Kd) and inversely proportional to the expression level of the E3 ligase and the effective ubiquitylati...
Source: ChemMedChem - October 31, 2023 Category: Chemistry Authors: Hongtao Zhao Frank Narjes Source Type: research

Terpene-functionalized Fluoroquinolones as Potential Antimicrobials: Synthesis and Properties
This study was the first to synthesize terpene-containing conjugates of fluoroquinolones, ciprofloxacin and norfloxacin, and to evaluate their antibacterial activity against gram-positive methicillin sensitive (MSSA) and methicillin resistant (MRSA) S. aureus, gram-negative P. aeruginosa as well as antifungal activity against C. albicans. The ability of obtained fluoroquinolones to inhibit S. aureus growth was found to depend upon the presence of a linker separating the bulky terpene and fluoroquinolone fragments, and this activity diminished with increasing its length. The highest activity against MSSA was demonstrated by...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Evgeniy Sergeevich Izmest'ev Pestova V Svetlana Alena I Kolesnikova Diana R Baidamshina Airat R Kayumov Svetlana A Rubtsova Source Type: research