An organophotoredox-catalyzed 1,7-enyne bicyclization for the cis-diastereoselective synthesis of ester-substituted phenanthridinones has been achieved through radical cascade cyclization involving 1,6-hydrogen atom transfer. This transition-metal- and oxidant-free one-pot protocol generates three distinct C-C bonds and two quaternary carbon centers.
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Advances in the selective c-MET kinase inhibitors: Application of fused [5,6]-Bicyclic nitrogen-containing cores for anticancer drug design.
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Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran. Electronic address:
Over the past two decades, small molecules bearing [5,6]-bicyclic nitrogen-containing cores have emerged as one of the most extensively studied structures for the development of selective c-MET kinase inhibitors. Structure-activity relationship (SAR) studies have demonstrated that modifying these cores can significantly impact the biological properties of c-MET inhibitors, including safety/toxicity, potency, and metabolic stability. For example, although c-MET kinase inhibitors containing the [1,2,4]triazolo[4,3-b][1,2,4]triazine scaffold (core P) exhibit high inhibitory potency, they often face challenges due to metabolic stability defects.
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J Am Chem Soc
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Institute for Molecular Bioscience, Australian Research Council Centre of Excellence for Innovations in Peptide and Protein Science, The University of Queensland, Brisbane, Queensland 4072, Australia.
Transpeptidases are specialized enzymes that have evolved for site-selective modification of peptides and proteins at their backbone termini. Approaches for adapting transpeptidases to catalyze side chain modifications are substantially more restricted, and typically rely on large recognition tags or require specific reaction conditions that are not easily compatible with broader applications. Here we show that the engineered asparaginyl ligase AEP1 catalyzes direct isopeptide ligation by accepting an internal 2,3-diaminopropionic acid (Dap) residue adjacent to Leu, a motif that mimics the canonical N-terminal Gly-Leu substrate.
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Angew Chem Int Ed Engl
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Xi'an Jiaotong University, Frontier Institute of Science and Technology, 99 Yanxiang road, Yanta district, 710054, Xi'an, CHINA.
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ACS Omega
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College of Pharmacy, Gachon University, Medical Campus, Pharmacy, Hambakmoero 191, Yeonsu-gu, Incheon City 21936, Republic of Korea.
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View Article and Find Full Text PDFMetal-free [2+2]-photocycloaddition of unactivated alkenes enabled by continuous flow processing.
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School of Chemistry, University College Dublin, Science Centre South, Dublin 4, Ireland.
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