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Articles 1 - 3 of 3
Full-Text Articles in Heterocyclic Compounds
Visible Light Kinetics Of N-Heterocyclic Carbenes As Additives For Native Chemical Ligation, Hannah M. Werle, Kaitlyn S. Marley, John P. Morgan
Visible Light Kinetics Of N-Heterocyclic Carbenes As Additives For Native Chemical Ligation, Hannah M. Werle, Kaitlyn S. Marley, John P. Morgan
SURF Posters 2026
Spectroscopic data have been obtained demonstrating that N-heterocyclic carbenes are effective catalysts for linking shorter peptides to form longer ones, a reaction known as “native chemical ligation” (NCL). This reaction is key to the preparation of GLP-1 agonists, such as Zepbound®, Ozempic®, and Wegovy®, which are currently undergoing an explosion in popularity due to their treatment of diabetes, obesity, and cardiac issues. To assess which catalysts are faster, the kinetics model developed by Raines et al., involving the reaction of N-acetylphenylalanine p-nitrophenylthioester and L-cysteine, is being utilized. This published model allows for easy monitoring of the rate of reaction for …
Design And In Silico Modeling Of Heterocyclic-Based Xanthone Derivatives As Potential Anticancer Agents Through Tyrosine Kinase Inhibition, Yehezkiel Steven Kurniawan, Ervan Yudha, Nela Fatmasari, Radite Yogaswara, Harno Dwi Pranowo, Eti Nurwening Sholikhah, Jumina Jumina
Design And In Silico Modeling Of Heterocyclic-Based Xanthone Derivatives As Potential Anticancer Agents Through Tyrosine Kinase Inhibition, Yehezkiel Steven Kurniawan, Ervan Yudha, Nela Fatmasari, Radite Yogaswara, Harno Dwi Pranowo, Eti Nurwening Sholikhah, Jumina Jumina
Makara Journal of Science
Cancer is one of the deadliest diseases nowadays, and tyrosine kinase receptors play crucial roles in cancer cell survival, differentiation, proliferation, and migration. This study designed and developed a new inhibitor from heterocyclic-based xanthone derivatives to target two tyrosine kinase receptors, epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR), through in silico screening. Eighteen heterocyclic-based xanthones were evaluated through molecular docking for both receptors. All heterocyclic-based xanthones gave the root mean square deviation (RMSD) value lower than 2.00 Å. Xanthone with isobenzothiazole substituent (iBzThio) was found as the most potent inhibitor with binding energies of -10.60 and …
Synthesis And Characterization Of Succinate Dehydrogenase Inhibitors H2/Z14 And C6/Z96 In Order To Combat Small Cell Lung Cancer, Lauren M. Graves
Synthesis And Characterization Of Succinate Dehydrogenase Inhibitors H2/Z14 And C6/Z96 In Order To Combat Small Cell Lung Cancer, Lauren M. Graves
Honors Undergraduate Theses
The use of ubiquinone inhibitors to combat cancer is a recent development in medicinal science and procedures to efficiently synthesize these drugs remain limited. C6/Z96 and H2/Z14, two succinate dehydrogenase inhibitors, have been previously tested in vitro against NSCLC with positive results. Their similarity to ubiquinone is what makes them a strong candidate for a succinate dehydrogenase inhibitor at the ubiquinone binding site. The heterocyclic scaffolds and substituents are proposed to bind strongly through a combination of electronics, hydrogen-bonding, and fit, allowing them to bind well and prove to be more favorable than ubiquinone when competing for the Q-site. By …