{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["15(1)"],"submitter":["Walunj D"],"pubmed_abstract":["Modifying existing drugs to enhance their activity and reduce toxicity is a major focus of drug development. We developed a novel class of dual-action chimeric molecules for cancer therapy, linking known drugs to a DNA-methylating monomethyl triazene moiety (azene) via nucleophilic substitution. In-vitro screening of these chimeras on various leukemia cell lines identified a potent chimera, doxorubizen, a sequel of the known DNA intercalator and topoisomerase 2 (Topo-II) inhibitor doxorubicin (Dox) and azene. Molecular docking and dynamic simulations showed doxorubizen as a more potent Topo-II inhibitor than Dox as it binds to major grooves in DNA. Moreover, the monomethyl triazene portion is positioned favorably through tetracene core intercalation, potentially facilitating methylation at"],"journal":["Scientific reports"],"pagination":["10607"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11950436"],"repository":["biostudies-literature"],"pubmed_title":["Novel dual action chimera doxorubizen demonstrates superior efficacy to doxorubicin in acute leukemia."],"pmcid":["PMC11950436"],"pubmed_authors":["Hershkovitz-Rokah O","Walunj D","Mitra P","Bazylevich A","Muddineni SSNA","Tkachenko I","Milyavsky M","Gellerman G","Tobi D","Zipin-Roitman A","Egarmina K","Shpilberg O"],"additional_accession":[]},"is_claimable":false,"name":"Novel dual action chimera doxorubizen demonstrates superior efficacy to doxorubicin in acute leukemia.","description":"Modifying existing drugs to enhance their activity and reduce toxicity is a major focus of drug development. We developed a novel class of dual-action chimeric molecules for cancer therapy, linking known drugs to a DNA-methylating monomethyl triazene moiety (azene) via nucleophilic substitution. In-vitro screening of these chimeras on various leukemia cell lines identified a potent chimera, doxorubizen, a sequel of the known DNA intercalator and topoisomerase 2 (Topo-II) inhibitor doxorubicin (Dox) and azene. Molecular docking and dynamic simulations showed doxorubizen as a more potent Topo-II inhibitor than Dox as it binds to major grooves in DNA. Moreover, the monomethyl triazene portion is positioned favorably through tetracene core intercalation, potentially facilitating methylation at","dates":{"release":"2025-01-01T00:00:00Z","publication":"2025 Mar","modification":"2026-06-01T22:59:36.908Z","creation":"2025-07-13T03:04:30.887Z"},"accession":"S-EPMC11950436","cross_references":{"pubmed":["40148439"],"doi":["10.1038/s41598-025-94373-8"]}}