{"id":980,"date":"2023-10-31T11:58:48","date_gmt":"2023-10-31T11:58:48","guid":{"rendered":"https:\/\/amm-journal.org\/?p=980"},"modified":"2023-10-31T11:58:48","modified_gmt":"2023-10-31T11:58:48","slug":"photoredox-catalyzed-reaction-as-a-powerful-tool-for-rapid-natural-product-gem-dimethylation-modification-discovery-of-potent-anti-cancer-agents-with-improved-druggability","status":"publish","type":"post","link":"https:\/\/amm-journal.org\/index.php\/2023\/10\/31\/photoredox-catalyzed-reaction-as-a-powerful-tool-for-rapid-natural-product-gem-dimethylation-modification-discovery-of-potent-anti-cancer-agents-with-improved-druggability\/","title":{"rendered":"Photoredox-catalyzed reaction as a powerful tool for rapid natural product Gem-dimethylation modification: discovery of potent anti-cancer agents with improved druggability"},"content":{"rendered":"

Announcing a new publication for Acta Materia Medica<\/em> journal. Tylophorine has diverse biological activities; however, the stability, solubility, and central nervous system toxicity have severely limited use of tylophorine. The\u00a0gem<\/em>-dimethyl group is an organic chemistry functional group that consists of two methyl groups bonded to the same carbon atom. This feature has gained significant attention in medicinal chemistry due to its unique properties and potential applications in drug design.<\/p>\n

The authors of this article applied a new photoredox methodology to tylophorine modification, resulting in a series of gem-dimethyl tylophorine analogues. Among the analogues,\u00a0compound 4b<\/strong>\u00a0demonstrated promising activity against a wide range of tumor cell lines and exhibited significantly improved drug-like properties, including enhanced solubility and stability.\u00a0Compound 4b<\/strong>\u00a0showed an exceptional inhibitory effect (7.8 nM) against a C481S mutation-induced ibrutinib-resistant non-Hodgkin\u2019s lymphoma cell line, as well as primary tumor cell lines obtained from patients. Importantly,\u00a0compound 4b<\/strong>\u00a0exhibited significantly reduced anti-proliferative activity against the normal cell line tested, indicating the potential for an enhanced therapeutic window for\u00a0compound 4b<\/strong>.<\/p>\n

Based on these early-stage data, this study provides a solid foundation for the development of new therapeutic agents for potential drug-resistant cancer treatment in the near future.<\/p>\n

https:\/\/www.scienceopen.com\/hosted-document?doi=10.15212\/AMM-2023-0032<\/a><\/p>\n

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eISSN <\/strong>2737-7946<\/p>\n

Chao Zhang, Yugang Song and Xiuyun Sun et al. Photoredox-catalyzed reaction as a powerful tool for rapid natural product Gem-dimethylation modification: discovery of potent anti-cancer agents with improved druggability.\u00a0Acta Materia Medica.\u00a0<\/em>2023. Vol. 2(4):400-408. DOI: 10.15212\/AMM-2023-0032<\/p>\n","protected":false},"excerpt":{"rendered":"

Announcing a new publication for Acta Materia Medica journal. Tylophorine has diverse biological activities; however, the stability, solubility, and central nervous system toxicity have severely limited use of tylophorine. The\u00a0gem-dimethyl group is an organic chemistry functional group that consists of two methyl groups bonded to the same carbon atom. This feature has gained significant attention […]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[2],"tags":[214,236,235,237],"class_list":["post-980","post","type-post","status-publish","format-standard","hentry","category-news-and-events","tag-anti-cancer","tag-central-nervous-system","tag-gem-dimethyl","tag-natural-product"],"yoast_head":"\nPhotoredox-catalyzed reaction as a powerful tool for rapid natural product Gem-dimethylation modification: discovery of potent anti-cancer agents with improved druggability - AMM Journal<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/amm-journal.org\/index.php\/2023\/10\/31\/photoredox-catalyzed-reaction-as-a-powerful-tool-for-rapid-natural-product-gem-dimethylation-modification-discovery-of-potent-anti-cancer-agents-with-improved-druggability\/\" \/>\n<meta property=\"og:locale\" content=\"en_GB\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Photoredox-catalyzed reaction as a powerful tool for rapid natural product Gem-dimethylation modification: discovery of potent anti-cancer agents with improved druggability - AMM Journal\" \/>\n<meta property=\"og:description\" content=\"Announcing a new publication for Acta Materia Medica journal. 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