On February 1, 2020, Pedatella, Silvana; Cerchia, Carmen; Manfra, Michele; Cioce, Anna; Bolognese, Adele; Lavecchia, Antonio published an article.Reference of tert-Butyl trichloroacetimidate The title of the article was Antitumor agents 7. Synthesis, antiproliferative activity and molecular modeling of new L-lysine-conjugated pyridophenoxazinones as potent DNA-binding ligands and topoisomerase IIα inhibitors. And the article contained the following:
A series of L-lysine-conjugated pyridophenoxazinones (I), (II), (III) and (IV) were designed and synthesized for developing compounds with multimodal anticancer potentialities. All compounds inhibited the proliferation of a panel of human liquid and solid neoplastic cell lines. Compounds I (X = N, Y = CH) and IV (X = N, Y = CH) were the most active compounds with IC50 values in the submicromolar range. UV-vis, 1H NMR, unwinding, and docking experiments demonstrated that they intercalate between the middle 5′-GC-3′ base pairs with the carboxamide side chain lying into major groove. Charge-transfer contribution to the complex stability, evaluated by ab initio calculations, was found to correlate with cytotoxicity. Relaxation and cleavage assays showed that I (X = N, Y = CH) and IV (X = N, Y = CH) selectively target Topo IIα over Topo IIβ and stimulate the formation of covalent Topo II-DNA complexes, functioning as poisons. Moreover, compound IV (X = N, Y = CH) induced DNA damage and arrested MCF-7 cells at the G2/M phase. Altogether, the work provides interesting structure-activity relationships in the pyridophenoxazinone-L-lysine conjugate series and identifies IV (X = N, Y = CH) as a promising candidate for further in vivo evaluation. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Reference of tert-Butyl trichloroacetimidate
The Article related to lysine pyridophenoxazinone synthesis antitumor agent dna damage topoisomerase inhibiting, structure activity antitumor dna binding enzyme inhibiting mol docking, dna lysine pyridophenoxazinone complex, mol structure lysine pyridophenoxazinone hydrogen bond qm ab initio, antiproliferative activity, dna damage, docking studies and other aspects.Reference of tert-Butyl trichloroacetimidate
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