Sun, Tao; Lv, Tian; Wu, Jianbing; Zhu, Mingchao; Fei, Yue; Zhu, Jie; Zhang, Yihua; Huang, Zhangjian published the artcile< General Strategy for Integrated Bioorthogonal Prodrugs: Pt(II)-Triggered Depropargylation Enables Controllable Drug Activation In Vivo>, Synthetic Route of 4064-06-6, the main research area is bioorthogonal prodrug decaging platinum triggered depropargylation controllable drug activation.
Bioorthogonal decaging reactions for controllable drug activation within complex biol. systems are highly desirable yet extremely challenging. Herein, we find a new class of Pt(II)-triggered bioorthogonal cleavage reactions in which Pt(II) but not Pt(IV) complexes effectively trigger the cleavage of O/N-propargyl in a variety of ranges of caged mols. under biocompatible conditions. Based on these findings, we propose a general strategy for integrated bioorthogonal prodrugs and accordingly design a prodrug 16 (I), in which a Pt(IV) moiety is covalently connected with an O2-propargyl diazeniumdiolate moiety. It is found that I can be specifically reduced by cytoplasmic reductants in human ovarian cancer cells to liberate cisplatin, which subsequently stimulates the cleavage of O2-propargyl to release large amounts of NO in situ, thus generating synergistic and potent tumor suppression activity in vivo. Therefore, Pt(II)-triggered depropargylation and the integration concept might provide a general strategy for broad applicability of bioorthogonal cleavage chem. in vivo.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 4064-06-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H20O6, Synthetic Route of 4064-06-6.
Referemce:
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Alcohols – Chemistry LibreTexts