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1. The investigation and bioorthogonal anticancer activity enhancement of a triphenylphosphine-labile prodrug of seleno-combretastatin-4.

Author

Hou L, Huang W, Cheng J, Deng X, Lai H, Chen Z, Zhan Z, Feng P, Li Y, Yang F, and Chen T

Subjects
Antineoplastic Agents pharmacology, Cell Membrane Permeability, Dose-Response Relationship, Drug, Drug Liberation, Drug Screening Assays, Antitumor, Human Umbilical Vein Endothelial Cells, Humans, Intercellular Signaling Peptides and Proteins metabolism, Prodrugs pharmacology, Vascular Endothelial Growth Factor A metabolism, Antineoplastic Agents chemistry, Bibenzyls chemistry, Organophosphorus Compounds chemistry, Organoselenium Compounds chemistry, Prodrugs chemistry
Abstract

Here, a triphenylphosphine (TPP)-labile prodrug of seleno-combretastatin-4 (CSeD) was designed and synthesized. A detailed investigation revealed that CSeD, which was shown to be very safe in circulating blood, could react with TPP to release CA-4 and a selenodiazole derivative, with accompanying powerful anticancer and antiangiogenesis effects, as well as radiosensitization properties.

Published
2020
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