Novel Maleimide Linkers Based on a Piperazine Motif for Strongly Increased Aqueous Solubility.

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Tác giả: Martijn Dijkstra, Anja Federa, Petra Heffeter, Caroline Kast, Bernhard K Keppler, Christian R Kowol, Hemma Schueffl, Alexander Unterlercher

Ngôn ngữ: eng

Ký hiệu phân loại: 305.568 +Alienated and excluded classes

Thông tin xuất bản: United States : ACS omega , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 171994

Maleimides remain very popular conjugation moieties in the fields of bio(in)organic chemistry and biotechnology. They are particularly interesting for endogenous albumin binding in the bloodstream to exploit the enhanced permeability and retention (EPR) effect and to increase tumor accumulation of anticancer drugs. However, during drug development, insufficient aqueous solubility is frequently a limiting factor. In the present study, four new maleimide linkers were synthesized containing a water-soluble piperazine scaffold. Respective maleimide-platinum(IV)-acetato complexes demonstrated similar hydrolytic stability, albumin-binding kinetics,
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