Development of Prodrug-Payloads for Targeted Therapeutic Applications of Platinum-Acridine Anticancer Agents.

Authors

Ikeer Y Mancera-Ortiz
Jiangxue Chen
Tyler A Slade, Lehigh Valley Health NetworkFollow
Xiyuan Yao
Shenjie Zhang
Cynthia S Day
Ulrich Bierbach

Publication/Presentation Date

10-18-2023

Abstract

A synthetic platform has been developed that provides access to platinum(IV) prodrugs of highly cytotoxic platinum-acridine anticancer agents and allows them to be incorporated into conjugation-ready prodrug-payloads (PPLs). The PPLs can be conveniently assembled in highly efficient microscale reactions utilizing strain-promoted azide-alkyne cycloaddition chemistry. Model reactions were performed to study the stability of the PPLs in buffers and media and to assess their compatibility with cysteine-maleimide Michael addition chemistry. Amide coupling was a successful strategy to generate a conjugate containing integrin-targeted

Volume

34

Issue

10

First Page

1873

Last Page

1881

ISSN

1520-4812

Published In/Presented At

Mancera-Ortiz, I. Y., Chen, J., Slade, T. A., Yao, X., Zhang, S., Day, C. S., & Bierbach, U. (2023). Development of Prodrug-Payloads for Targeted Therapeutic Applications of Platinum-Acridine Anticancer Agents. Bioconjugate chemistry, 34(10), 1873–1881. https://doi.org/10.1021/acs.bioconjchem.3c00368

Disciplines

Medical Education | Medicine and Health Sciences

PubMedID

37813818

Department(s)

USF-LVHN SELECT Program, USF-LVHN SELECT Program Students

Document Type

Article