Doctoral Dissertation Themes

Structure-activity relationship study of potential topoisomerase II inhibitors

Project aims at the synthesis and SAR studies of dexrazoxane analogues and other structural types of topoisomerase II (TopII) inhibitors. Several structural types of potential TopII inhibitors will be synthesized and their ability to protect cardiomyocytes against anthracycline toxicity and their ability to inhibit/deplete TopIIa and TopIIb will be evaluated. Structural optimizations will be driven by the results of in vitro studies. Lead compounds that would result from this project will be studied on the rabbit model of chronic anthracycline cardiotoxicity.

Supervisor: doc. PharmDr. Jaroslav Roh, Ph.D.

Keywords: topoisomeráza II; dexrazoxan; vztahy mezi strukturou a účinností; kardioprotektiva

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