Beilstein J. Org. Chem.2018,14, 1583–1594, doi:10.3762/bjoc.14.136
in compounds with increased therapeutic efficacy. The objective of the present study was to examine the cytotoxic effect of anticancer drug–GnRH-conjugates against two essential cardiovascular cell types, such as cardiomyocytes and endothelial cells. Sixteen different previously developed GnRH
: cardiotoxicity; drug targeting; GnRH-conjugates; HCM; HUVEC; impedimetry; Introduction
Gonadotropin-releasing hormone (GnRH) is a peptide hormone secreted by the hypothalamus, which stimulates the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary. Thus, it represents
and Figure 4b–g), whereas the data on short-term effects are presented in Supporting Information File 2. As mentioned above, the modified cytotoxic/cardiotoxic moiety of antitumor drugs in GnRHconjugates is focused in the present work.
Results
Synthesis of GnRH derivative–drug conjugates
In this
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Graphical Abstract
Figure 1:
Chemical structures of the GnRH-drug conjugates synthesized and investigated in the present work. A...