Re-Exploring the Anthracycline Chemical Space for Better Anti-Cancer Compounds.

ABSTRACT: The anthracycline anti-cancer drugs are intensely used in the clinic to treat a wide variety of cancers. They generate DNA double strand breaks, but recently the induction of chromatin damage was introduced as another major determinant of anti-cancer activity. The combination of these two events results in their reported side effects. While our knowledge on the structure-activity relationship of anthracyclines has improved, many structural variations remain poorly explored. Therefore, we here report on the preparation of a diverse set of anthracyclines with variations within the sugar moiety, amine alkylation pattern, saccharide chain and aglycone. We assessed the cytotoxicity in vitro in relevant human cancer cell lines, and the capacity to induce DNA- and chromatin damage. This co

SUBMITTER: van Gelder MA 

PROVIDER: S-EPMC10461226 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature