Eur J Med Chem 2021 Oct 24;221:113521. Epub 2021 May 24.
Blokhin Cancer Center, 24 Kashirskoye Shosse, Moscow, 115478, Russia; Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow, 119021, Russia.
The anthraquinone scaffold has long been known as a source of efficacious antitumor drugs. In particular, the various chemical modifications of the side chains in this scaffold have yielded the compounds potent for the wild type tumor cells, their counterparts with molecular determinants of altered drug response, as well as in vivo settings. Further exploring the chemotype of anticancer heteroarene-fused anthraquinones, we herein demonstrate that derivative of anthra[2,3-b]thiophene-2-carboxamide, (compound 8) is highly potent against a panel of human tumor cell lines and their drug resistant variants. Read More