Synthesis of some steroidal mitocans of nanomolar cytotoxicity acting by apoptosis

  • Eur J Med Chem. 2020 Aug 1;199:112425. doi: 10.1016/j.ejmech.2020.112425.
Immo Serbian  1 ,  Sophie Hoenke  1 ,  René Csuk  2
Affiliations
  • 1. Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany.
  • 2. Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany. Electronic address: [email protected].
PMID: 32422522 DOI: 10.1016/j.ejmech.2020.112425
Abstract

Several Steroids (abiraterone, prednisone, testosterone, Cholesterol) and the Bcl-2 Inhibitor bexarotene were used as starting Materials to synthesize iperazinyl-spacered rhodamine B conjugates. The conjugates were screened for their cytotoxicity in SRB assays against several human tumor cell lines and found to be active in a low μM to nM range. The conjugate derived from testosterone held an EC50 = 59 nM against MCF-7 tumor cells and acted mainly by necrosis. The prednisone conjugate, however, was less cytotoxic but acted mainly by Apoptosis and held a moderate selectivity against MCF-7 tumor cells.

Keywords
Apoptosis; Cytotoxicity; Prednisone; Rhodamine B; Steroids; Synthesis.
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