Synthesis and cytotoxicity of diarylpentanoids against sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells

Chem Biodivers. 2021 Dec 6. doi: 10.1002/cbdv.202100451. Online ahead of print.

ABSTRACT

This paper describes the synthesis and biological investigation of a series of symmetric diarylpentanoids, characterized by a dienone moiety and by a different pattern of substitution on the two phenyl rings. The series of compounds 1a-p were tested against drug-sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 cells to evaluate their cytotoxicity profile, and all the diarypentanoids revealed to be active against both the leukemia cell lines, with the best activity shown by compound 1o that showed a submicromolar activity against both CCRF-CEM and CEM/ADR5000 cell lines (EC 50 =0.54 and 0.25 µM, respectively).

PMID:34871465 | DOI:10.1002/cbdv.202100451