Development and evaluation of novel artemisinin-isatin hybrids with potential anti-leukemic cytotoxicity.

ABSTRACT: Twenty-one novel ester tethered artemisinin-isatin hybrids were designed, synthesized and screened against human myeloid leukemia cell lines (K562 and K562/ADR), human acute lymphoblastic leukemia cell line (CCRF-CEM) as well as normal human peripheral blood mononuclear cells (PBMCs) for their cytotoxicity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The structure-activity relationships (SARs) were also discussed to facilitate further rational design of more effective candidates. The preliminary results showed that most of the ester tethered artemisinin-isatin hybrids (IC₅₀: 0.32-29.35 µM) exhibited promising activity against CCRF-CEM cells, and some of them (IC₅₀: 1.23-49.84 µM) were also active against K562 and K562/ADR

SUBMITTER: Wang P 

PROVIDER: S-EPMC10140581 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature