Two-carbon tethered artemisinin-isatin hybrids: design, synthesis, anti-breast cancer potential, and in silico study.

ABSTRACT: Eleven two-carbon tethered artemisinin-isatin hybrids (4a-k) were designed, synthesized, and evaluated for their antiproliferative activity against MCF-7, MDA-MB-231, and MDA-MB-231/ADR breast cancer cell lines, as well as cytotoxicity toward MCF-10A cells in this paper. Among them, the representative hybrid 4a (IC₅₀: 2.49-12.6 µM) was superior to artemisinin (IC₅₀: 72.4->100 µM), dihydroartemisinin (IC₅₀: 69.6-89.8 µM), and Adriamycin (IC₅₀: 4.46->100 µM) against the three tested breast cancer cell lines. The structure-activity relationship revealed that the length of the alkyl linker between artemisinin and isatin was critical for the activity, so further structural modification could focus on evaluatio

SUBMITTER: Wang R 

PROVIDER: S-EPMC10620963 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature