Journal
DRUG DEVELOPMENT RESEARCH
Volume 84, Issue 6, Pages 1175-1182Publisher
WILEY
DOI: 10.1002/ddr.22078
Keywords
breast cancer; dihydroartemisinin; isatin; structure-activity relationship; thiosemicarbazide
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A series of ester tethered dihydroartemisinin-3-(oxime/thiosemicarbazide)isatin hybrids 7a-p were designed, synthesized, and evaluated for their antiproliferative activity against breast cancer cell lines. The hybrids showed potent activity against both drug-sensitive and drug-resistant breast cancers. The structure-activity relationships obtained from this study may aid in the design of more active candidates.
A series of ester tethered dihydroartemisinin-3-(oxime/thiosemicarbazide)isatin hybrids 7a-p were designed, synthesized, and assessed for their antiproliferative activity against MCF-7, MDA-MB-231, MCF-7/ADR, and MDA-MB-231/ADR breast cancer cell lines. Among them, hybrids 7a,f (IC50: 1.33-3.84 mu M) showed potent activity against triple-negative (MDA-MB-231 and MDA-MB-231/ADR) breast cancer cell lines, and hybrid 7f (IC50: 3.90 and 10.18 mu M) also demonstrated promising activity against estrogen receptor-positive breast cancer cells (MCF-7 and MCF-7/ADR), and the activity was superior to these of artemisinin, dihydroartemisinin, and ADR, revealing their potential to fight against both drug-sensitive and drug-resistant breast cancers. The enriched structure-activity relationships may facilitate further design of more active candidates.
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