Novel ester tethered dihydroartemisinin-3-(oxime/thiosemicarbazide)isatin hybrids as potential anti-breast cancer agents: Synthesis, in vitro cytotoxicity and structure-activity relationship

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 (IC : 1.33-3.84 µM) s...

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Bibliographic Details
Published in:Drug development research 2023-09, Vol.84 (6), p.1175-1182
Main Authors: Liu, Shaohuan, Wang, Shu, Xu, Dan, Pan, Bowen, Chen, Linzhi, Zhao, Shijia, Xu, Zhi, Zhou, Wei
Format: Article
Language:English
Subjects:
Artemisinin
Breast cancer
Cytotoxicity
Dihydroartemisinin
Estrogen receptors
Estrogens
Hybrids
Thiosemicarbazides
Tumor cell lines
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Summary: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 (IC : 1.33-3.84 µM) showed potent activity against triple-negative (MDA-MB-231 and MDA-MB-231/ADR) breast cancer cell lines, and hybrid 7f (IC : 3.90 and 10.18 µM) 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.
ISSN:0272-4391
1098-2299
DOI:10.1002/ddr.22078