AI Article Synopsis
- A series of new compounds called ester tethered dihydroartemisinin-3-(oxime/thiosemicarbazide)isatin hybrids (7a-p) were created to study their effects on breast cancer cells.
- Some of these hybrids (specifically 7a and 7f) showed strong anti-cancer activity, particularly against difficult cases of triple-negative breast cancer.
- The results indicate that these new compounds might be more effective than existing treatments like artemisinin and ADR, suggesting they could be useful for both drug-sensitive and drug-resistant breast cancer cases.
Article Abstract
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.
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| http://dx.doi.org/10.1002/ddr.22078 | DOI Listing |
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