The Anti-Breast Cancer Potential of Bis-Isatin Scaffolds

Author(s): Hua Guo*, Quan-Ping Diao

Journal Name: Current Topics in Medicinal Chemistry

Volume 20 , Issue 16 , 2020

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Graphical Abstract:


Aim: To develop novel anti-breast cancer agents and discuss the structure-activity relationship of bis-isatin scaffolds.

Background: Breast cancer is the most common invasive cancer and the second leading cause of cancer death in women after lung cancer. Bis-isatin scaffolds possess potential anti-breast cancer activity, and some of them such as Indirubin could induce cancer cells apoptosis via multiply mechanisms.

Objective: The primary objective of this study was to evaluate the potential of bis-isatin scaffolds with alkyl/ether linkers between the two isatin moieties against different human breast cancer cell lines including MCF-7, AU565, MDA-MB-231, MDA-MB-435 and MDA-MB-468 cells.

Methods: The synthesized bis-isatin scaffolds with alkyl/ether linker between the two isatin moieties were evaluated for their in vitro activity against MCF-7, AU565, MDA-MB-231, MDA-MB-435, and MDA-MB-468 human breast cancer cell lines by MTT assay.

Results: All the synthesized compounds (IC50: 38.3-197.6 µM) possess considerable activity against MCF-7, AU565, MDA-MB-231, MDA-MB-435, and MDA-MB-468 human breast cancer cell lines, and the most potent compound 4e (IC50: 38.3-63.5 µM) was no inferior to Cisplatin (IC50: 20.1-38.6 μM) against the five tested human breast cancer cell lines.

Conclusion: All the synthesized bis-isatin scaffolds were active against a panel of breast cancer cell lines, highlighting the significance of exploring the bis-isatin scaffolds to fight against breast cancers. The enriched structure-activity relationship may set up the direction for the rational design and development of novel bis-isatin scaffolds with higher efficiency.

Keywords: Bis-isatin, Breast cancer, Structure-activity relationships, Alkyl/ether linkers, Cisplatin, Nintedanib.

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Article Details

Year: 2020
Page: [1499 - 1503]
Pages: 5
DOI: 10.2174/1568026620666200310124416
Price: $65

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