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Molecules 2018, 23(2), 310; https://doi.org/10.3390/molecules23020310

Synthesis of Scutellarein Derivatives with a Long Aliphatic Chain and Their Biological Evaluation against Human Cancer Cells

1
College of Pharmaceutic Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China
2
Engineering Laboratory for National Healthcare Theories and Products of Yunnan Province, Yunnan University of Traditional Chinese Medicine, Kunming 650500, China
3
School of Public Health, Kunming Medical University, Kunming 650500, China
*
Authors to whom correspondence should be addressed.
Received: 14 January 2018 / Revised: 29 January 2018 / Accepted: 30 January 2018 / Published: 1 February 2018
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Scutellarin is the major active flavonoid extracted from the traditional Chinese herbal medicine Erigeron breviscapus (Vant.) Hand-Mazz., which is widely used in China. Recently, accumulating evidence has highlighted the potential role of scutellarin and its main metabolite scutellarein in the treatment of cancer. To explore novel anticancer agents with high efficiency, a series of new scutellarein derivatives with a long aliphatic chain were synthesized, and the antiproliferative activities against Jurkat, HCT-116 and MDA-MB-231 cancer cell lines were assessed. Among them, compound 6a exhibited the strongest antiproliferative effects on Jurkat (IC50 = 1.80 μM), HCT-116 (IC50 = 11.50 μM) and MDA-MB-231 (IC50 = 53.91 μM). In particular, 6a even showed stronger antiproliferative effects than the positive control NaAsO2 on Jurkat and HCT-116 cell lines. The results showed that a proper long aliphatic chain enhanced the antiproliferative activity of scutellarein. View Full-Text
Keywords: scutellarein; scutellarin; flavonoid; cancer; anti-proliferation; long aliphatic chain scutellarein; scutellarin; flavonoid; cancer; anti-proliferation; long aliphatic chain
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Ni, G.; Tang, Y.; Li, M.; He, Y.; Rao, G. Synthesis of Scutellarein Derivatives with a Long Aliphatic Chain and Their Biological Evaluation against Human Cancer Cells. Molecules 2018, 23, 310.

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