Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity. Issue 15 (1st August 2016)

• Record Type: Journal Article
• Authors: Yang, Chao; Chen, Hui; Lu, Shihai; Zhang, Meng; Tian, Wei; Wang, Mingping; Zhang, Ling; Song, Yunlong; Shen, Aijun; Zhou, Youjun; Zhu, Ju; Zheng, Canhui
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 15(2016)
• Page Start: 3464
• Page End: 3467
• Publication Date: 2016-08-01
• Subjects: Luteolin -- Flos Chrysanthemi -- Structural modification -- Bcl-2 protein -- Anti-tumor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.06.043
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The luteolin from Flos Chrysanthemi was found to directly bind to the Bcl-2 protein and inhibit the tumor cell growth in our previous study. However, it has been shown to possess wide and week biological activities. In this study, a series of derivatives of luteolin were designed and synthesized, and their tumor cell growth inhibitory activities were evaluated against human leukemia cell line HL-60. The results showed that compounds1B-2, 2A-3, and2B-5, with hydrophobic substituted benzyl groups introduced to B ring and hydrogen or methyl introduced to 7-OH group of luteolin, exhibited the strongest inhibitory activity with the IC50 lower than 10 μM, which were significantly more potent than luteolin. The studies presented here offer a good example for modifications of flavones to improve their tumor cell growth inhibitory activities.