Developing a Novel Indolocarbazole as Histone Deacetylases Inhibitor against Leukemia Cell Lines. (16th November 2015)

• Record Type: Journal Article
• Authors: Wang, Wenjing; Lv, Maomin; Zhao, Xiong; Zhang, Jingang
• Other Names: Montuori Paolo Academic Editor.
• Is Part Of: Journal of analytical methods in chemistry. Volume 2015(2015)
• Publication Date: 2015-11-16
• Subjects: Chemistry, Analytic -- Periodicals; Chemistry, Analytic -- Technique -- Periodicals; 543.05
• DOI: 10.1155/2015/675053
• Languages: English
• ISSNs: 2090-8865

Abstract

Abstract : A novel indolocarbazole (named as ZW2-1) possessing HDAC inhibition activity was synthesized and evaluated against human leukemia cell lines HL-60 and NB4. ZW2-1 performed anti-population growth effect which was in a concentration-dependent manner (2–12 μ M) by inducing both apoptosis and autophagy in cells. The compound also caused differentiation of HL-60 and NB4 cells as shown by increasing expression of CD11b, CD14, and CD38 at moderate concentration (4 μ M). At relatively high concentration (8 μ M), ZW2-1 significantly decreased intracellular histone deacetylase 1 level which was also observed. All the results indicated that ZW2-1 could be a novel antileukemia lead capable of simultaneously inducing apoptosis, autophagy, and differentiation.