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Short Paper | Regular issue | Vol 94, No. 6, 2017, pp.1107-1114
Published online, 10th May, 2017
DOI: 10.3987/COM-17-13667
Development of N6-(Heteroarylcarbonyl)adenines as BRD4 Inhibitors

Seika Amemiya, Takao Yamaguchi, Yuichi Hashimoto, and Tomomi Noguchi-Yachide*

*Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan

Abstract

N6-(Heteroarylcarbonyl)adenines were synthesized as candidate BRD4 inhibitors, and their structure-activity relationships were investigated. Among the synthesized compounds, N6-[(3-methoxythiophen-2-yl)carbonyl]adenine (15) showed the most potent BRD4-inhibitory activity.