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. Author manuscript; available in PMC: 2021 Jul 9.
Published in final edited form as: J Med Chem. 2020 Jun 15;63(13):7186–7210. doi: 10.1021/acs.jmedchem.0c00456

Figure 4.

Figure 4.

Inhibition of growth and transcriptional regulation of MCF-7:CFR cells by 27 compared to other BET inhibitors: (A) comparison of compound 27 with benchmark BET inhibitors in cell proliferation assay of MCF-7:CFR 2D cell cultures showing resistance to fulvestrant and 4OHT (TAM) (1 μM); (B) heatmap comparing gene expression changes among control (DMSO), 27 (100 nM), and 1 (100 nM) treated MCF-7:CFR cells after 24 h; (C) volcano plot showing top 10 downregulated genes from RNA-seq comparing 27 with vehicle control; (D) log 2-fold change of significantly regulated oncogenes and tumor suppressors in various oncogenic (Myc, cell cycle) and apoptotic pathways; (E) representative images on day 9 of treatment with DMSO (0.01%), fulvestrant (100 nM), JQ1 (1, 100 nM), AZD5153 (5, 100 nM), and compound 27 (10 and 100 nM) in MCF7:CFR 3D spheroids; scale bar = 1 mm.