Design, synthesis and anticancer/antiestrogenic activities of novel indole-benzimidazoles was written by Karadayi, Fikriye Zengin;Yaman, Murat;Kisla, Mehmet Murat;Keskus, Ayse G.;Konu, Ozlen;Ates-Alagoz, Zeynep. And the article was included in Bioorganic Chemistry in 2020.COA of Formula: C9H6ClNO This article mentions the following:
In this study, a novel ethylsulfonyl indole-benzimidazole derivatives I [R1 = H, Me, cyclohexyl, etc.; R2 = H, MeO, Cl, Br] were synthesized. Subsequently, 1H NMR, 13C NMR, and Mass spectral and in silico docking analyses, and anticancer activity screening studies of these novel indole-benzimidazoles were performed. The antiproliferative effects of indole-benzimidazoles I were found to be more similar between the estrogen (E2) responsive cell lines MCF-7 and HEPG2 in comparison to the Estrogen Receptor neg. (ER–) cell line MDA-MB-231. Microarray expression profiling and gene enrichment analyses (GSEA) of the selected compounds I [R1 = 4-fluorobenzyl, R2 = H, MeO, Cl, Br; R1 = 3,4-difluorobenzyl, R2 = MeO] helped determine the similarly modulated cellular signaling pathways among derivatives Moreover, some known compounds were identified that had significantly similar gene signatures to that of I [R1 = 4-fluorobenzyl; R2 = Br] via queries performed in LINCS database; and further transcriptomics comparisons were made using public GEO datasets (GSE35428, GSE7765, GSE62673). Results strongly demonstrated that these novel indole-benzimidazoles can modulate ER target gene expression as well as dioxin-mediated aryl hydrocarbon receptor and amino acid deprivation-mediated integrated stress response signaling in a dose-dependent manner. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0COA of Formula: C9H6ClNO).
5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.COA of Formula: C9H6ClNO
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