Discovery of BET specific bromodomain inhibitors with a novel scaffold was written by Pandit, Navin;Yoo, Miyoun;Hyun Park, Tae;Kim, Jiin;Mi Kim, Seul;Myung Lee, Kyu;Kim, Yeongrin;Min Bong, Seoung;Il Lee, Byung;Jung, Kwan-Young;Hoon Park, Chi. And the article was included in Bioorganic & Medicinal Chemistry in 2022.Category: indole-building-block This article mentions the following:
Bromodomain and extra-terminal domain (BET) proteins have been considered as potent candidates for anti-cancer drug development. As epigenetic readers, they modulate gene expression by recognizing acetylated lysine residues on histones. Therefore, the pharmacol. inhibition of BET proteins has been extensively studied. Herein, we report the novel chem. scaffold of N-(pyridin-2-yl)-1H-benzo[d][1,2,3]triazol-5-amine as BET inhibitors using high-throughput screening assay. Through the anal. of structure-activity relationships, we developed a potent novel compound, which exhibited a better IC50 value about 2-fold compared to iBet762 against the BRD4 bromodomain (BD). The addition of a sulfonyl group to the pyridine ring enhanced the inhibitory activity. Structural studies showed a clear electron d. map for the inhibitor and revealed the structural basis for the critical role of the sulfonyl group in the interaction with BRD4. In the experiment, the researchers used many compounds, for example, 2-(1H-Indol-3-yl)ethanamine (cas: 61-54-1Category: indole-building-block).
2-(1H-Indol-3-yl)ethanamine (cas: 61-54-1) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Category: indole-building-block
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Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles