Development of Selective Clk1 and -4 Inhibitors for Cellular Depletion of Cancer-Relevant Proteins was written by ElHady, Ahmed K.;Abdel-Halim, Mohammad;Abadi, Ashraf H.;Engel, Matthias. And the article was included in Journal of Medicinal Chemistry in 2017.COA of Formula: C10H8O3S This article mentions the following:
In cancer cells, kinases of the Clk family control the supply of full-length, functional mRNAs coding for a variety of proteins essential to cell growth and survival. Thus, inhibition of Clks might become a novel anticancer strategy, leading to a selective depletion of cancer-relevant proteins after turnover. On the basis of a Weinreb amide hit compound, the authors designed and synthesized a diverse set of methoxybenzothiophene-2-carboxamides, of which the N-benzylated derivative showed enhanced Clk1 inhibitory activity. Introduction of a m-fluorine in the benzyl moiety eventually led to the discovery of compound 21b (5-methoxybenzo[b]thiophene-2-carboxylic acid (3-fluorobenzyl)methylamide), a potent inhibitor of Clk1 and -4 (IC50 = 7 and 2.3 nM, resp.), exhibiting an unprecedented selectivity over Dyrk1A. Compound 21b triggered the depletion of EGFR, HDAC1, and p70S6 kinase from the cancer cells, with potencies in line with the measured GIC50 values. In contrast, the cellular effects of congener 21a (5-methoxybenzo[b]thiophene-2-carboxylic acid 3-fluorobenzylamide), which inhibited Clk1 only weakly, were substantially lower. In the experiment, the researchers used many compounds, for example, 5-Methoxybenzo[b]thiophene-2-carboxylic acid (cas: 23046-02-8COA of Formula: C10H8O3S).
5-Methoxybenzo[b]thiophene-2-carboxylic acid (cas: 23046-02-8) belongs to benzothiophene derivatives. Benzothiophene finds use in research as a starting material for the synthesis of larger, usually bioactive structures. It is found within the chemical structures of pharmaceutical drugs such as raloxifene, zileuton, and sertaconazole, and also BTCP.COA of Formula: C10H8O3S
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem