Synthesis and evaluation of RNase L-binding 2-aminothiophenes as anticancer agents was written by Hwang, Jimin;Qiu, Xiaqiu;Borgelt, Lydia;Haacke, Neele;Kanis, Laurin;Petroulia, Stavroula;Gasper, Raphael;Schiller, Damian;Lampe, Philipp;Sievers, Sonja;Imig, Jochen;Wu, Peng. And the article was included in Bioorganic & Medicinal Chemistry in 2022.Category: chlorides-buliding-blocks The following contents are mentioned in the article:
Aminothiophene is a scaffold that is widely present in drugs and biol. active small mols. as chem. probes. In this study, 43 compounds sharing a 2-aminothiophenone-3-carboxylate (ATPC) scaffold, known to activate the RNase L (RNase L), were synthesized and selected ATPCs showed enhancement of thermal stability of RNase L upon binding. Screening of antiproliferation activities against human cancer cell lines revealed that ATPCs represented by compounds 4l and 50 showed potent single-digit micromolar antiproliferation activity against human cancer cell lines. Compounds 4l and 50 exhibited time- and dose-dependent proliferation inhibition, induced cellular apoptosis measured by cleaved PARP and via flow cytometry, inhibited cell migration, and inhibited cell colony formation. Combining the results reported in this work, ATPCs were evaluated as potential anticancer agents mediated by RNase L-binding and apoptosis induction. The work contributes to the study on the polypharmacol. properties of aminothiophene-containing small mols. This study involved multiple reactions and reactants, such as Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3Category: chlorides-buliding-blocks).
Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics