Development of Small Molecules with a Noncanonical Binding Mode to HIV-1 Trans Activation Response (TAR) RNA was written by Abulwerdi, Fardokht A.;Shortridge, Matthew D.;Sztuba-Solinska, Joanna;Wilson, Robert;Le Grice, Stuart F. J.;Varani, Gabriele;Schneekloth, John S.. And the article was included in Journal of Medicinal Chemistry in 2016.COA of Formula: C7H5ClN2 This article mentions the following:
Small mols. that bind to RNA potently and specifically are relatively rare. The study of mols. that bind to the HIV-1 transactivation response (TAR) hairpin, a cis-acting HIV genomic element, has long been an important model system for the chem. of targeting RNA. Here the authors report the synthesis, biochem. and structural evaluation of a series of mols. that bind to HIV-1 TAR RNA. A promising analog, 6-methyl-2-(5-(3-(trifluoromethyl)phenyl)-1,3,4-oxadiazol-2-yl)thieno[2,3-b]pyridin-3-amine (compound 15), retained the TAR binding affinity of the initial hit and displaced a Tat-derived peptide with an IC50 of 40 μM. NMR characterization of a soluble analog, 3-amino-6-methyl-N-(pyridin-4-yl)thieno[2,3-b]pyridine-2-carboxamide (compound 2), revealed a non-canonical binding mode for this class of compounds Finally, evaluation of 2 and 15 by Selective 2′-hydroxyl acylation analyzed by primer extension (SHAPE) indicates specificity in binding to TAR within the context of an in vitro-synthesized 365-nt HIV-1 5′- untranslated region (UTR). Thus, these compounds exhibit a novel and specific mode of interaction with TAR, providing important implications for RNA ligand design. In the experiment, the researchers used many compounds, for example, 2-Chloro-4-methylpyridine-3-carbonitrile (cas: 65169-38-2COA of Formula: C7H5ClN2).
2-Chloro-4-methylpyridine-3-carbonitrile (cas: 65169-38-2) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.COA of Formula: C7H5ClN2