Cdc7 Kinase Inhibitors: 5-Heteroaryl-3-Carboxamido-2-Aryl Pyrroles as Potential Antitumor Agents. 1. Lead Finding was written by Menichincheri, Maria;Albanese, Clara;Alli, Cristina;Ballinari, Dario;Bargiotti, Alberto;Caldarelli, Marina;Ciavolella, Antonella;Cirla, Alessandra;Colombo, Maristella;Colotta, Francesco;Croci, Valter;D’Alessio, Roberto;D’Anello, Matteo;Ermoli, Antonella;Fiorentini, Francesco;Forte, Barbara;Galvani, Arturo;Giordano, Patrizia;Isacchi, Antonella;Martina, Katia;Molinari, Antonio;Moll, Jurgen K.;Montagnoli, Alessia;Orsini, Paolo;Orzi, Fabrizio;Pesenti, Enrico;Pillan, Antonio;Roletto, Fulvia;Scolaro, Alessandra;Tato, Marco;Tibolla, Marcellino;Valsasina, Barbara;Varasi, Mario;Vianello, Paola;Volpi, Daniele;Santocanale, Corrado;Vanotti, Ermes. And the article was included in Journal of Medicinal Chemistry in 2010.Computed Properties of C9H10O3S This article mentions the following:
Cdc7 serine/threonine kinase is a key regulator of DNA synthesis in eukaryotic organisms. Cdc7 inhibition through siRNA or prototype small mols. causes p53 independent apoptosis in tumor cells while reversibly arresting cell cycle progression in primary fibroblasts. This implies that Cdc7 kinase could be considered a potential target for anticancer therapy. We previously reported that pyrrolopyridinones are potent and selective inhibitors of Cdc7 kinase, with good cellular potency and in vitro ADME properties but with suboptimal pharmacokinetic profiles. Here we report on a new chem. class of 5-heteroaryl-3-carboxamido-2-substituted pyrroles that offers advantages of chem. diversification and synthetic simplification. This work led to the identification of (aminopyrimidinyl)phenylpyrrolecarboxamide I, with biochem. data and ADME profile similar to the originally reported pyrrolopyridinones but characterized by superior efficacy in an in vivo model. Derivative I represents a new lead compound worthy of further investigation toward the ultimate goal of identifying a clin. candidate. In the experiment, the researchers used many compounds, for example, Ethyl 3-oxo-3-(thiophen-2-yl)propanoate (cas: 13669-10-8Computed Properties of C9H10O3S).
Ethyl 3-oxo-3-(thiophen-2-yl)propanoate (cas: 13669-10-8) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Computed Properties of C9H10O3S
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics