5-Keto-3-cyano-2,4-diaminothiophenes as selective maternal embryonic leucine zipper kinase inhibitors was written by Boutard, Nicolas;Sabiniarz, Aleksandra;Czerwinska, Klaudia;Jarosz, Malgorzata;Cierpich, Anna;Kolasinska, Ewa;Wiklik, Katarzyna;Gluza, Karolina;Commandeur, Claude;Buda, Anna;Stasiowska, Agata;Bobowska, Aneta;Galek, Mariusz;Fabritius, Charles-Henry;Bugaj, Marta;Palacz, Edyta;Mazan, Andrzej;Zarebski, Adrian;Krawczynska, Karolina;Zurawska, Malgorzata;Zawadzki, Przemyslaw;Milik, Mariusz;Wegrzyn, Paulina;Dobrzanska, Monika;Brzozka, Krzysztof;Kowalczyk, Piotr. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Synthetic Route of C4H7NS The following contents are mentioned in the article:
Maternal embryonic leucine zipper kinase (MELK) is involved in several key cellular processes and displays increased levels of expression in numerous cancer classes (colon, breast, brain, ovary, prostate and lung). Although no selective MELK inhibitors have yet been approved, increasing evidence suggest that inhibition of MELK would constitute a promising approach for cancer therapy. A weak high-throughput screening hit (17, IC50 â?5 μM) with lead-like properties was optimized for MELK inhibition. The early identification of a plausible binding mode by mol. modeling offered guidance in the choice of modifications towards compound 52 which displayed a 98 nM IC50. A good selectivity profile was achieved for a representative member of the series (29) in a 486 protein kinase panel. Future elaboration of 52 has the potential to deliver compounds for further development with chemotherapeutic aims. This study involved multiple reactions and reactants, such as Isopropylisothiocyanate (cas: 2253-73-8Synthetic Route of C4H7NS).
Isopropylisothiocyanate (cas: 2253-73-8) 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. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Synthetic Route of C4H7NS
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics