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. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is γ-valerolactone.Synthetic Route of C4H7NS
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics