Bataille, Carole J. R. published the artcileThiazolidine derivatives as potent and selective inhibitors of the PIM kinase family, Synthetic Route of 634905-21-8, the publication is Bioorganic & Medicinal Chemistry (2017), 25(9), 2657-2665, database is CAplus and MEDLINE.
The PIM family of serine/threonine kinases have become an attractive target for anti-cancer drug development, particularly for certain hematol. malignancies. Here, we describe the discovery of a series of inhibitors of the PIM kinase family using a high throughput screening strategy. Through a combination of mol. modeling and optimization studies, the intrinsic potencies and mol. properties of this series of compounds was significantly improved. An excellent pan-PIM isoform inhibition profile was observed across the series, while optimized examples show good selectivity over other kinases. Two PIM-expressing leukemic cancer cell lines, MV4-11 and K562, were employed to evaluate the in vitro anti-proliferative effects of selected inhibitors. Encouraging activities were observed for many examples, with the best example (44) giving an IC50 of 0.75 μM against the K562 cell line. These data provide a promising starting point for further development of this series as a new cancer therapy through PIM kinase inhibition.
Bioorganic & Medicinal Chemistry published new progress about 634905-21-8. 634905-21-8 belongs to piperidines, auxiliary class Piperidine,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (3-(Piperidin-1-yl)phenyl)boronic acid, and the molecular formula is C11H16BNO2, Synthetic Route of 634905-21-8.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem