Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors

Bioorganic & Medicinal Chemistry Letters
Yan FuHuixin Wan

Abstract

The discovery of a class of diheteroaromatic amines based on LY2835219 as cyclin-dependent kinase (CDK1/4/6) inhibitors was described. The series was found to have much more improved CDK1 inhibition and potent in vitro anti-proliferative effects against cancer cell lines. The synthesis and structure-activity relationship studies of these compounds were reported. One promising compound was selected to evaluate as a novel lead compound after in vitro and in vivo profiling.

Citations

Jun 27, 2019·Medicinal Chemistry·Jiajia MouYanru Deng
Jul 25, 2020·European Journal of Medicinal Chemistry·Brilliant N MarakVed Prakash Singh
Apr 4, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Alessandra AmmazzalorsoMarialuigia Fantacuzzi

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cell Checkpoints & Regulators

Cell cycle checkpoints are a series of complex checkpoint mechanisms that detect DNA abnormalities and ensure that DNA replication and repair are complete before cell division. They are primarily regulated by cyclins, cyclin-dependent kinases, and the anaphase-promoting complex/cyclosome. Here is the latest research.