Pharmacologic inhibition of the oncogenic protein kinases using small molecules is a
promising strategy to combat several human malignancies. CDK1 is an example of such a …

Title. CDK2 Inhibitors Patent Publication Number. WO 2020/157652 A2 Publication Date.
August 6, 2020 Priority Application. US 62/799,455 and US 62/959,042 Priority Date …

Simple Summary Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal
cancers in humans, due to late diagnosis and limited treatment possibilities. Improved …

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and
thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4 …

Cyclin-dependent kinases play significant roles in cell cycle progression and are promising
targets for cancer therapy. However, most potent CDK inhibitors lack the balance between …

Cyclin-dependent kinases (CDKs) are a group of multifunctional enzymes consisting of
catalytic and regulatory subunits. The regulatory subunit, cyclin, remains dissociated under …

Selective inhibition of cyclin-dependent kinase 8 (CDK8) has been recently regarded as a
potential approach for cancer therapy. A series of novel CDK8 inhibitors with the pyridine …

Abstract Cyclin-dependent kinase 4 (CDK4), which is involved in dynamic regulation of cell
cycle, has gained particularly attention for its role in controlling tumor growth. Increasing …

A fragment library screen was carried out to identify starting points for novel CDK8 inhibitors.
Optimization of a fragment hit guided by co-crystal structures led to identification of a novel …

A novel series of imidazo [4, 5‐c] pyridine‐based CDK2 inhibitors were designed from the
structure of CYC202 via scaffold hopping strategy. These compounds were synthesized and …