Highlights•CDK2 has key roles in cell cycle, DNA replication and DNA damage.•Multiple
biomarkers can indicate increased CDK2 activity.•Some cancers have particular …

ABSTRACT CDK9 is a protein in constant development in cancer therapy. Herein we
present an overview of the enzyme as a target for cancer therapy. We provide data on its …

In the current work, a hybridisation strategy was adopted between the privileged building
blocks, benzofuran and piperazine, with the aim of designing novel CDK2 type II inhibitors …

Cancer is one of the major leading causes of death worldwide despite many breakthroughs
in the development of novel anticancer drugs. The heterodimer CDK-Cyclin complex plays …

The piperazine ring system is among the medicinally important nitrogen-containing
heterocyclic ring systems and is exploited for the synthesis of various drug molecules. A …

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 …

Uncontrolled cell proliferation, primarily regulated by cyclin-dependent kinases (CDKs), is a
critical driver of cancer progression, with dysregulation of CDKs contributing to various …

Cyclin-dependent kinases (CDKs) are pivotal kinases in cell cycle transition and gene
transcription. A series of N2, N4-diphenylpyrimidine-2, 4-diamines were previously identified …

2020-01-14 Assigned to Epizyme, Inc. reassignment Epizyme, Inc. ASSIGNMENT OF
ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: PENEBRE, Elayne …

A series of novel LEE011 derivatives containing pyridine N-oxide were designed,
synthesized and evaluated. Systematic study of the structure-activity relationship (SAR) …