CDK9 inhibitors in cancer research

Z Huang, T Wang, C Wang, Y Fan - RSC Medicinal Chemistry, 2022 - pubs.rsc.org
Cyclin dependent kinase 9 (CDK9) plays an essential role in regulating transcriptional
elongation. Aberrations in CDK9 activity have been observed in various cancers, which …

Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic Indications

Y Zhang, L Shan, W Tang, Y Ge, CX Li… - Journal of Medicinal …, 2024 - ACS Publications
CDK9 is a cyclin-dependent kinase that plays pivotal roles in multiple cellular functions
including gene transcription, cell cycle regulation, DNA damage repair, and cellular …

Ligand-and structure-based identification of novel CDK9 inhibitors for the potential treatment of leukemia

H Zhang, J Huang, R Chen, H Cai, Y Chen, S He… - Bioorganic & Medicinal …, 2022 - Elsevier
Abstract Cyclin-dependent kinase 9 (CDK9) plays a vital role in controlling cell transcription
and has been an attractive target for cancer treatment. Herein, ten predictive models derived …

Aminopyridone-linked benzimidazoles: a fragment-based drug design for the development of CDK9 inhibitors

EM Husseiny, HS Abulkhair, SSA El-Hddad… - Future Medicinal …, 2023 - Taylor & Francis
Aim: A fragment-based design and synthesis of three novel series of aminopyridone-linked
benzimidazoles as potential anticancer candidates with significant CDK9 inhibition was …

Construction of a Pyrimidine Framework through [3 + 2 + 1] Annulation of Amidines, Ketones, and N,N-Dimethylaminoethanol as One Carbon Donor

Z Qin, Y Ma, F Li - The Journal of Organic Chemistry, 2021 - ACS Publications
An efficient, facile, and eco-friendly synthesis of pyrimidine derivatives has been developed.
It involves a [3+ 2+ 1] three-component annulation of amidines, ketones, and one carbon …

Design, synthesis and anticancer evaluation of selective 2, 4-disubstituted pyrimidine CDK9 inhibitors

Z Xu, B Zhang, Z Liu, S Gou - European Journal of Medicinal Chemistry, 2022 - Elsevier
Specific inhibition on CDK9 has been proven to be a promising targeted cancer therapy. In
this work, fourteen novel 2, 4-disubstituted pyrimidine derivatives were designed and …

Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer

L Wu, W Liu, Y Huang, C Zhu, Q Ma, Q Wu… - European Journal of …, 2022 - Elsevier
CDK2/9 are members of the CDKs family, which play key roles in the occurrence and
development of many cancers by regulating cell cycle and transcriptional prolongation …

Copper-Free Halodediazoniation of Arenediazonium Tetrafluoroborates in Deep Eutectic Solvents-like Mixtures

G Ghigo, M Bonomo, A Antenucci, C Reviglio… - Molecules, 2022 - mdpi.com
Deep Eutectic Solvent (DES)-like mixtures, based on glycerol and different halide organic
and inorganic salts, are successfully exploited as new media in copper-free …

Combined In Silico and In Vitro Evidence Supporting an Aurora A Kinase Inhibitory Role of the Anti-Viral Drug Rilpivirine and an Anti-Proliferative Influence on …

S Islam, T Teo, M Kumarasiri, M Slater, JH Martin… - Pharmaceuticals, 2022 - mdpi.com
The global burden of cancer necessitates rapid and ongoing development of effective
cancer therapies. One promising approach in this context is the repurposing of existing non …

Unveiling the promise of pyrimidine-modified CDK inhibitors in cancer treatment

R Dubey, R Makhija, A Sharma, A Sahu, V Asati - Bioorganic Chemistry, 2024 - Elsevier
Cyclin-dependent kinases (CDKs) constitute a vital family of protein-serine kinases, pivotal
in regulating various cellular processes such as the cell cycle, metabolism, proteolysis, and …