Inhibitors of cyclin-dependent kinases as cancer therapeutics

SR Whittaker, A Mallinger, P Workman… - Pharmacology & …, 2017 - Elsevier
Over the past two decades there has been a great deal of interest in the development of
inhibitors of the cyclin-dependent kinases (CDKs). This attention initially stemmed from …

Pyrimidine: a review on anticancer activity with key emphasis on SAR

A Mahapatra, T Prasad, T Sharma - Future journal of pharmaceutical …, 2021 - Springer
Background Cancer is a global health challenge, it impacts the quality of life and its
treatment is associated with several side effects. Resistance of the cancer cells to the …

Iridium-catalyzed C–H borylation of heteroarenes: scope, regioselectivity, application to late-stage functionalization, and mechanism

MA Larsen, JF Hartwig - Journal of the American Chemical …, 2014 - ACS Publications
A study on the iridium-catalyzed C–H borylation of heteroarenes is reported. Several
heteroarenes containing multiple heteroatoms were found to be amenable to C–H borylation …

Overview of CDK9 as a target in cancer research

F Morales, A Giordano - Cell Cycle, 2016 - Taylor & Francis
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 …

Lessons learned from past cyclin-dependent kinase drug discovery efforts

Z Xie, S Hou, X Yang, Y Duan, J Han… - Journal of Medicinal …, 2022 - ACS Publications
Inhibition of cyclin-dependent kinases (CDKs) has become an effective therapeutic strategy
for treating various diseases, especially cancer. Over almost three decades, although great …

Identification of atuveciclib (BAY 1143572), the first highly selective, clinical PTEFb/CDK9 inhibitor for the treatment of cancer

U Lücking, A Scholz, P Lienau, G Siemeister… - …, 2017 - Wiley Online Library
Selective inhibition of exclusively transcription‐regulating PTEFb/CDK9 is a promising new
approach in cancer therapy. Starting from lead compound BAY‐958, lead optimization …

Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity

J Bian, J Ren, Y Li, J Wang, X Xu, Y Feng, H Tang… - Bioorganic …, 2018 - Elsevier
Wogonin is a natural product isolated from the Scutellaria baicalensis and has been proved
to be a potent and selective inhibitor of CDK9. Using this scaffold, we designed and …

The renaissance of cyclin dependent kinase inhibitors

T Ettl, D Schulz, RJ Bauer - Cancers, 2022 - mdpi.com
Simple Summary This review provides an overview of the state of knowledge and general
understanding of CDK inhibitors currently under development or clinically approved, with a …

[HTML][HTML] Selective inhibition of CDK4/6: A safe and effective strategy for developing anticancer drugs

K Yuan, X Wang, H Dong, W Min, H Hao… - … Pharmaceutica Sinica B, 2021 - Elsevier
The sustained cell proliferation resulting from dysregulation of the cell cycle and activation of
cyclin-dependent kinases (CDKs) is a hallmark of cancer. The inhibition of CDKs is a highly …

Revealing quinquennial anticancer journey of morpholine: A SAR based review

F Arshad, MF Khan, W Akhtar, MM Alam… - European journal of …, 2019 - Elsevier
Morpholine, a six-membered heterocycle containing one nitrogen and one oxygen atom, is a
moiety of great significance. It forms an important intermediate in many industrial and …