Real-world clinical multi-omics analyses reveal bifurcation of ER-independent and ER-dependent drug resistance to CDK4/6 inhibitors

Nature Communications, Journal Year: 2025, Volume and Issue: 16(1)

Published: Jan. 22, 2025

Language: Английский

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Novel Nano-sized N-Thiazolylpyridylamines Targeting CDK2: Design, Divergent Synthesis, Conformational Studies, and Multifaceted In Silico Analysis

Chemico-Biological Interactions, Journal Year: 2025, Volume and Issue: unknown, P. 111366 - 111366

Published: Jan. 1, 2025

Language: Английский

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Novel Bicyclic Amines as CDK2 Inhibitors for Treating Metastatic Breast Cancer or Metastatic Lung Cancer

ACS Medicinal Chemistry Letters, Journal Year: 2025, Volume and Issue: 16(2), P. 198 - 199

Published: Jan. 16, 2025

Provided herein are novel bicyclic amines as CDK2 inhibitors, pharmaceutical compositions, use of such compounds in treating metastatic breast cancer or lung and processes for preparing compounds.

Language: Английский

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Beyond failure of endocrine-based therapies in HR+/HER2 negative advanced breast cancer: what before chemotherapy? A glimpse into the future.

Critical Reviews in Oncology/Hematology, Journal Year: 2025, Volume and Issue: 208, P. 104634 - 104634

Published: Feb. 1, 2025

Language: Английский

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Design, Synthesis and Evaluation of Quinazoline-Chalcone Hybrids as Inducers of Cell-Cycle Arrest and Apoptosis in Breast Cancer via DNA Damage and CDK2/ATR Inhibition

European Journal of Medicinal Chemistry Reports, Journal Year: 2025, Volume and Issue: unknown, P. 100250 - 100250

Published: Feb. 1, 2025

Language: Английский

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Discovery of potent and selective CDK2 inhibitors with high safety and favorable bioavailability for the treatment of cancer

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 290, P. 117503 - 117503

Published: March 13, 2025

Language: Английский

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Recent advances in regulating the cell cycle through inhibiting CDKs for cancer treatment

Chinese Journal of Natural Medicines, Journal Year: 2025, Volume and Issue: 23(3), P. 286 - 298

Published: March 1, 2025

Language: Английский

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Design, synthesis, and anticancer evaluation of novel coumarin/thiazole congeners as potential CDK2 inhibitors with molecular dynamics

RSC Advances, Journal Year: 2024, Volume and Issue: 14(27), P. 18838 - 18855

Published: Jan. 1, 2024

A series of novel coumarin-thiazoles was designed and synthesized as a possible CDK2 inhibitor with anticancer activity low toxicity. The design relied on having hydrazine thiazole or its open-form thioamide to form H-bonds the ATP binding site while coumarin maintained crucial hydrophobic interactions for proper fitting. biological evaluation revealed that hydroxycoumarin-thiazole derivative 6c demonstrated best inhibition HepG2 HCT116 IC50 2.6 3.5 μM, respectively. Similarly, open chain congener 5c exhibited potent MCF-7 4.5 5.4 Molecular docking simulations supported assumption inhibiting by preserving interaction pattern hinge surrounding (HPO) side chains. Furthermore, molecular dynamics established satisfactory stability affinity within active site.

Language: Английский

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Recent advancement in developing small molecular inhibitors targeting key kinase pathways against triple-negative breast cancer

Bioorganic & Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 112, P. 117877 - 117877

Published: Aug. 18, 2024

Triple-negative breast cancer (TNBC) stands out as the most formidable variant of cancer, predominantly affecting younger women and characterized by a bleak outlook high likelihood spreading. The absence safe effective targeted treatments leaves standard cytotoxic chemotherapy primary option. role protein kinases, frequently altered in many cancers, is significant advancement drug resistance TNBC, making them logical target for creating new, potent therapies against TNBC. Recently, an array promising small molecules aimed at various kinases have been developed specifically with combination studies showing synergistic improvement combatting this condition. This review underscores effectiveness molecule kinase inhibitors battling lethal form sheds light on prospective pathways crafting novel treatments.

Language: Английский

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Advances in Cancer Therapy: A Comprehensive Review of CDK and EGFR Inhibitors

Cells, Journal Year: 2024, Volume and Issue: 13(19), P. 1656 - 1656

Published: Oct. 6, 2024

Protein kinases have essential responsibilities in controlling several cellular processes, and their abnormal regulation is strongly related to the development of cancer. The implementation protein kinase inhibitors has significantly transformed cancer therapy by modifying treatment strategies. These received substantial FDA clearance recent decades. emerged as primary objectives for therapeutic interventions, particularly context treatment. At present, 69 therapeutics been approved that target approximately 24 kinases, which are specifically prescribed neoplastic illnesses. novel agents inhibit certain such receptor protein-tyrosine protein-serine/threonine dual-specificity nonreceptor kinases. This review presents a comprehensive overview targets inhibitors, with specific focus on cyclin-dependent (CDKs) epidermal growth factor (EGFR). majority reviewed studies commenced an assessment cell lines concluded biological evaluation individual targets. articles provide detailed information structural features potent anticancer activity, refers ability selectively cancer-promoting including CDKs EGFR. Additionally, latest FDA-approved targeting these enzymes were highlighted accordingly.

Language: Английский

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