The rapidly growing interest in the literature about the anticancer activity of 3,5-disubstituted pyrazolines and their promising therapeutic potentials/pharmacological properties, supported by the number of pyrazoline derivatives currently in clinical use or clinical trials, encouraged us to review the antiproliferative effects and biochemical investigations of probable mechanisms of action. Nevertheless, many reported pyrazoline-bearing compounds have anticancer activity without an explored mode of action, which opens new research avenues to examine their biochemical profiles further. Therefore, 3,5-disubstituted pyrazoline is a promising core that can be used to design new derivatives with anticancer activity based on the structure-activity relationship summarized in this review to obtain higher potency and selectivity.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1080/17568919.2025.2476393 | DOI Listing |
Dalton Trans
March 2025
Institute of Flow Chemistry and Engineering, School of Chemistry and Materials, Jiangxi Normal University, Nanchang 330022, China.
Platinum-based chemotherapy, despite being a cornerstone of cancer treatment, faces significant challenges due to acquired drug resistance. To address this issue, we have designed three organelle-targeting platinum(IV) prodrugs conjugated with BODIPY fluorophores, enabling spatiotemporal control through green light irradiation. These BODIPY-Pt(IV) conjugates exhibit excellent stability in PBS buffer, demonstrating resilience under physiological conditions.
View Article and Find Full Text PDFFASEB J
March 2025
Department of Gerontology and Geriatrics, Shengjing Hospital of China Medical University, Shenyang, Liaoning, China.
Neuron-derived clone 77 (Nur77), a member of the orphan nuclear receptor family, is expressed and activated rapidly in response to diverse physiological and pathological stimuli. It exerts complex biological functions, including roles in the nervous system, genome integrity, cell differentiation, homeostasis, oxidative stress, autophagy, aging, and infection. Recent studies suggest that Nur77 agonists alleviate symptoms of neurodegenerative diseases, highlighting its potential as a therapeutic target in such conditions.
View Article and Find Full Text PDFJ Biomol Struct Dyn
March 2025
Applied Organic Chemistry Department, National Research Center, Dokki, Egypt.
The discovery of novel, selective inhibitors targeting CDK2 and PIM1 kinases, which regulate cell survival, proliferation, and treatment resistance, is crucial for advancing cancer therapy. This study reports the design, synthesis, and biological evaluation of three novel pyrazolo[3,4-]pyridine derivatives (), confirmed spectral analyses. These compounds were assessed for anti-cancer activity against breast, colon, liver, and cervical cancers using the MTT assay.
View Article and Find Full Text PDFFuture Med Chem
March 2025
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
The rapidly growing interest in the literature about the anticancer activity of 3,5-disubstituted pyrazolines and their promising therapeutic potentials/pharmacological properties, supported by the number of pyrazoline derivatives currently in clinical use or clinical trials, encouraged us to review the antiproliferative effects and biochemical investigations of probable mechanisms of action. Nevertheless, many reported pyrazoline-bearing compounds have anticancer activity without an explored mode of action, which opens new research avenues to examine their biochemical profiles further. Therefore, 3,5-disubstituted pyrazoline is a promising core that can be used to design new derivatives with anticancer activity based on the structure-activity relationship summarized in this review to obtain higher potency and selectivity.
View Article and Find Full Text PDFOrg Biomol Chem
March 2025
Univ Rouen Normandie, INSA Rouen Normandie, Univ Caen Normandie, ENSICAEN, CNRS, Institut CARMeN UMR 6064, F-76000 Rouen, France.
A visible-light-mediated chlorotrifluoromethylation catalyzed by a copper-based photo-redox catalyst of internal alkenes is reported. The reaction proceeds with complete regioselectivity under mild reaction conditions using commercially available FCSOCl as both the trifluoromethyl and chlorine source, leading to the synthesis of added-value chemicals with atom-economy. A vast array of internal alkenes were functionalized in decent to good yields, highlighting a great tolerance to various functional groups.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!