The Pyrazole Scaffold in Anticancer Drug Discovery: A Review of Synthetic Approaches, Structure-Activity Relationships, and Target-Based Mechanism of Action. [PDF]
K R K +5 more
europepmc +1 more source
Design and Synthesis of Pyrimidino[4,5‐d]Pyrimidine‐Based Compounds as Potent B‐RAF V600E Inhibitors
Novel pyrimido[4,5‐d]pyrimidine‐based inhibitors selectively target B‐RAF V600E with nanomolar affinity and adopt distinct type‐II binding modes. Complementary cellular profiling reveals highly active analogs, underscoring the versatility of this chemotype and establishing it as a promising scaffold for the development of next‐generation kinase ...
Eleftheria A. Georgiou +10 more
wiley +1 more source
Synthesis and Antiproliferative Activity of Fluorinated <i>N</i>-Acetylmannosamine Analogs. [PDF]
Krčil A +8 more
europepmc +1 more source
Probing 3‐Amino‐2H‐Azaindazoles as Allosteric Inhibitors of the Protein Tyrosine Phosphatase SHP2
A palladium‐catalyzed domino reaction facilitated the discovery and rapid synthesis of selective, potent 3‐amino‐2H‐azaindazole derivatives serving as allosteric inhibitors of SHP2. Structural analysis via co‐crystallography confirmed binding at the allosteric site, thereby stabilizing the autoinhibited SHP2 conformation, qualifying this scaffold as a ...
Machoud Amoussa +20 more
wiley +1 more source
In Silico and In Vitro Investigation of Apoptosis-Mediated Antiproliferative Activity of Capsaicin and Alpha-Lipoic Acid Against Prostate Cancer Cells. [PDF]
Meral O +9 more
europepmc +1 more source
Total Synthesis and Antimalarial Studies of Caelestines A–C
Total synthesis of caelestines A–C (alkaloids from the Australian ascidian, Aplidium caelestis) was accomplished, constituting the first synthesis of caelestines B and C. Caelestines A–C, with five other novel quinolones, were assessed against Plasmodium falciparum 3D7 and Dd2. Caelestine B was found to be a selective antimalarial alkaloid. Caelestines
Henry S. T. Smith +3 more
wiley +1 more source
Impact of Pretreatment Degree and Enzyme Type on the Production of Radical Scavenging and Antiproliferative Peptides from Starfish. [PDF]
Vate NK +7 more
europepmc +1 more source
A modular library of structurally robust palladacyclopentadienyl Pd(II) complexes bearing achiral and chiral diphosphines was developed, revealing a strong influence of diphosphine design and ligand chirality on cytotoxicity and selectivity against ovarian cancer cells, including platinum‐resistant models.
Stefania Mautone +7 more
wiley +1 more source
Evaluation of the phenolic profile and biological activities of Boletus speciosus extracts optimized with response surface methodology and artificial neural networks-genetic algorithm. [PDF]
Korkmaz AF.
europepmc +1 more source
Potential therapeutic targeting of BKCa channels in glioblastoma treatment
This review summarizes current insights into the role of BKCa and mitoBKCa channels in glioblastoma biology, their potential classification as oncochannels, and the emerging pharmacological strategies targeting these channels, emphasizing the translational challenges in developing BKCa‐directed therapies for glioblastoma treatment.
Kamila Maliszewska‐Olejniczak +4 more
wiley +1 more source

