Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/978-1-4615-5381-6_158 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Pyrimidine: A Privileged Scaffold for the Development of Anticancer Agents as Protein Kinase Inhibitors (Recent Update).
Curr Pharm Des
January 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.
The pyrimidine nucleus is a fundamental component of human DNA and RNA, as well as the backbone of many therapeutic agents. Its significance in medicinal chemistry is well-established, with pyrimidine derivatives receiving considerable attention due to their potent anticancer properties across various cancer cell lines. Numerous derivatives have been synthesized, drawing structural inspiration from known anticancer agents like dihydropyrimidine compounds, which include the active cores of drugs such as 5-fluorouracil and monastrol, both of which have demonstrated strong anticancer efficacy.
View Article and Find Full Text PDFUpdates on Intrinsic Medicinal Chemistry of 1,4-dihydropyridines, Perspectives on Synthesis and Pharmacokinetics of Novel 1,4-dihydropyrimidines as Calcium Channel Blockers: Clinical Pharmacology.
Curr Top Med Chem
January 2025
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education & Research (JSS AHER), Mysuru, Karnataka, India.
Background: Several chemical studies described the physiological efficacy of 1,4- dihydropyridines (DHPs). DHPs bind to specific sites on the α1 subunit of L-type calcium channels, where they demonstrate a more pronounced inhibition of Ca2+ influx in vascular smooth muscle compared to myocardial tissue. This selective inhibition is the basis for their preferential vasodilatory action on peripheral and coronary arteries, a characteristic that underlies their therapeutic utility in managing hypertension and angina.
View Article and Find Full Text PDFDPYD genotype should be extended to rare variants: report on two cases of phenotype / genotype discrepancy.
Cancer Chemother Pharmacol
January 2025
Service de Génomique des Tumeurs et Pharmacologie, Hôpital Saint-Louis, Assistance Publique Hôpitaux de Paris, Paris, France.
The enzyme dihydropyrimidine dehydrogenase (DPD) is the primary catabolic pathway of fluoropyrimidines including 5 fluorouracil (5FU) and capecitabine. Cases of lethal toxicity have been reported in cancer patients with complete DPD deficiency receiving standard dose of 5FU or capecitabine. DPD is encoded by the pharmacogene DPYD in which more than 200 variants have been identified.
View Article and Find Full Text PDFA bacteria-responsive nanoplatform with biofilm dispersion and ROS scavenging for the healing of infected diabetic wounds.
Acta Biomater
December 2024
Key Laboratory of Endocrine Glucose & Lipids Metabolism and Brain Aging, Ministry of Education, Department of Endocrinology, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Shandong First Medical University, Jinan, Shandong 250021, China; Shandong Key Laboratory of Endocrinology and Lipid Metabolism, Jinan, Shandong 250021, China. Electronic address:
Delayed wound healing in patients with diabetes remains a major health challenge worldwide. Uncontrolled bacterial infection leads to excessive production of reactive oxygen species (ROS) and persistent inflammatory responses, which seriously hinder conventional physiological healing processes after injury. Biofilms, as protective barriers for bacteria, pose a critical obstacle to effective bacterial eradication.
View Article and Find Full Text PDFUnveiling the potential anticancer activity of new dihydropyrimidines through dual inhibition of EGFR and TrkA: Design, synthesis, and in silico study.
Bioorg Chem
January 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Article Synopsis
- - A series of dihydropyrimidine compounds were created as inhibitors of tyrosine kinases through a one-pot Biginelli reaction, yielding a variety of 1,4-DHPM hybrids by alkylating with different chloroacetylamine derivatives.
- - These synthesized compounds were tested for their ability to inhibit cancer cell growth in different cell lines (HCT-116, PC-3, MCF-7) and showed that compounds 8h and 8i were the most effective, with low concentrations needed to inhibit cancer cells while being more selective towards normal cells.
- - Further analysis revealed that compound 8h was particularly potent in inhibiting key kinases (EGFR and Trk
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!