The syntheses and SAR studies of various quinazolinone compounds are described for the dual inhibition of Pgp and MRP1 in multidrug resistance.
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http://dx.doi.org/10.1016/s0960-894x(01)00804-6 | DOI Listing |
Int J Pharm
January 2025
Drug Delivery and Disposition, KU Leuven, Gasthuisberg ON2, Herestraat 49 - box 921, 3000 Leuven, Belgium. Electronic address:
The widespread prevalence of colorectal cancer and its high mortality rate emphasize the urgent need for more effective therapies. When developing new drug products, a key aspect is ensuring that sufficiently high concentrations of the active drug are reached at the site of action. Drug transporters and drug-metabolizing enzymes can significantly influence the absorption and local accumulation of drugs in intestinal tissue.
View Article and Find Full Text PDFZhongguo Shi Yan Xue Ye Xue Za Zhi
December 2024
Department of Pediatrics, Binzhou Medical University Hospital, Binzhou 256603, Shandong Province, China.
Transl Cancer Res
November 2024
Department of Pathology, Medical College, Shandong University of Traditional Chinese Medicine, Jinan, China.
Breast cancer is one of the most common cancers among women. Nowadays postoperative adjuvant chemotherapy is the mainstay for clinical treatment of breast cancer. However, the emergence of multidrug resistance (MDR) in breast cancer has become a main reason for the failure of clinical chemotherapy.
View Article and Find Full Text PDFEur J Med Chem
January 2025
School of Pharmacy, Fudan University, Shanghai, 201203, China. Electronic address:
J Drug Target
November 2024
School of Medicine, College of Medicine, I-Shou University, Kaohsiung, Taiwan, R.O.C.
Drug efflux transporters, especially those belonging to the ATP-binding cassette (ABC) transporter superfamily, play a crucial role in various drug resistance issues, including multidrug resistance (MDR) in cancer and treatment-resistant depression (TRD) in individuals with major depressive disorder. Key transporters in this context include P-glycoprotein (P-gp), multidrug resistance protein 1 (MRP1), and breast cancer resistance protein (BCRP). This study aimed to investigate the modulatory effects of polyoxyethylene (20) sorbitan monolaurate (Tween 20) on these efflux transporters and to evaluate its potential for overcoming drug resistance in two models: an cancer MDR model and an TRD model.
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