I found the field of Pharmacology & Pharmacy very interesting. Saw the article Synthesis and biological evaluation of quinazoline derivatives – A SAR study of novel inhibitors of ABCG2 published in 2019. Recommanded Product: 3-(Trifluoromethyl)phenol, Reprint Addresses Wiese, M (corresponding author), Univ Bonn, Inst Pharmaceut, Immenburg 4, D-53121 Bonn, Germany.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol
Multidrug resistance (MDR) is a major obstacle for effective chemotherapeutic treatment of cancer frequently leading to failure of the therapy. MDR is often associated with the overexpression of ABC transport proteins like ABCB1 or ABCG2 which efflux harmful substances out of cells at the cost of ATP hydrolysis. One way to overcome MDR is to apply potent inhibitors of ABC transporters to restore the sensitivity of the cells toward cytostatic agents. This study focusses on the synthesis and evaluation of novel 2,4-disubstituted quinazoline derivatives regarding the structure-activity-relationship (SAR), their ability to reverse MDR and their mode of interaction with ABCG2. Hence, the inhibitory potency and selectivity toward ABCG2 was determined. Moreover, the intrinsic cytotoxicity and the reversal of MDR were investigated. Interaction type studies with the substrate Hoechst 33342 and conformational analyses of ABCG2 with 5D3 monoclonal antibody were performed for a better understanding of the underlying mechanisms. In our study we could further enhance the inhibitory effect against ABCG2 (compound 31, IC50: 55 nM) and identify the structural features that are crucial for inhibitory potency, the impact on transport activity and binding to the protein. (C) 2018 Elsevier Masson SAS. All rights reserved,
About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Krapf, MK; Gallus, J; Spindler, A; Wiese, M or concate me.. Recommanded Product: 3-(Trifluoromethyl)phenol
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles