Synthesis and biological assessment of new pyrimidopyrimidines as inhibitors of breast cancer resistance protein (ABCG2)

[Display omitted] •Pyrimidopyrimidines: new Inhibitors of Breast Cancer Resistance Protein.•7 g, 7 h and 7i are the most potent inhibitors of ABCG2 with IC50 equal to 0.487, 0.493 and 0.434 μM respectively.•7 g and 7i showed additional inhibition of ABCB1 with IC50 equal to 5.46 and 7.88 μM.•No inhi...

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Veröffentlicht in:	Bioorganic chemistry 2021-11, Vol.116, p.105326-105326, Article 105326
Hauptverfasser:	Dakhlaoui, Imen, Vahdati, Sahel, Maalej, Emna, Chabchoub, Fakher, Wiese, Michael, Marco-Contelles, Jose, Ismaili, lhassane
Format:	Artikel
Sprache:	eng
Schlagworte:	ABC transporter ABCB1 ABCC1 ABCG2 inhibitor Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology ATP Binding Cassette Transporter, Subfamily G, Member 2 - antagonists & inhibitors ATP Binding Cassette Transporter, Subfamily G, Member 2 - metabolism Breast Neoplasms - drug therapy Breast Neoplasms - metabolism Breast Neoplasms - pathology Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Female Humans Molecular Structure Multidrug resistance Neoplasm Proteins - antagonists & inhibitors Neoplasm Proteins - metabolism Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Pyrimidopyrimidines Structure-Activity Relationship Tumor Cells, Cultured
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