Boumendjel Ahcène, Beney Chantal, Deka Nabajyoti, Mariotte Anne-Marie, Lawson Martin Ata, Trompier Doriane, Baubichon-Cortay Hélène, Di Pietro Attilio
Laboratory of Pharmacognosy, UMR-CNRS 5063, Grenoble Pharmacy School, La Tronche, France.
Chem Pharm Bull (Tokyo). 2002 Jun;50(6):854-6. doi: 10.1248/cpb.50.854.
A series of 4-hydroxy-6-methoxyaurones and 4,6-dimethoxyaurones has been synthesised and tested for their binding affinity toward the nucleotide-binding domain of P-glycoprotein, an ABC (ATP-Binding Cassette) transporter which mediates the resistance of cancer cells to chemotherapy. These compounds differ from each other by the nature of the substituent on the aurone B-ring. The binding affinity seems to be linked to the nature of the substituent, as well as to the presence or the absence of a hydroxy group at position 4. The most active compounds were 4'-bromo-4-hydroxy-6-methoxyaurone and 4-hydroxy-4'-iodo-6-methoxyaurone.
已经合成了一系列4-羟基-6-甲氧基奥酮和4,6-二甲氧基奥酮，并测试了它们对P-糖蛋白核苷酸结合域的结合亲和力，P-糖蛋白是一种ABC（ATP结合盒）转运蛋白，介导癌细胞对化疗的耐药性。这些化合物在奥酮B环上的取代基性质上彼此不同。结合亲和力似乎与取代基的性质以及4位羟基的存在与否有关。活性最高的化合物是4'-溴-4-羟基-6-甲氧基奥酮和4-羟基-4'-碘-6-甲氧基奥酮。
