Misbahi Houria, Brouant Pierre, Hevér Aniko, Molnár Anna Maria, Wolfard Krysztina, Spengler Grabriela, Mefetah Hafid, Molnár Joseph, Barbe Jacques
GERCTOP/UMR CNRS 6009, Faculté de Pharmacie, Marseille, France.
Anticancer Res. 2002 Jul-Aug;22(4):2097-101.
A series of benzo[b]-1,8-naphthyridine derivatives branched with various side-chains and substituents were prepared with the aim of being investigated as multidrug resistance (MDR) modulators. The syntheses were achieved from 2-halonicotinic acid and suitable aryl-amines according to a three-step procedure. All the derivatives were tested in vitro on mouse T-Lymphoma cell line L5178 transfected by MDR1 gene and the chemosensitizing properties of the compounds were compared to those of verapamil and propranolol, as well as to several other tricyclic derivatives like phenothiazines and acridines. Most of the compounds tested reversed the MDR of tumour cells more effectively than the reference drugs did and they showed more potent chemosensitizing activity than phenothiazine and acridine derivatives have.
制备了一系列带有各种侧链和取代基的苯并[b]-1,8-萘啶衍生物，目的是将其作为多药耐药性（MDR）调节剂进行研究。根据三步程序，由2-卤代烟酸和合适的芳基胺实现合成。所有衍生物均在体外对转染了MDR1基因的小鼠T淋巴瘤细胞系L5178进行了测试，并将化合物的化学增敏特性与维拉帕米和普萘洛尔以及其他几种三环衍生物（如吩噻嗪和吖啶）的特性进行了比较。大多数测试化合物比参比药物更有效地逆转了肿瘤细胞的MDR，并且它们显示出比吩噻嗪和吖啶衍生物更强的化学增敏活性。
