吡唑并[4,5 - g]吡啶并[1,2 - a]苯并咪唑的区域选择性合成：吡啶并[1,2 - a]苯并咪唑环系的细胞毒性衍生物
Regioselective synthesis of pyrazolo[4,5-g]pyrido[1,2-a]benzimidazoles: cytotoxic derivatives of pyrido[1,2-a]benzimidazolic ring system.
作者信息
Dupuy M, Pinguet F, Blache Y, Chavignon O, Teulade J C, Chapat J P
机构信息
Laboratoire de Chimie Organique Pharmaceutique, Faculté de Pharmacie, Montpellier, France.
出版信息
Chem Pharm Bull (Tokyo). 1998 Nov;46(11):1820-3. doi: 10.1248/cpb.46.1820.
N-1 and N-2 substituted pyrazolo[4,5-g]pyrido[1,2-a]benzimidazoles were prepared regioselectively, and cytotoxicities evaluated in vitro against K562 and HL60 cells. All compounds displayed weaker activity than doxorubicin against sensitive lines, but showed the same activity against resistant cell lines (multidrug resistance+, (MDR+); K562R and HL60R) indicating no resistance phenomena.
区域选择性地制备了N-1和N-2取代的吡唑并[4,5-g]吡啶并[1,2-a]苯并咪唑，并在体外评估了其对K562和HL60细胞的细胞毒性。所有化合物对敏感细胞系的活性均比阿霉素弱，但对耐药细胞系（多药耐药阳性，（MDR+）；K562R和HL60R）显示出相同的活性，表明不存在耐药现象。
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