Baraldi P G, Leoni A, Cacciari B, Manfredini S, Simoni D, Bergomi M, Menta E, Spinelli S
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
J Med Chem. 1994 Dec 9;37(25):4329-37. doi: 10.1021/jm00051a009.
A new class of pyrrolo[1,4]benzodiazepine (PBD) analogues featuring a pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone ring system has been designed and synthesized. These compounds, 2a-o, are characterized by the substitution of the aromatic A ring, characteristic of the PBDs, with a disubstituted pyrazole ring bearing alkyl and benzyl substituents at N6 or N7 and alkyl or carbomethoxy substituents at C8. Biological evaluation revealed an appreciable in vitro cytotoxic activity for compounds 2a,b,f-i.
一类具有吡唑并[4,3-e]吡咯并[1,2-a][1,4]二氮杂卓酮环系统的新型吡咯并[1,4]苯并二氮杂卓（PBD）类似物已被设计并合成。这些化合物（2a-o）的特征在于，具有PBD特征的芳香A环被一个在N6或N7处带有烷基和苄基取代基且在C8处带有烷基或甲氧基羰基取代基的二取代吡唑环所取代。生物学评价显示化合物2a、b、f-i具有明显的体外细胞毒性活性。
