Gregson Stephen J, Howard Philip W, Thurston David E
Cancer Research UK Gene Targeted Drug Design Research Group, The School of Pharmacy, University of London, 29/39 Brunswick Square, WC1N 1AX, London, UK.
Bioorg Med Chem Lett. 2003 Jul 21;13(14):2277-80. doi: 10.1016/s0960-894x(03)00436-0.
We report the synthesis of novel A-C8/C-C2 amide-linked pyrrolo[2,1-c][1,4]benzodiazepine dimers (4a and 4b) via convergent routes. These compounds lack the potent DNA interstrand cross-linking ability and resultant pronounced cytotoxicity of the known A-C8/A-C8' linked dimers (e.g., 2a-b).
我们报道了通过汇聚路线合成新型的A-C8/C-C2酰胺连接的吡咯并[2,1-c][1,4]苯并二氮杂卓二聚体(4a和4b)。这些化合物缺乏已知的A-C8/A-C8'连接的二聚体(例如2a-b)的有效DNA链间交联能力以及由此产生的显著细胞毒性。