Keuser C, Pindur U
Institute of Pharmacy, Department of Chemistry and Pharmacy, Johannes Gutenberg-University, Mainz, Germany.
Pharmazie. 2006 Apr;61(4):261-8.
The synthesis of a series of new oligopyrrole carboxamides closely related to netropsin and distamycin A, linked with a nucleobase is reported. The new compounds possess similar structure elements as the known peptide nucleic acids which are interesting sequence reading DNA ligands. Cytotoxicity in vitro, the DNA binding characteristics and the inhibition of topoisomerase I were studied. Four of the compounds, 27, 31, 33 and 37 bind to DNA probably at AT sequences like netropsin or distamycin A in the minor groove. Surprisingly, no cytotoxicity and no inhibition of topoisomerase I was found.
报道了一系列与纺锤菌素和偏端霉素A密切相关且与核碱基相连的新型寡聚吡咯羧酰胺的合成。这些新化合物具有与已知肽核酸相似的结构元件，而肽核酸是有趣的序列读取DNA配体。研究了它们的体外细胞毒性、DNA结合特性以及对拓扑异构酶I的抑制作用。其中四种化合物，即27、31、33和37，可能在小沟中与DNA结合，结合序列类似于纺锤菌素或偏端霉素A的AT序列。令人惊讶的是，未发现细胞毒性和对拓扑异构酶I的抑制作用。
