Krapcho A P, Maresch M J, Hacker M P, Menta E, Oliva A, Giuliani F C, Spinelli S
Department of Chemistry, University of Vermont, Burlington 05405, USA.
Acta Biochim Pol. 1995;42(4):427-32.
Synthetic routes to aza and diaza bioisosteres related to the anthracene-9,10-dione, mitoxantrone, have been developed. The antitumor properties of these chemotypes are compared with those exhibited by the corresponding carbocyclic analogues. The sensitivity of the expressed cytotoxicities on the position(s) of the nitrogen atom(s) are discussed in terms of potential cellular targets. Several analogues show potential for clinical evaluations.
已开发出与蒽-9,10-二酮米托蒽醌相关的氮杂和二氮杂生物电子等排体的合成路线。将这些化学类型的抗肿瘤特性与相应的碳环类似物所表现出的特性进行了比较。根据潜在的细胞靶点讨论了所表达的细胞毒性对氮原子位置的敏感性。几种类似物显示出临床评估的潜力。
