AZA AND DIAZA BIOISOSTERIC ANTHRACENE-9,10-DIONES AS ANTITUMOR AGENTS

Synthetic routes to aza and diaza bioisosteres related to the anthrace ne-9,10-dione, mitoxantrone, have been developed. The antitumor proper ties of these chemotypes are compared with those exhibited by the corr esponding carbocyclic analogues. The sensitivity of the expressed cyto toxicities on the position(s) of the nitrogen atom(s) are discussed in terms of potential cellular targets. Several analogues show potential for clinical evaluations.