Heterocyclic quinones with potential antitumor activity. 2. Synthesis and antitumor activity of some benzimidazole-4,7-dione derivatives.
A series of benzimidazole-4,7-dione derivatives, bearing substituents at positions 1, 2, 5, and 6 of the benzimidazole ring, has been synthesized and tested for antitumor activity in vivo on P388 leukemia. Some of the synthesized compounds show significant antitumor activity, associated with high toxicity, however. Compounds 7, 18, and 27 show the highest antitumor activity in this series, whereas 17, 19, and 22 are scarcely active. Some hypothetical biological precursors of these quinones are devoid of antitumor activity. Some structure-activity relationships are discussed.
Antonini
I
I
Dipartimento di Scienze Chimiche, Universitá di Camerino, Italy.
Claudi
F
F
Cristalli
G
G
Franchetti
P
P
Grifantini
M
M
Martelli
S
S
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000627:therapeutic use; D007202:Indicators and Reagents; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D011809:Quinones / Q000138:chemical synthesis* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D001562:Benzimidazoles; D007202:Indicators and Reagents; D011809:Quinones