Antonini I, Claudi F, Cristalli G, Franchetti P, Grifantini M, Martelli S
Dipartimento di Scienze Chimiche, Universitá di Camerino, Italy.
J Med Chem. 1988 Jan;31(1):260-4. doi: 10.1021/jm00396a041.
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.
合成了一系列在苯并咪唑环的1、2、5和6位带有取代基的苯并咪唑-4,7-二酮衍生物，并在P388白血病体内模型上测试了其抗肿瘤活性。然而，一些合成化合物显示出显著的抗肿瘤活性，但伴有高毒性。化合物7、18和27在该系列中显示出最高的抗肿瘤活性，而17、19和22几乎没有活性。这些醌类化合物的一些假设生物前体没有抗肿瘤活性。讨论了一些构效关系。
