托酚酮衍生物的合成及其抗肿瘤活性。2.

Synthesis and antitumor activity of tropolone derivatives. 2.

作者信息

Yamato M, Hashigaki K, Ishikawa S, Kokubu N, Inoue Y, Tsuruo T, Tashiro T

出版信息

J Med Chem. 1985 Aug;28(8):1026-31. doi: 10.1021/jm00146a009.

PMID:4020825

Abstract

Structural requirement for antitumor activity of tropolone derivatives 2-4 was explored. Isochroman derivatives (6-17, 20, and 23) and alpha, alpha-disubstituted compounds 26-30 were synthesized and their antitumor activities were tested. These nontroponoid derivatives were all inactive, implying that a tropolone ring is essential for the activity. Several compounds related to the monotropolone analogue 3 were synthesized. Among them, 31-33 showed significant activity, but their potencies were considerably weaker than those of binary tropolone analogues 4.

摘要

对托酚酮衍生物2-4的抗肿瘤活性的结构要求进行了探索。合成了异苯并二氢吡喃衍生物（6-17、20和23）以及α,α-二取代化合物26-30，并测试了它们的抗肿瘤活性。这些非托酚酮衍生物均无活性，这意味着托酚酮环对活性至关重要。合成了几种与单托酚酮类似物3相关的化合物。其中，31-33显示出显著活性，但其效力明显弱于二元托酚酮类似物4。