环戊酮衍生物的合成及其抗癌、抗炎活性

SYNTHESIS OF SOME CYCLOPENTANONE DERIVATIVES AND THEIR ANTITUMOR AND ANTI-INFLAMMATORY ACTIVITY

本文选取α-正亚辛基环戌酮为先导化合物,设计并合成了α-亚烷基环戌酮、α-取代环戊烯酮、α-亚烷基-α′-二甲胺甲基环戊酮盐酸盐及α;α,B-烷基取代环戊酮共四个系列二十五个环戊酮衍生物,其中九个为未见于文献的新化合物。抗癌及抗炎活性的药理初筛实验的结果表明,其中的某些化合物具有一定的抗癌、抗炎活性。深入的药理实验正在进行中。

It was reported that there were certain relations between the antitumor and anti-inflammatory activity of some drugs and that both were basically related to prostaglandins. In view of the fact that cyclopentanones are similar to prostaglandins in chemical structures, the tentative idea of searching new antitumor and anti-inflammatory drugs from cyclopentanones was proposed, a-Octylidene cyclopentanone was chosen as the leading compound, twenty-six cyclopentanone derivatives were designed and synthesized. These included series of α-alkylidene and α-arylidene cyclopentanones、α-substituted alkylcyclopentenones、α-alkylidene-α-'dimethylaminomethylcyclopentanone hydrochlorides and α, or α,β-substituted alkylcyclopentanones. Among them nine of the compounds were new. The antitumor activity of these compounds was tested in vitro and the anti-inflammatory effects on oedema of mice ears induced by dimethylbenzene were screened preliminarily by dimethylbenzene. The preliminary pharmacoogical screening tests showed that these compounds exhibited a certain degree of antitumor and anti-inflammatory activity. Further pharmacological examinations are in progress.