2－（E）－烷亚甲基环己酮Mannich碱盐酸盐类化合物的合成及抗癌、抗炎活性研究

Synthesis and Anticancer and Antiinflammatory Activities of 2-(E)-Alkylidene or Benzylidene Cyclohexanone Mannich Base Hydrochlorides

本文设计、合成了２－（Ｅ）－烷亚甲基环己酮Ｍａｎｎｉｃｈ碱盐酸盐类化合物２４个；其中２２个为未见文献报道的新化合物。初步药理结果显示：大部分化合物对Ｐ３８８和Ｈｅｌａ细胞均有作用，特别是化合物Ⅱ２３，它对两种细胞的ＬＣ５０分别为４．１０１ｍｇ／Ｌ和０．１３５ｍｇ／Ｌ；部分化合物对Ｌ１２１１０和Ｈｅｐ２细胞也有一定的抑制作用；动物体内实验也显示出一定的活性。该类化合物还有效强的抗炎活性，有些化合物的抗炎活性与消炎痛相当。

The Mannich bases(Ⅱ1～13)and the Mannich bases(Ⅱ14～23) have been synthesized from the corresponding alkylidene cyclohexanones(Ⅱ1～4)and benzylidene cyclohexanones(Ⅱ5～7)by the Mannich reaction. The anticancer activity of some of the part compounds has been evaluated. Most compounds tested were found to be active against the P388 and Hela tumour in vitro. In particular,(Ⅱ23)shows LC50 was respectively 4. 101 and 0. 135 mg/L. Some compounds were active against the L1210 and Hep2 tumour, too, Some compounds or type Ⅱ compounds exhibited antiinflammatory activity on the edema of ears of mice induced by xylene and on the edema of paws of rats induced by carrageen. The activity of(Ⅱ23)was found to be twice times the activity of indomethacin.