柠檬烯类似物的合成及其体外抗癌活性

Synthesis of limonene derivatives and their antitumor activities in vitro

目的设计并合成柠檬烯类似物,并对其体外抗癌活性进行初步的评价。方法以l-香芹酮为起始原料,通过氯代、亲核取代、选择性还原制备目标化合物;以MTT法测试目标化合物对人前列腺癌细胞LNCaP的增殖抑制活性。结果与结论所合成的14个新化合物经1H-NMR和MS确证结构。初步药理实验结果表明12个目标化合物的抗癌活性比d-柠檬烯和l-香芹酮更强。

Aim To design and synthesize limonene analogues, and to assess their antitumor activity in vitro. Methods The target compounds were synthesized from l-carvone via chlorination, nucleophilic substitution and selective reduction. Their in vitro antitumor activities were evaluated in prostate cell line LNCaP by using MTT assay. Results and conclusion The structures of 14 novel compounds were characterized by MS and ^1H-NMR. Preliminary pharmacological results showed that 12 compounds possessed stronger antitumor activities than d-limonene and l-carvone did in vitro.