摘要
为了开发具有较高生物活性的异海松酸类衍生物,将硫脲结构拼接到异海松酸骨架上,设计合成了15个未见报道的异海松酰(胺)基硫脲类化合物,其结构经FT-IR、~1H NMR、^(13)C NMR和HRMS或元素分析确证.对化合物进行了初步的抑菌和抗癌活性测试,大多数化合物对白色念珠菌表现出显著的抑制活性,且活性高于异海松酸.在浓度为100μmol/L时,部分化合物对人黑色素瘤(A375)和前列腺癌(PC-3)癌细胞具有明显的增殖抑制作用,尤其化合物N-异海松酰基-N′-(3-甲基苯基)硫脲(3c)和N-异海松酰胺基-N'-(4-氟苯基)硫脲(6b)对癌细胞的抑制率达到90%以上.
To develop isopimaric acid derivatives with high bioactivity, fifteen acyl （amide） thiourea derivatives containing isopimaric acid skeleton were synthesized and confirmed by FT-IR, 1H NMR, 13C NMR and HRMS or elemental analysis. All the compounds were evaluated for their antibacterial and anticancer activity. Most of the compounds showed siginificant in- hibitory activity which was higher than that of isopiamric acid against the Candida Albicans, At the concentration of 100 μmol/L, many compounds exhibited pronounced inhibitory effects on human melanoma cells （A375） and prostatic carcinoma （PC-3） cell lines, especially compounds N-isopimaric acyl-N＇-（3-methylphenyl）sulfourea （3c） and N-isopimaric acyla- mino-N＇-（4-fluorophenyl）sulfourea （6b） have the best anticancer activity, both with the inhibitory rate of over 90%.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2017年第3期731-738,共8页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(No.31370575)资助项目~~
关键词
异海松酸
酰基硫脲
抑菌活性
抗癌活性
构效关系
isopimaric acid
acylthiourea
antibacterial activity
anticancer activity
structure-activity relationship
