文献类型：期刊文献

英文题名：New Hybrids Derived from the Natural Compound (-)-beta-Pinene and Amides or Acylthioureas as Antitumor Agents

作者：Liao, Shengliang[1,2] Rao, Xiaoping[1] Shen, Minggui[1] Si, Hongyan[1,2] Song, Jie[3] Shang, Shibin[1] Song, Zhanqian[1]

第一作者：Liao, Shengliang

通信作者：Shang, SB[1];Song, ZQ[1]

机构：[1]China Acad Forestry, Natl Engn Lab Biomass Chem Utilizat, Key & Open Lab Forest Chem Engn, State Forestry Adm,Key Lab Biomass Energy & Mat,I, Nanjing 210042, Jiangsu, Peoples R China;[2]Jiangxi Agr Univ, Coll Forestry, Camphor Tree Engn & Technol Res Ctr State Forestr, Nanchang 330045, Jiangxi, Peoples R China;[3]Univ Michigan, Dept Chem & Biochem, 303E Kearsley St, Flint, MI 48502 USA

年份：2020

卷号：17

期号：3

起止页码：271-284

外文期刊名：LETTERS IN DRUG DESIGN & DISCOVERY

收录：;Scopus(收录号：2-s2.0-85083220705);WOS:【SCI-EXPANDED(收录号:WOS:000522436400004)】；

基金：This work was supported by the National Natural S cience Foundation of China (Grant number 31500487) and the Fundamental Research Funds for the Central Nonprofit Research Institution of CAF (Grant number CAFYBB2016QB014).

语种：英文

外文关键词：Pinene; amide; acylthiourea; synthesis; antitumor; MCF7; SW1116

摘要：Background: Plant-derived natural compounds have a unique molecular structure and rich biological activity, hence, they are treated as important raw materials for the development of drugs. Methods: A natural compound (-)-beta-pinene was used as a raw material, and twenty-six novel derivatives with amide or acylthiourea groups were synthesized based on the molecular hybridization method. In vitro antitumor activity of these derivatives on human breast cancer cell line MCF7 and human colon cancer cell line SW1116 were tested by MTT method. The effects of the synthesized derivatives on the morphology of MCF7 and SW1116 were observed by fluorescent inverted microscope. Results: The preliminary structure-activity relationship analysis demonstrates that the position and species of substituents on the aromatic ring of derivatives have an effect on the antitumor activity of derivatives. Observation of the cell morphology reveals that derivatives with antitumor activity can lead to rounding of the cell morphology, a decrease in cell volume and cell density, and ultimately inhibition of the proliferation of MCF7 and SW1116 cells. The antitumor activity evaluation results show that among these derivatives, compounds 5c, 5e, 5h, 7c, 7b and 7e exhibit good antitumor activity against MCF7, and compounds 5c, 5e, 5h and 7j exert moderate antitumor activity against SW1116. Conclusion: This study hopes to promote the high value-added utilization of natural compounds beta-pinene and the development of novel antitumor drugs.