Synthesis and Anti-Tumor Effects of Novel Pomalidomide Derivatives Containing Urea Moieties
文献类型： 外文期刊
作者： Guo, Yajie 1 ; Wang, Xi 2 ; Wang, Zhenzhen 2 ; Mao, Longfei 2 ; Wang, Jiahao 2 ; Peng, Lizeng 5 ; Xu, Guiqing 2 ;
作者机构： 1.Sun Yat Sen Univ, Affiliated Hosp 8, Shenzhen 518033, Peoples R China
2.Henan Normal Univ, Sch Chem & Chem Engn, Xinxiang 453007, Peoples R China
3.Nankai Univ, Coll Pharm, State Key Lab Med Chem Biol, Haihe Educ Pk, 38 Tongyan Rd, Tianjin 300353, Peoples R China
4.Nankai Univ, Tianjin Key Lab Mol Drug Res, Haihe Educ Pk, 38 Tongyan Rd, Tianjin 300353, Peoples R China
5.Shandong Acad Agr Sci, Inst Agro Food Sci & Technol, Key Lab Agro Prod Proc Technol Shandong Prov, Key Lab Novel Food Resources Proc,Minist Agr, Jinan 250100, Peoples R China
关键词： pomalidomide derivatives; urea moieties; immunomodulatory; anti-tumor effects
期刊名称：PHARMACEUTICALS （ 影响因子：5.215； 五年影响因子：5.711 ）
ISSN：
年卷期： 2022 年 15 卷 12 期
页码：
收录情况： SCI
摘要： In order to explore novel immunomodulatory agents as anti-tumor drugs, we designed and synthesized a series of new pomalidomide derivatives containing urea moieties. Interestingly, in vitro biological experiments performed in several cancer cell lines showed that some of them displayed potent anti-tumor ability. These novel compounds 5a-5e and 6a-6e demonstrated the best cell growth inhibitive activity in human breast cancer cell lines MCF-7, but weaker inhibitive activity in human hepatocellular carcinoma cell lines Huh7. Moreover, compound 5d had the most powerful effects in this study, with an IC50 value of 20.2 mu M in MCF-7. Further study indicated that compound 5d could inhibit cell growth and induce cell death in a concentration-dependent manner. Besides, compound 5d increased cellular ROS levels and induced DNA damage, thereby potentially leading to cell apoptosis. These observations suggest that the novel pomalidomide derivatives containing urea moieties may be worth further investigation to generate potential anti-tumor drugs.
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