Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity
文献类型：期刊论文
| 作者 | Sun, Jianan2,3; Mu, Jiahui2,3; Wang, Shenglin2,3; Jia, Cai1; Li, Dahong2,3; Hua, Huiming2,3; Cao, Hao2,3,4 |
| 刊名 | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
 |
| 出版日期 | 2022-12-31 |
| 卷号 | 37期号:1页码:431-444 |
| ISSN号 | 1475-6366 |
| 关键词 | Chromone nitrogen mustard breast cancer apoptosis |
| DOI | 10.1080/14756366.2021.2018685 |
| 英文摘要 | Chromone has emerged as one of the most important synthetic scaffolds for antitumor activity, which promotes the development of candidate drugs with better activity. In this study, a series of nitrogen mustard derivatives of chromone were designed and synthesised, in order to discover promising anti-breast tumour candidates. Almost all target derivatives showed antiproliferative activity against MCF-7 and MDA-MB-231 cell lines. In particular, methyl (S)-3-(4-(bis(2-chloroethyl)amino)phenyl)-2-(5-(((6-methoxy-4-oxo-4H-chromen-3-yl)methyl)amino)-5-oxopentanamido)propanoate showed the most potent antiproliferative activity with IC50 values of 1.83 and 1.90 mu M, respectively, and it also exhibited certain selectivity between tumour cells and normal cells. Further mechanism exploration against MDA-MB-231 cells showed that it possibly induced G2/M phase arrest and apoptosis by generating intracellular ROS and activating DNA damage. In addition, it also inhibited MDA-MB-231 cells metastasis, invasion and adhesion. Overall, methyl (S)-3-(4-(bis(2-chloroethyl)amino)phenyl)-2-(5-(((6-methoxy-4-oxo-4H-chromen-3-yl)methyl)amino)-5-oxopentanamido)propanoate showed potent antitumor activities and relatively low side effects, and deserved further investigation. |
| WOS关键词 | PRIVILEGED SCAFFOLD ; ANTITUMOR-ACTIVITY ; DRUG DISCOVERY ; CELLS ; DNA ; RESISTANCE ; THERAPY ; HYBRIDS ; SELECTIVITY ; INHIBITORS |
| 资助项目 | General Scientific Research Projects of Department of Education in Liaoning Province[2019LJC11] ; Career Development Support Plan for Young and Middle-aged Teachers in Shenyang Pharmaceutical University |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | TAYLOR & FRANCIS LTD |
| WOS记录号 | WOS:000734710100001 |
| 资助机构 | General Scientific Research Projects of Department of Education in Liaoning Province ; Career Development Support Plan for Young and Middle-aged Teachers in Shenyang Pharmaceutical University |
| 源URL | [http://ir.ipe.ac.cn/handle/122111/51472]  |
| 专题 | 中国科学院过程工程研究所 |
| 通讯作者 | Jia, Cai; Li, Dahong; Cao, Hao |
| 作者单位 | 1.Chinese Acad Sci, Inst Proc Engn, State Key Lab Multiphase Complex Syst, Beijing 100190, Peoples R China 2.Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, 103 Wenhua Rd, Shenyang 110016, Peoples R China 3.Shenyang Pharmaceut Univ, Sch Tradit Chinese Mat Med, 103 Wenhua Rd, Shenyang 110016, Peoples R China 4.Shenyang Pharmaceut Univ, Sch Life Sci & Biopharmaceut, Shenyang, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Jianan,Mu, Jiahui,Wang, Shenglin,et al. Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2022,37(1):431-444. |
| APA | Sun, Jianan.,Mu, Jiahui.,Wang, Shenglin.,Jia, Cai.,Li, Dahong.,...&Cao, Hao.(2022).Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity.JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,37(1),431-444. |
| MLA | Sun, Jianan,et al."Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 37.1(2022):431-444. |
入库方式： OAI收割
来源：过程工程研究所
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