文献类型： 外文期刊

作者： Luo, Xiong-Fei ¹ ; Zhang, Zhi-Jun ¹ ; Song, Zi-Long ¹ ; Wang, Zhi-Ping ² ; Yan, Jia-Xuan ³ ; Liu, Xiao-Fei ⁴ ; Peng, Li-Zeng ⁴ ; Yang, Cheng-Jie ¹ ; Liu, Ying-Qian ¹ ;

作者机构： 1.Lanzhou Univ, Sch Pharm, Lanzhou, Peoples R China

2.Lanzhou Univ, Inst Urol, Dept Urol, Hosp 2,Gansu Nephro Urol Clin Ctr,Key Lab Urol Dis, Lanzhou, Gansu, Peoples R China

3.Peking Univ, Sch Pharmaceut Sci, Beijing, Peoples R China

4.Jinan AISI Pharmaceut Technol Co Ltd, Jinan, Peoples R China

5.Shandong Acad Agr Sci, Inst Agrofood Sci & Technol, Jinan, Peoples R China

关键词： Camptothecin; sulphonamide; sulfonylurea; cytotoxic activity; synthesis

期刊名称：NATURAL PRODUCT RESEARCH （ 影响因子：1.9； 五年影响因子：2.1 ）

ISSN： 1478-6419

年卷期： 2024 年

页码：

收录情况： SCI

摘要： With the intention of advancing our research on diverse C-20 derivatives of camptothecin (CPT), 38 CPT derivatives bearing sulphonamide and sulfonylurea chemical scaffolds and different substituent groups have been designed, synthesised and evaluated in vitro for cytotoxicity against four tumour cell lines, A-549 (lung carcinoma), KB (nasopharyngeal carcinoma), MDA-MB-231 (triple-negative breast cancer) and KBvin (an MDR KB subiline). As a result, all the synthesised compounds showed promising in vitro cytotoxic activity against the four cancer cell lines tested, and were more potent than irinotecan. Importantly, compounds 12b, 12f, 12j and 13 l possessed better antiproliferative activity against all tested tumour cell lines with IC50 values of 0.0118 - 0.5478 mu M, and resulted approximately 3 to 4 times more cytotoxic than topotecan against multidrug-resistant KBvin subline. Convincing evidences are achieved that incorporation of sulphonamide and sulfonylurea motifs into position-20 of camptothecin confers markedly enhanced cytotoxic activity against cancer cell lines. {Graphical Abstract}