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Ester and amide derivatives of rhodamine B exert cytotoxic effects on different human tumor cell lines
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-06-22 , DOI: 10.1007/s00044-020-02591-8
Immo Serbian , Sophie Hoenke , Oliver Kraft , René Csuk

Three esters of rhodamine B (13) differing in their alkyl chain lengths as well as several rhodamine B amides (49) were synthesized in good yields and tested for their cytotoxicity in SRB assays employing several human tumor cell lines. The rhodamine B esters were unselective but showed cytotoxicity of as low as EC50 = 0.15 ± 0.02 µM. The rhodamine B amides were slightly less cytotoxic but showed good selectivity against MCF-7 and A2780 tumor cell lines. Especially a morpholinyl derivative 4 was ~20 time more cytotoxic for MCF-7 than for nonmalignant NIH 3T3 cells.


中文翻译:

罗丹明B的酯和酰胺衍生物对不同的人类肿瘤细胞系产生细胞毒性作用

若丹明B(三个酯1 - 3在它们的烷基链长度以及若干若丹明B色酰胺(不同)4 - 9)以良好的收率合成和它们在使用几种人肿瘤细胞系SRB测定的细胞毒性测试。罗丹明B酯是非选择性的,但显示出低至EC 50  = 0.15±0.02 µM的细胞毒性。罗丹明B酰胺的细胞毒性略低,但对MCF-7和A2780肿瘤细胞系表现出良好的选择性。特别是吗啉基衍生物4对MCF-7的细胞毒性比对非恶性NIH 3T3细胞高20倍。
更新日期:2020-06-22
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