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Three esters of rhodamine B ( 1 – 3 ) differing in their alkyl chain lengths as well as several rhodamine B amides ( 4 – 9 ) 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 EC 50  = 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.

Ester and amide derivatives of rhodamine B exert cytotoxic effects on different human tumor cell lines