Twenty-one coumarins were examined for their antiproliferative activity tow
ards several cancer cell lines, namely lung carcinoma (A549), melanin pigme
nt producing mouse melanoma (B16 melanoma 4A5), human T-cell leukemia (CCRF
-HSB-2), and human gastric cancer, lymph none metastasized (TGBC11TKB). The
structure-activity relationship established from the results revealed that
the 6,7-dihydroxy moiety had an important role for their antiproliferative
activity. Analysis of cell cycle distribution indicated that esculetin-tre
ated cells accumulated in the GI (at 400 muM) or in S phase (at 100 muM).