Three naturally isolated isoflavones (2, 4 and 5), two synthetically modified
isoflavones (3 and 6) and four synthesised isoflavones (10, 12, 13 and 15) were
tested in-vitro to access their activities against Chang liver (normal cell line),
JURKAT (leukemia), MCF-17 (breast), HEP-G2 (liver), PC3 (prostate) and LNCap
(prostate) cell lines. In the test against liver cancer, the synthetically modified
isoflavone 3 was better than the curcumin (CUR) control with IC50 value of 5.14
μM. Synthesised isoflavone 12 showed promising activity against prostate cancer
(PC3) (IC50 = 6.11 μM). Whereas intermediate 2,4-dihydroxydeoxybenzoin (10)
showed appreciable to moderate activity against breast, liver and prostate (PC3)
cancer cell lines (IC50 values of 14.59, 31.79 and 65.20 μM, respectively). By
comparison, the synthesised isoflavones showed better activity than the naturally
isolated isoflavones against the same cancer cell lines. These results could serve as
the basis of a structure activity relationship (SAR) study to identify potential anticancer
drug candidates, with improved biological properties based on the
isoflavone scaffold.
Keywords: Anti-cancer, malignancies, Milletia thonningii, isoflavones