Synthesis of Monocarbonyl Analogues of Curcumin that Required for Biological Screening

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صابر, رهام نافز احمد
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An-Najah National University
Curcumin and isoflavone have exhibited wide anti-tumor effect in vivo and in vitro. It has been developed a new adjuvant chemotherapy protocol of cancer by synthesis of monocarbonyl curcumin analogues and isoflavone derivatives. The compounds of monocarbonyl curcumin analogues (MCACs) and isoflavone derivative were synthesized by condensation reaction under basic condition followed by oxidation reaction and identified by IR. They were evaluated for their cytotoxic activity against cervical (Hela), liver (Hep3B, HepG2) and breast (MCF-7) cancer cell lines, and also evaluated as antioxidant agents. Compounds 56, 58 and 56a showed no anticancer activity against MCF-7. On the contrary, compounds 57 and 59a showed anticancer activity against MCF-7 with IC50 values of 39.8 μg/ml and 50.11 μg/ml, respectively. Compound 57 displayed inhibitory activity against HepG2 and Hela cancer cell lines with IC50 values of 50.11 and 22.3 μg/ml, respectively. Moreover, compound 56a showed inhibition of cell growth against HepG2 cancer cell line with IC50 value of 7.194 μg/ml better than that of curcumin (IC50 23.15 μg/ml). These results indicate that compound 56a has a potent and promising anticancer activity against HepG2 cancer cell line. Compounds 67, 66 and 61 exhibited very weak anticancer activity against all cancer cell lines. On other hand, 56a and 57a showed excellent antioxidant activity with IC50 values of 11.8 and 15.8 μg/ml, respectively, compared with the strong antioxidant agent Trolox (IC50 = 3.4 μg/ml).