Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
4 years ago

Synthesis of novel forskolin isoxazole derivatives with potent anti-cancer activity against breast cancer cell lines

Synthesis of novel forskolin isoxazole derivatives with potent anti-cancer activity against breast cancer cell lines
Forskolin C1-isoxazole derivatives (3,5-regioisomers) (11a-e, 14,15a-h and 15,16a-g) were synthesized regioselectively by adopting 1,3-dipolar cycloadditions. These derivatives were tested using estrogen receptor positive breast cancer cell lines MCF-7 and BT-474. Majority of the compounds exhibited activity against the p53-positive MCF-7 breast cancer cells but not against the p53-negative BT-474 breast cancer cells. Among forskolin derivatives, compounds 11a, 11c, 14a, 14f, 14g, 14h, 15b, 16g and 17b exhibited higher anti-cancer activity against MCF-7 cell line with an IC50 ≤ 1µM. The derivative 14f exhibited highest activity in both p53-positive (MCF-7) and p53-negative (BT-474) breast cancer cell lines with an IC50 of 0.5µM.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X1730834X

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