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  • Title: Synthesis of novel forskolin isoxazole derivatives with potent anti-cancer activity against breast cancer cell lines.
    Author: Burra S, Voora V, Rao CP, Vijay Kumar P, Kancha RK, David Krupadanam GL.
    Journal: Bioorg Med Chem Lett; 2017 Sep 15; 27(18):4314-4318. PubMed ID: 28838692.
    Abstract:
    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.
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