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

Authors :: Burra S
Voora V
Rao CP
Vijay Kumar P
Kancha RK
David Krupadanam GL
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Sep 15; Vol. 27 (18), pp. 4314-4318. Date of Electronic Publication: 2017 Aug 16.
Publication Year :: 2017
Abstract: Forskolin C <subscript>1</subscript> -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 IC <subscript>50</subscript> ≤1µM. The derivative 14f exhibited highest activity in both p53-positive (MCF-7) and p53-negative (BT-474) breast cancer cell lines with an IC <subscript>50</subscript> of 0.5µM.<br /> (Copyright © 2017. Published by Elsevier Ltd.)

Subjects :: Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Breast Neoplasms pathology
Cell Line, Tumor
Cell Proliferation drug effects
Colforsin chemical synthesis
Colforsin chemistry
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Isoxazoles chemical synthesis
Isoxazoles chemistry
MCF-7 Cells
Molecular Structure
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Breast Neoplasms drug therapy
Colforsin pharmacology
Isoxazoles pharmacology

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