Novel p-carborane-containing multitarget anticancer agents inspired by the metabolism of 17β-estradiol.

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Novel p-carborane-containing multitarget anticancer agents inspired by the metabolism of 17β-estradiol.

Bioorg Med Chem. 2017 Oct 12;:

Authors: Kaise A, Ohta K, Endo Y

Abstract
The female hormone 17 β-estradiol (E2) is synthesized from estrone by steroid sulfatase (STS), and metabolized into 2-methoxyestradiol (2-ME), whereby the biological activity of the latter is substantially different from that of E2. Based on the metabolic pathways of E2, a carborane-containing 2-ME mimic (1c) and its derivatives (1 and 2) were designed and synthesized as novel multitarget anticancer agents. Bissulfamate 1f exhibited potent STS-inhibitory activity and tubulin-polymerization-inhibitory activity. Moreover, the cell-growth-inhibitory (CGI) activity of 1f was similar to that of 2-ME in a panel screening against 39 human cancer cell lines. Accordingly, 1f should be a promising perspective therapeutic agent for hormone-dependent breast tissue.

PMID: 29054710 [PubMed - as supplied by publisher]

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