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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kaise A,Ohta K,Endo Y

doi

10.1016/j.bmc.2017.10.006

subject

Has Abstract

pub_date

2017-12-15 00:00:00

pages

6371-6378

issue

24

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(17)31945-4

journal_volume

25

pub_type

杂志文章

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