In:
Archiv der Pharmazie, Wiley, Vol. 350, No. 1 ( 2017-01)
Abstract:
DNA topoisomerase I inhibitors, both synthetic and of natural origin, are receiving increasing consideration primarily as drugs against refractory tumors. Alkannin and shikonin, two enantiomeric dyes from Alkanna tinctoria and Lithospermum erythrorhizon , have been known over many centuries as dyestuff, wound healing, anti‐inflammatory, antibacterial and antitumor substances. Although multiple mechanisms appear to be implicated, their potency is associated with the inhibition of topoisomerase I and with the redox properties of the naphthazarin scaffold. Here, the synthesis of new naphthalene and naphthoquinone derivatives inspired by alkannin and shikonin is described and their structural and biological properties were examined. Different oxidation states of the naphthalene nucleus were examined to observe the effect of this parameter on cytotoxicity. Antiproliferative activities against a panel of human cancer cell lines were evaluated and the implication of topoisomerase I was assessed.
Type of Medium:
Online Resource
ISSN:
0365-6233
,
1521-4184
DOI:
10.1002/ardp.201600286
Language:
English
Publisher:
Wiley
Publication Date:
2017
detail.hit.zdb_id:
1496815-0
SSG:
15,3
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