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4'-Methylangelicins: new potential agents for the photochemotherapy of psoriasis.

Abstract：

:Three derivatives of angelicin (1) [4'-methyl-, 4,4'-dimethyl-, and 4',5-dimethylangelicin (2a-c)] have been prepared with the aim of obtaining new agents for the photochemotherapy of psoriasis. These compounds form a complex in the dark with DNA that shows an affinity for the macromolecule higher than that of the parent angelicin (1). A correlation between their octanol/water partition coefficients and the association constants of the complexes has been observed. Compounds 2a-c photobind to DNA to a much higher extent than 1 and also more effectively than 8-methoxypsoralen (8-MOP), taken as reference compound. When activated with UV-A, the three compounds strongly inactivate T2 phage and inhibit epidermal DNA synthesis in mice. Moreover, they show a mutagenic activity markedly lower than that of 8-methoxypsoralen on Escherichia coli wild-type strain. Due to its lack of skin phototoxicity, its low mutagenic activity, and its antiproliferative activity, 2c was chosen for clinical evaluation. It proved to be effective in clearing psoriasis in two patients.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Dall'Acqua F,Vedaldi D,Bordin F,Baccichetti F,Carlassare F,Tamaro M,Rodighiero P,Pastorini G,Guiotto A,Recchia G,Cristofolini M

doi

10.1021/jm00360a016

subject

Has Abstract

pub_date

1983-06-01 00:00:00

pages

870-6

issue

6

eissn

0022-2623

issn

1520-4804

journal_volume

26

pub_type

杂志文章

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