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Synthesis and photobiological activity of N,N-disubstituted 4-amino-3-chloro-2H-thieno[2,3-h]-1-benzopyran-2-ones, 7-thioisosteres of 4-amino-3-chloroangelicins

Mosti, L.; Schenone, P.; Menozzi, G.; Romussi, G.; Baccichetti, F.; Carlassare, F.; Bordin, F.

Il Farmaco; Edizione Scientifica 39(2): 81-94

1984

ISSN/ISBN: 0430-0920
PMID: 6714412
Document Number: 226914
A convenient synthesis of a series of N,N-disubstituted 4-amino-3-chloro-2H-thienothiophen-4(5H)-ones . Some aspects of the photobiological activity of these thioangelicins were studied; three of them (IV a, e, f) appeared to inhibit DNA synthesis in Ehrlich ascites tumor cells. The most active compound, namely 3-chloro-4-morpholino-7-thioangelicin (IV e), afforded 70% of the antiproliferative effect of 8-MOP, but unlike this reference compound was unable to induce erythema on guinea pig skin. However, compounds (IV a, f) produced a slight erythema, thus suggesting that a relationship between antiproliferative and phototoxic effects does not exist.

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