European Journal of Medicinal Chemistry 2002-04-01

Synthesis and cytotoxic evaluation of alpha-methylene-gamma-butyrolactone bearing naphthalene and naphtho[2,1-b]furan derivatives.

Kuan-Han Lee, Bor-Ruey Huang

Index: Eur. J. Med. Chem. 37(4) , 333-8, (2002)

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Abstract

Naphthalene alpha-methylene-gamma-butyrolactones exhibits a unique cytotoxicity profile. They are highly cytostatic for leukaemia cancer cells but are not cytocidal. For almost all the solid tumours tested, they are both cytostatic and cytocidal. Substitution of a bromo atom on either naphthalene or both naphthalene and gamma-phenyl moiety of the lactone enhanced potency while retaining the same cytotoxicity profile. The tricyclic naphtho[2,1-b]furan derivatives, prepared from 2-hydroxy-1-naphthaldehyde in an efficient pathway, also possess the same cytotoxicity profile.