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In Vitro Antitumor Structure–Activity Relationships of threo/trans/threo mono-Tetrahydrofuranic Acetogenins: Correlations With Their Inhibition of Mitochondrial Complex I

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In this study we evaluated a mono-tetrahydrofuranic subgroup of natural acetogenins that had shown in previous enzyme inhibition studies different potency trends compared with the bis-tetrahydrofuranic acetogenin subgroup. The compounds were tested against colon, breast, lung, liver, and ovarian tumor cell lines. A drug-resistant ovarian cell line was also included in the panel. In general the compounds were more potent than doxorubicin. The goal was to determine how well the mitochondrial complex I inhibition correlates with the in vitro antitumor potency of these natural mono-tetrahydrofuranic acetogenins and of some derivatives. The results indicate that both the reduction of the terminal γ-lactone after its translactonization and the introduction of an hydroxylimine group in the alkyl chain, near the mono-tetrahydrofuranic moiety, increased the antitumor activity, even against the doxorubicin-resistant cell line.
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Keywords: Acetogenins; Cancer; Cytotoxicity; Mitochondrial respiratory chain inhibitors; Tumor cell line growth inhibitors

Document Type: Research Article

Affiliations: 1: *CIBE-Merck Research Laboratories, Merck, Sharp & Dohme de España S.A., C/ Josefa Valcárcel, 38, Madrid 28027, Spain 2: †Departament de Farmacologia Facultat de Farmàcia, Universitat de València, Avgd. Vicent Andrés Estellés s/n, Burjassot 46100, València, Spain

Publication date: January 1, 2003

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