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In Vitro and In Vivo Evaluation of Two Rational-Designed Nonpeptidic Farnesyltransferase Inhibitors on HT29 Human Colon Cancer Cell Lines

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FTase inhibitors constitute a new class of potential cancer therapeutics, especially in colorectal cancer where K-ras-selective mutations exist and have a role in tumorigenesis. The synthesis and biological evaluation of two nonpeptidic molecules (13 and 16) designed on the basis of a zinc chelator imidazole linked to two aromatic fragments able to fit in the “exit groove” and in the “A2 binding site” of FTase are described. These molecules are characterized respectively by a flexible phenylmethyl chain and a more constrained scaffold so as to evaluate their respective influences on site recognition. They have been evaluated in vitro and in vivo against human colon cancer cell lines and 13 not only inhibited tumor growth but also showed no toxic effects at the dose used.
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Keywords: Colon cancer; Farnesyltransferase inhibitors; Ras

Document Type: Research Article

Affiliations: 1: Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, BP 83, 3 rue du Professeur Laguesse, 59006 Lille, France 2: Cellvax, Parc Eurasanté, 180 avenue Eugène Avinée, 59120 Loos, France

Publication date: March 1, 2006

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  • Formerly: Oncology Research Incorporating Anti-Cancer Drug Design
    Oncology Research Featuring Preclinical and Clincal Cancer Therapeutics publishes research of the highest quality that contributes to an understanding of cancer in areas of molecular biology, cell biology, biochemistry, biophysics, genetics, biology, endocrinology, and immunology, as well as studies on the mechanism of action of carcinogens and therapeutic agents, reports dealing with cancer prevention and epidemiology, and clinical trials delineating effective new therapeutic regimens.
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