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Aranciamycin analogs generated by combinatorial biosynthesis show improved antitumor activity

Aranciamycin analogs generated by combinatorial biosynthesis show improved antitumor activity,10.1007/s00253-008-1515-1,Applied Microbiology and Biote

Aranciamycin analogs generated by combinatorial biosynthesis show improved antitumor activity   (Citations: 2)
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Expression of the aranciamycin biosynthetic gene cluster in Streptomyces diastatochromogenes Tü6028 resulted in production of four novel compounds, aranciamycins E, F, G, and H with different decorations in the tetracyclic backbone. Two derivatives contain a d-amicetose moiety at C7 (aranciamycins F and G), two are hydroxylated at position C1 (aranciamycins E and G), and one is hydroxylated at C13 (aranciamycin F). Analysis of the biological activities of the aranciamycins against two human tumor cell lines—MCF-7 and MATU—shows surprising impact of the hydroxyl group at position C1 on activity. As aranciamycins E and G were the most active derivatives, hydroxylation of the C1 appears to coincide with increased antitumor activity of aranciamycins.
Journal: Applied Microbiology and Biotechnology - APPL MICROBIOL BIOTECHNOL , vol. 80, no. 1, pp. 15-19, 2008
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