Targeted Discovery of Pentaketide Ansamycin Aminoansamycins A–G

Abstract

Ansamycins are a class of macrolactams with diverse bioactivities, characterized by the unique 3-amino-5-hydroxybenzoic acid moiety. In this study, the ansamycin gene cluster <i>aas</i> in <i>Streptomyces</i> sp. S35 was activated by the constitutive coexpression of two pathway-specific regulator genes <i>aas1</i> and <i>aas10</i>, and seven novel pentaketide ansamycin aminoansamycins A-G (<b>1</b>-<b>7</b>) were identified. Compound <b>4</b> with better antiproliferative activity indicated that the anthranilate analogues are probably promising building blocks for the production of unnatural ansamycins with improved activity.