Mithramycin (MTM) is an anticancer agent/antibiotic that is produced by soil bacteria of the genus Streptomyces. By inactivating the last enzyme in the MTM biosynthetic pathway, the analogues MTM SK, MTM SDK, and MTM SA have been produced. MTM SK and SDK show improved anti-cancer activity in comparison to MTM, but MTM SA, in which the 3-side chain is terminated by a carboxylic acid, exhibits decreased activity. This carboxylic acid was modified by the addition of several different small molecules to generate a series of new analogues. The new MTM analogues were able to improve the cytotoxicity compared to that of MTM SA, displaying significantly lower IC<sub>50 </sub>values than even MTM SK when tested on the A549 non-small cell lung cancer cell line.<br/>

Modification of mithramycin SA for improved cytotoxicity

2019 Spring National Meeting

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