Discovery, synthesis, and cytotoxic evaluation of isoquinolinequinones produced by Streptomyces albidoflavus derived from lichen.

ABSTRACT: Four isoquinolinequinones (1-4) were isolated from the fermentation broth of Streptomyces albidoflavus which were derived from lichens. Among them, mansouramycin H (1) was identified as a new isoquinolinequinone by comprehensive spectroscopic data analysis. The mansouramycins from S. albidoflavus presented broad cytotoxic activities, especially against MDA-MB-231, but the SAR and mechanism were still unclear. The total synthesis of mansouramycin H (1) and its twenty-three derivatives were completed and their cytotoxic activities against MDA-MB-231 were evaluated in vitro. Primary SAR revealed that the piperazine moieties introduced into the amino group at C-7 could improve the activities of mansouramycins. Benzoyl and phenylacetyl groups on piperazine fragments had bet

SUBMITTER: Jin Y 

PROVIDER: S-EPMC10682742 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature