AUTHOR=Lin Xiao , Zhou Yongjun , Liu Liyun , Zhu Hongrui , Chen Yeping , Wang Shuping , Sun Fan , Chai Ling , Liu Buming , Xu Shihai , Lin Hou-Wen 

TITLE=Compound Discovery and Structure-Activity Relationship Study of Neoantimycins Against Drug-Resistant Cancer Cells

JOURNAL=Frontiers in Chemistry

VOLUME=Volume 7 - 2019

YEAR=2019

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2019.00481

DOI=10.3389/fchem.2019.00481

ISSN=2296-2646

ABSTRACT=Four neoantimycins H-K (1-4) with C1-keto, including the new ones (1-2), were isolated from the culture of Streptomyces conglobatus RJ8. After enzymatically converting into their respective reduced type derivatives (5-8) in vitro, the absolute structures of 1-8 were established/reconfirmed by analyzing hydrolyzed components. The obtained NATs (4, 7 and 8) exhibited excellent cytotoxicity against drug-resistant colon and gastric cancer cells but low toxicity in the noncancerous cell. Further SAR investigation suggested that C1-hydroxyl, C9-isobutyl, and N-formyl contribute to the antiproliferation remarkably.