AUTHOR=Guo Qingfeng , Chen Jinhua , Ren Yuwei , Yin Zhenhua , Zhang Juanjuan , Yang Baocheng , Wang Xuewei , Yin Wenbing , Zhang Wancun , Ding Gang , Chen Lin 

TITLE=Hydrazine-Containing Heterocycle Cytochalasan Derivatives From Hydrazinolysis of Extracts of a Desert Soil-Derived Fungus Chaetomium madrasense 375

JOURNAL=Frontiers in Chemistry

VOLUME=9

YEAR=2021

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2021.620589

DOI=10.3389/fchem.2021.620589

ISSN=2296-2646

ABSTRACT=<p>“Diversity-enhanced extracts” is an effective method of producing chemical libraries for the purpose of drug discovery. Three rare new cytochalasan derivative chaetoglobosins B<sub>1</sub>-B<sub>3</sub> (<bold>1</bold>–<bold>3</bold>) were obtained from chemically engineered crude broth extracts of <italic>Chaetomium madrasense</italic> 375 prepared by reacting with hydrazine monohydrate and four known metabolite chaetoglobosins (<bold>4–7</bold>) were also identified from the fungus. The structures were identified by NMR and MS analysis and electronic circular dichroism simulation. In addition, the antiproliferative activities of these compounds were also evaluated, and the drug-resistant activities of cytochalasans were evaluated for the first time. Compound <bold>6</bold> possessed potent activity against four human cancer cells (A549, HCC827, SW620, and MDA-MB-231), and two drug-resistant HCC827 cells (Gefitinib-resistant, Osimertinib-resistant) compared with the positive controls.</p>