AUTHOR=Gao Zilin , Chen Yu , Nie Yufei , Chen Keming , Cao Xiufang , Ke Shaoyong 

TITLE=Structural diversity-guided optimization of carbazole derivatives as potential cytotoxic agents

JOURNAL=Frontiers in Chemistry

VOLUME=11

YEAR=2023

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2023.1104868

DOI=10.3389/fchem.2023.1104868

ISSN=2296-2646

ABSTRACT=<p>Carbazole alkaloids, as an important class of natural products, have been widely reported to have extensive biological activities. Based on our previous three-component reaction to construct carbazole scaffolds, we introduced a methylene group to provide a rotatable bond, and designed series of carbazole derivatives with structural diversity including carbazole amide, carbazole hydrazide and carbazole hydrazone. All synthesized carbazole derivatives were evaluated for their <italic>in vitro</italic> cytotoxic activity against 7901 (gastric adenocarcinoma), A875 (human melanoma) and MARC145 (African green monkey kidney) cell lines. The preliminary results indicated that compound <bold>14a</bold> exhibited high inhibitory activities on 7901 and A875 cancer cells with the lowest IC<sub>50</sub> of 11.8 ± 1.26 and 9.77 ± 8.32 μM, respectively, which might be the new lead compound for discovery of novel carbazole-type anticancer agents.</p>