Design, synthesis of N9– acyl substituted β-carboline derivatives containing 5-phenyl-2-furan moiety as potent anticancer agents was written by Huang, Zhi;Yang, Zhi-Kun;Chen, Si-Qing;Chen, Jian-Wei;Bao, Xiao-Ze;Ye, Xin-Yi;Wei, Bin;Cui, Zi-Ning;Li, Ya-Sheng;Wang, Hong. And the article was included in Results in Chemistry in 2022.COA of Formula: C11H8N2 This article mentions the following:
β-Carbolines are of great interest due to their broad spectrum of biochem. effects and pharmaceutical functions, especially antitumor activity. The N9 position at β-carboline is a modification site for important antitumor activity. Several phenylfuran derivatives displayed significant antitumor activity in our previous work. Here, we designed and preparated a series of novel N9-acyl substituted β-carboline derivatives containing 5-phenyl-2-furan moiety as potent anticancer agents. All newly synthesized compounds and β-carboline were evaluated for antitumor activity on five cancer cells. β-Carboline had only weak antitumor activity, while the introduction of the phenylfuran fragment significantly improved the activity. The primary structure-activity relationship study showed that 4-substituted phenylfuran played a key role in anti-cancer activity and compound 8 displayed superior than Camptothecin in anti-proliferative activity against breast cancer cells MCF-7. Flow cytometry studied revealed that compounds 8 and 15 effectively mediated MCF-7 apoptosis. This study lays a working foundation for the research and development of new broad-spectrum antitumor drugs based on β-carboline and phenylfurans, compound 8 would be great promise as a hit antitumor candidate in the future study. In the experiment, the researchers used many compounds, for example, 9H-Pyrido[3,4-b]indole (cas: 244-63-3COA of Formula: C11H8N2).
9H-Pyrido[3,4-b]indole (cas: 244-63-3) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.COA of Formula: C11H8N2
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles