Synthesis and antitumor activity evaluation of indole-2-carbohydrazide derivatives was written by Wang, Ning-wei;Han, Ying-long;Zhang, Guo-qiang;Huang, Xue-tao;Liu, Ming-hui;Yang, Ye-xian;Wang, Hai-jun;Bu, Ming. And the article was included in Huaxue Shiji in 2020.Electric Literature of C9H6ClNO This article mentions the following:
Using 5-chloroindole-2-carboxylic acid as starting material, seven indole-2-carbohydrazide derivatives had been synthesized, and their structures were confirmed by MS, 1HNMR and 13CNMR. The antiproliferative activity of the compounds was evaluated against human colon cancer cells (HCT116), human breast cancer cells (MCF-7) and human lung cancer cells (A549) by methylthiazolyl tetrazolium (MTT) staining. The results showed that 5-chloro-N’-((5-fluoro-1H-indol-3-yl) methylene)-1H-indole-2-carbohydrazide displayed significant inhibitory activity against HCT116 cell lines with IC50 value of 7.72μmol/L. Furthermore, the compound could induce HCT116 cells apoptosis in a dose-dependent manner. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Electric Literature of C9H6ClNO).
5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Electric Literature of C9H6ClNO
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