Synthesis and Anticancer Evaluation of Novel Indole Based Arylsulfonylhydrazides against Human Breast Cancer Cells

A series of novel indole based sulfonohydrazide derivatives (5a-k) containing morpholine heterocyclic ring were synthesized through multistep chemical reactions. The target compounds (5a-k) were prepared by the reaction of substituted phenyl sulfonylhydrazides (2a-k) with morpholine derivative of indole 3-carboxaldehyde. All the target compounds were screened for their anticancer activity in vitro against the estrogen receptor-positive breast cancer line MCF-7 and triple-negative breast cancer cell line, MDA-MB-468. It was found that among all the evaluated compounds, the chemotype 4-chloro-N '-((1-(2-morpholinoethyl)-1H-indol-3-yl)methylene)benzenesulfonohydrazide (5f) showed promising inhibition of both MCF-7 and MDA-MB-468 cancer cells with the respective IC50 values of 13.2 mu M and 8.2 mu M. Compound 5f was found to be nontoxic against HEK 293 noncancerous cells in the studied concentration range, therefore indicating that such chemotypes inhibit the proliferation of cancerous cells selectively and significantly.

Automated summary

A series of novel indole based sulfonohydrazide derivatives containing morpholine heterocyclic ring were synthesized and evaluated for their anticancer activity. Compound 5f showed promising inhibition of breast cancer cells and was found to be non-toxic to noncancerous cells.