Synthesis and cytotoxic activity of new indolylpyrrole derivatives

The current approach described the synthesis of a new series of indolylpyrrole derivatives through multicomponent reaction of a-cyano chalcones, appropriate aldehydes, and ammonium acetate in refluxed acetic acid. The chemical structures of the designed compounds were confirmed with spectroscopic data and elemental analysis and then tested for their in vitro cytotoxic activity by SRB assay method towards three cell lines involving human Prostate adenocarcinoma; metastatic cells (PC-3), human ovary adenocarcinoma (SKOV3) and human dukes' type B, colorectal adeno-carcinoma (LS 174 T). Most significant activity provided with compounds 5c, 5h and, 5j against prostate cancer cells (PC-3) with IC50s of 3.30 +/- 0.20, 3.60 +/- 0.10, and 3.60 +/- 0.90 mg/ml, respec-tively. In human ovarian carcinoma (SKOV3), the compounds 5a, and 5i have stronger cytotoxicity with IC50s of 1.20 +/- 0.04, 1.90 +/- 0.50 mg/ml, respectively than the standard doxorubicin (IC50 = 2.20 +/- 0.02 mg/ml). On the other hand, only compound 5a has the ability to diminish the viability of LS174T cells in an active manner with IC50 2.80 +/- 0.10 mg/ml. Consequently, this effort offers groundwork for additional examination of nominated indolylpyrroles as antiprolifer-ative agents . (c) 2021 The Author(s). Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

Automated summary

The study described the synthesis of a new series of indolylpyrrole derivatives and tested their in vitro cytotoxic activity against prostate cancer cells, ovarian cancer cells, and colorectal cancer cells. Some compounds exhibited potent anticancer activity, laying the groundwork for further exploration of these compounds as antiproliferative agents.