Synthesis and cytotoxic activity of new indolylpyrrole derivatives

• Published in: Arabian journal of chemistry Vol. 14; no. 7; p. 103209
• Main Authors: Radwan, Mohamed A.A., Al Rugaie, Osamah, Al Abdulmonem, Waleed, Alfaifi, Mohammad Y., Elbehairi, Serag Eldin I.
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.07.2021; Elsevier
• Subjects: Cytotoxicity; Indole; LS174T; PC-3; Pyrrole; SKOV3; SRB assay; SKOV3; LS174T; Indole; Pyrrole; Cytotoxicity; PC-3; SRB assay
• ISSN: 1878-5352; 1878-5379
• DOI: 10.1016/j.arabjc.2021.103209

[Display omitted] The current approach described the synthesis of a new series of indolylpyrrole derivatives through multicomponent reaction of α-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 adenocarcinoma (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 µg/ml, respectively. In human ovarian carcinoma (SKOV3), the compounds 5a, and 5i have stronger cytotoxicity with IC50s of 1.20 ± 0.04, 1.90 ± 0.50 µg/ml, respectively than the standard doxorubicin (IC50 = 2.20 ± 0.02 µg/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 µg/ml. Consequently, this effort offers groundwork for additional examination of nominated indolylpyrroles as antiproliferative agents.