Synthesis and Antiproliferative Ativity of 2,4-Bis(indol-3-yl)pyrrole Derivatives: Marine Nortopsentin Analogs

Rdwan, Mohamed; Alrugaie, Osama; Al Abdulmonem, Waleed; Alfaifi, Mohammad; Elbehairi, Serag Eldin

doi:10.21608/ejchem.2021.84060.4117

Synthesis and Antiproliferative Ativity of 2,4-Bis(indol-3-yl)pyrrole Derivatives: Marine Nortopsentin Analogs

Document Type : Original Article

Authors

¹ Department of Applied Organic Chemistry, National Research Center, Dokki 12622, Egypt

² Department of Basic Medical Sciences, Unaizah College of Medicine and Medical Sciences, Qassim University, Unaizah, Saudi Arabia

³ Department of Pathology, College of Medicine, Qassim University, Buraidah, Saudi Arabia. (dr.waleedmonem@qu.edu.sa)

⁴ King Khalid University, Faculty of Science, Biology Department, Abha 9004, Saudi Arabia

⁵ Cell Culture Lab, Egyptian Organization for Biological Products and Vaccines (VACSERA Holding Company), 51 Wezaret El-Zeraa St., Agouza, Giza, Egypt

10.21608/ejchem.2021.84060.4117

Abstract

Abstract
In this study, a series of nortopsentin analogs (2,4-bis(indol-3-yl)pyrrole derivatives) were designed, synthesized, and tested for their in vitro cytotoxic activity against three cell lines: human prostate adenocarcinoma (PC-3), human ovary adenocarcinoma (SKOV3), and human Dukes' type B colorectal adenocarcinoma (LS-174T). Compounds 5a, 5e, 5h, 5j, and 5k had stronger antiproliferative activity against SKOV3, compound 5h and 5b against LS-174T, and compound 5e against PC-3 than the known doxorubicin drug. As a result, this work provides the framework for further research into 2,4-bis(indol-3-yl)pyrrole derivatives as antiproliferative drugs.

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