» Articles » PMID: 34531644

Benzopyrylium Salts As New Anticancer, Antibacterial, and Antioxidant Agents

Overview
Journal Med Chem Res
Publisher Springer
Specialty Chemistry
Date 2021 Sep 17
PMID 34531644
Citations 1
Authors
Affiliations
Soon will be listed here.
Abstract

Benzopyrylium salts are an unexplored class of compounds and as a first, this study reports them as potential therapeutic agents. In this effort we pursue the synthesis and in vitro anticancer, antibacterial and antioxidant properties of some novel benzopyrylium salts. The benzopyrylium salts were synthesized and further characterized via UV-vis, IR, H-NMR, C-NMR and mass spectrometry. The benzopyrylium salts were tested in vitro for anticancer activity across NCI 60 cell line panel. showed the best activity against the MDA-MB-435 cell line of melanoma cancer in terms of the least GI (1.78 μM), TGI (3.47 μM) and LC (6.77 μM) values and showed selectivity against melanoma, colon cancer and leukemia. Mechanistic studies indicate that this compound inhibits MCF-7 cancer cells by inducing apoptosis and abrogates colony formation and wound healing in the cancer cells. Antibacterial studies show that some of the benzopyrylium salts are active on (ATCC 29213) and the best active compound has a MIC of 8 μg/mL. Antioxidant studies indicate that they have good free radical scavenging properties ( showed activity 1.48 times ascorbic acid). Fulfillment of the Lipinski's parameters of the benzopyrylium salts in silico showed tremendous drug likeness as potential pharmacophore leads.

Citing Articles

Combined Transcriptome and Metabolome Analysis Reveals That the Potent Antifungal Pyrylium Salt Inhibits Mitochondrial Complex I in Candida albicans.

Lv Q, Yan L, Wang J, Feng J, Gao L, Qiu L Microbiol Spectr. 2023; :e0320922.

PMID: 36790175 PMC: 10100848. DOI: 10.1128/spectrum.03209-22.

References
1.
Monks A, Scudiero D, Skehan P, Shoemaker R, Paull K, Vistica D . Feasibility of a high-flux anticancer drug screen using a diverse panel of cultured human tumor cell lines. J Natl Cancer Inst. 1991; 83(11):757-66. DOI: 10.1093/jnci/83.11.757. View

2.
Jones J, Wang H, Karanam B, Theodore S, Dean-Colomb W, Welch D . Nuclear localization of Kaiso promotes the poorly differentiated phenotype and EMT in infiltrating ductal carcinomas. Clin Exp Metastasis. 2014; 31(5):497-510. PMC: 4065802. DOI: 10.1007/s10585-014-9644-7. View

3.
Jayaram B, Singh T, Mukherjee G, Mathur A, Shekhar S, Shekhar V . Sanjeevini: a freely accessible web-server for target directed lead molecule discovery. BMC Bioinformatics. 2013; 13 Suppl 17:S7. PMC: 3521208. DOI: 10.1186/1471-2105-13-S17-S7. View

4.
Karna P, Gundala S, Gupta M, Shamsi S, Pace R, Yates C . Polyphenol-rich sweet potato greens extract inhibits proliferation and induces apoptosis in prostate cancer cells in vitro and in vivo. Carcinogenesis. 2011; 32(12):1872-80. PMC: 3220609. DOI: 10.1093/carcin/bgr215. View

5.
Arora R, Schmitt D, Karanam B, Tan M, Yates C, Dean-Colomb W . Inhibition of the Warburg effect with a natural compound reveals a novel measurement for determining the metastatic potential of breast cancers. Oncotarget. 2015; 6(2):662-78. PMC: 4359247. DOI: 10.18632/oncotarget.2689. View