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Communication

Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products

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Department of Chemistry, North Caucasus Federal University, 1a Pushkin St., 355017 Stavropol, Russia
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Department of Chemistry, Purdue University, Science Building R488, 2101 East Coliseum Blvd., Fort Wayne, IN 46805, USA
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Department of Chemistry, University of Kansas, 1567 Irving Hill Road, Lawrence, KS 66045, USA
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Authors to whom correspondence should be addressed.
Academic Editor: Hideto Miyabe
Molbank 2022, 2022(1), M1307; https://doi.org/10.3390/M1307
Received: 1 December 2021 / Revised: 18 December 2021 / Accepted: 20 December 2021 / Published: 22 December 2021
2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly developed protocol for chemoselective mono-methylation of hydroxamic acids. The cytotoxicity of these derivatives against the HeLa cell line was evaluated and found to be inferior compared to the parent lead compounds. View Full-Text
Keywords: hydroxamic acid; indoles; methylation; anti-cancer activity hydroxamic acid; indoles; methylation; anti-cancer activity
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MDPI and ACS Style

Aksenov, D.A.; Aksenov, A.V.; Prityko, L.A.; Aksenov, N.A.; Frolova, L.V.; Rubin, M. Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products. Molbank 2022, 2022, M1307. https://doi.org/10.3390/M1307

AMA Style

Aksenov DA, Aksenov AV, Prityko LA, Aksenov NA, Frolova LV, Rubin M. Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products. Molbank. 2022; 2022(1):M1307. https://doi.org/10.3390/M1307

Chicago/Turabian Style

Aksenov, Dmitrii A., Alexander V. Aksenov, Lidiya A. Prityko, Nicolai A. Aksenov, Liliya V. Frolova, and Michael Rubin. 2022. "Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products" Molbank 2022, no. 1: M1307. https://doi.org/10.3390/M1307

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