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

Dmitrii A. Aksenov; Alexander V. Aksenov; Lidiya A. Prityko; Nicolai A. Aksenov; Liliya V. Frolova; Michael Rubin

doi:10.3390/M1307

Molbank (Dec 2021)

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

Dmitrii A. Aksenov,
Alexander V. Aksenov,
Lidiya A. Prityko,
Nicolai A. Aksenov,
Liliya V. Frolova,
Michael Rubin

Affiliations

Dmitrii A. Aksenov: Department of Chemistry, North Caucasus Federal University, 1a Pushkin St., 355017 Stavropol, Russia
Alexander V. Aksenov: Department of Chemistry, North Caucasus Federal University, 1a Pushkin St., 355017 Stavropol, Russia
Lidiya A. Prityko: Department of Chemistry, North Caucasus Federal University, 1a Pushkin St., 355017 Stavropol, Russia
Nicolai A. Aksenov: Department of Chemistry, North Caucasus Federal University, 1a Pushkin St., 355017 Stavropol, Russia
Liliya V. Frolova: Department of Chemistry, Purdue University, Science Building R488, 2101 East Coliseum Blvd., Fort Wayne, IN 46805, USA
Michael Rubin: Department of Chemistry, North Caucasus Federal University, 1a Pushkin St., 355017 Stavropol, Russia

DOI: https://doi.org/10.3390/M1307
Journal volume & issue: Vol. 2022, no. 1
p. M1307

Abstract

Read online

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.

Published in Molbank

ISSN: 1422-8599 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Chemistry: Inorganic chemistry
Website: https://www.mdpi.com/journal/molbank

About the journal

Abstract

Keywords