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  • High Antiproliferative Activity of Hydroxythiopyridones over Hydroxypyridones and Their Organoruthenium Complexes.

High Antiproliferative Activity of Hydroxythiopyridones over Hydroxypyridones and Their Organoruthenium Complexes.

Biomedicines (2021-01-31)
Md Salman Shakil, Shahida Parveen, Zohaib Rana, Fearghal Walsh, Sanam Movassaghi, Tilo Söhnel, Mayur Azam, Muhammad Ashraf Shaheen, Stephen M F Jamieson, Muhammad Hanif, Rhonda J Rosengren, Christian G Hartinger
ABSTRACT

Hydroxypyr(id)ones are a pharmaceutically important class of compounds that have shown potential in diverse areas of drug discovery. We investigated the 3-hydroxy-4-pyridones 1a-1c and 3-hydroxy-4-thiopyridones 1d-1f as well as their Ru(η6-p-cymene)Cl complexes 2a-2f, and report here the molecular structures of 1b and 1d as determined by X-ray diffraction analysis. Detailed cell biological investigations revealed potent cytotoxic activity, in particular of the 3-hydroxy-4-thiopyridones 1d-1f, while the Ru complexes of both compound types were less potent, despite still showing antiproliferative activity in the low μM range. The compounds did not modulate the cell cycle distribution of cancer cells but were cytostatic in A549 and cytotoxic in NCI-H522 non-small lung cancer cells, among other effects on cancer cells.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Lawesson reagent, 97%
Sigma-Aldrich
N-Ethylbenzylamine, 97%
Sigma-Aldrich
SAHA, ≥98% (HPLC)