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Synthesis and Cytotoxicity of Thieno[2,3-b]Pyridine Derivatives Toward Sensitive and Multidrug-Resistant Leukemia Cells

Salah A. Al-Trawneh, Amer H. Tarawneh, Anastassiya V. Gadetskaya, Ean-Jeong Seo, Mohammad R. Al-Ta’ani, Samir A. Al-Taweel, Mustafa M. El-Abadelah

Abstract


A new series of substituted ethyl 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates 3ae were prepared by utilizing ethyl 2-chloro-7-cyclopropyl-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylate (1) and replacing of the 2-chlorine with anions obtained from phenol (2a), salicylaldehyde derivatives 2bd or thiophenol (2e), leading to the respective ethyl 7-cyclopropyl-2-(2-aryloxo)-3-nitro-4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxylates 3ae. The new compounds were evaluated for their in vitro cytotoxicity towards sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells. The screening revealed that compounds 3a, 3b, and 3e inhibited the growth of both cell lines. Compound 3b, with a phenol moiety, exhibited the highest growth inhibitory activity against CEM/ADR5000 and CCRF-CEM cells with IC50 values 4.486 ± 0.286 and 2.580 ± 0.550 µM, respectively. Collectively, the presented results demonstrate that the synthesized thieno[2,3-b]pyridines warrant further exploration for potential use as anti-cancer agents.


Keywords


Thieno[2,3-b]pyridine; Multidrug resistance; Cytotoxicity.

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DOI: http://dx.doi.org/10.17344/acsi.2020.6609

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Copyright (c) 2020 Salah A. Al-Trawneh, Amer H. Tarawneh, Anastassiya V. Gadetskaya, Ean-Jeong Seo, Mohammad R. Al-Ta’ani, Samir A. Al-Taweel, Mustafa M. El-Abadelah

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