Synthesis and Anticancer Activity of Isatin, Oxadiazole and 4-Thiazolidinone Based Conjugates

Maryan Lelyukh, Dmytro Havrylyuk and Roman Lesyk
Affiliation: 
Department of Pharmaceutical, Organic and Bioorganic Chemistry Danylo Halytsky Lviv National Medical University 69, Pekarska str., 79010 Lviv, Ukraine; dr_r_lesyk@org.lviv.net, roman.lesyk@gmail.com
DOI: 
https://doi.org/10.23939/chcht09.01.029
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Abstract: 
Following the N-alkylation reaction of starting 2-chloro-N-(5-aryl-1,3,4-oxadiazol-2-yl)-acetamides 1a-c with 2,4-thiazolidinedione or 5-sudstituted isatins the corresponding non-condensed oxadiazole derivatives with thiazolidine 2a-c or isatin 4a-h fragments were synthesized. The obtained compounds have been used in Knoevenagel condensation with 5R-isatin (for 2a-c) or 4-thiazolidinone derivatives (for 4a-h) for synthesis of the appropriate 5-ylidenederivatives 3a-g, 5a-k and 6a-d. Anticancer activity of eight synthesized compounds was evaluated toward 60 human tumor cell lines panel in National Cancer Institute.
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