Journal
MOLECULES
Volume 26, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/molecules26103057
Keywords
synthesis; 4-thiazolidinones; Ciminalum; anticancer activity; SAR analysis
Funding
- Ministry of Healthcare of Ukraine [0121U100690]
- National Research Foundation of Ukraine [2020.02/0035]
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A series of novel 5-[(Z,2Z)-2-chloro-3-(4-nitrophenyl)-2-propenylidene]-thiazolidinones were synthesized, with compound 2h showing the highest level of antimitotic activity against various cancer cell lines. Hit compounds were found to have low toxicity towards normal human blood lymphocytes and a fairly wide therapeutic range. The significance of specific substituents in the 4-thiazolidinone derivatives for anticancer cytotoxicity levels was established.
A series of novel 5-[(Z,2Z)-2-chloro-3-(4-nitrophenyl)-2-propenylidene]-thiazolidinones (Ciminalum-thiazolidinone hybrid molecules) have been synthesized. Anticancer activity screening toward the NCI60 cell lines panel, gastric cancer (AGS), human colon cancer (DLD-1), and breast cancer (MCF-7 and MDA-MB-231) cell lines allowed the identification of 3-{5-[(Z,2Z)-2-chloro-3-(4-nitrophenyl)-2-propenylidene]-4-oxo-2-thioxothiazolidin-3-yl}propanoic acid (2h) with the highest level of antimitotic activity with mean GI(50)/TGI values of 1.57/13.3 mu M and a certain sensitivity profile against leukemia (MOLT-4, SR), colon cancer (SW-620), CNS cancer (SF-539), melanoma (SK-MEL-5), gastric cancer (AGS), human colon cancer (DLD-1), and breast cancers (MCF-7 and MDA-MB-231) cell lines. The hit compounds 2f, 2i, 2j, and 2h have been found to have low toxicity toward normal human blood lymphocytes and a fairly wide therapeutic range. The significant role of the 2-chloro-3-(4-nitrophenyl)prop-2-enylidene (Ciminalum) substituent in the 5 position and the substituent's nature in the position 3 of core heterocycle in the anticancer cytotoxicity levels of 4-thiazolidinone derivatives have been established
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