Abstract
Single-step synthesis of novel 4-hydrazinothiazole derivatives 6a-e was achieved under mild conditions via the sequential four components method using isothiocyanate, aminoguanidine, carbonyl adduct, and α-haloketone derivatives. Deprotection of these hydrazinothiazoles was influenced by acylation, providing a novel group of diacylated molecular structures with a broader scope for the design of thiazolyl-containing drugs 7a and 7b. FTIR, 1 H/13 C NMR, LC-MS spectroscopy, and CHN elemental analyses have been used to study the compounds' chemical structures. Using an MTT assay on Human Periodontal Ligament Fibroblast (HPDLF) cells, the 4-hydrazinothiazole derivatives were screened for cytotoxicity in an in vitro cytotoxicity investigation. The 4-hydrazinothiazole compound 6b bearing an isopropylidene-hydrazino group demonstrated a strongly potent cytotoxicity against CAKI1 (IC50 = 1.65±0.24 μM) and A498 (IC50 of 0.85±0.24 μM). Furthermore, the chloroacetyl-containing thiazole compound 7a has displayed efficient inhibition of growth against the test cell lines CAKI1 and A498 at low micromolar IC50 of 0.78 and 0.74 μM, respectively.
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