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Mohareb, Rafat M.; Klapötke, Thomas M.; Reinhardt, Elena (2018): Uses of dimedone for the synthesis of thiazole derivatives as new anti-tumor, c-Met, tyrosine kinase, and Pim-1 inhibitions. In: Medicinal Chemistry Research, Vol. 27, No. 11-12: pp. 2494-2511
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Abstract

A series of heterocyclic compounds derived from dimedone were synthesized through the first reaction of dimedone with elemental sulfur and phenylisothiocyanate followed by heterocyclization of the produced thiazole derivative through its reaction with different chemical reagents. All the synthesized compounds were determined by elemental analysis, H-1 NMR, C-13 NMR, and MS. The newly synthesized compounds were evaluated for their in vitro cytotoxic activity against c-Met kinase, and the six typical cancer cell lines (A549, H460, HT-29, MKN-45, U87MG, and SMMC-7721). All target compounds were initially tested for their anti-proliferative activity against human prostatic cancer PC-3 cell line. The most promising compounds 5a, 7a, 7b, 9c, 9d, 9i, 9k, 12a, 12d, 14b, and 15d were further investigated against tyrosine kinase (c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR). Compounds 7a, 7b, 9c, 9d, 9k, 14b, and 15c were selected to examine their Pim-1 kinase inhibition activity where compounds 7a, 9d, 9k, and 15c showed high activities.