Synthesis and antiproliferative activity of new thiazole hybrids with [3.3.0]furofuranone or tetrahydrofuran scaffolds

New thiazole hybrids were synthesized and evaluated for their in vitro cytotoxicity against a panel of human malignant cell lines. The key steps the synthesis 3?7 involved initial condensation appropriate aldononitriles with cysteine ethyl ester hydrochloride, followed by subsequent treatment resulting thiazolines diazabicycloundecene to form ring. Bioisosteres 8 14 have been prepared after stereoselective addition 2-(trimethylsilyl)thiazole hemiacetals obtained periodate cleavage terminal diol functionality suitably protected d-glucose derivatives. analogues showed various antiproliferative activities cultures several tumour Hybrid 6 was most potent HeLa cells, exhibiting more than 10 4 times stronger activity both leads 1 2, respectively. active compound Raji cells hybrid 12, which nearly 2-fold clinical antitumour drug doxorubicin. All A549 respect lead 1, while compounds 7 slightly Preliminary structure?activity relationship analysis revealed that presence cinnamate group at C-3 position type increases molecular hybrids.