UDC: 615.276:547.789:542.91

Aim. To accomplish the synthesis and screening of anticancer and antimicrobial activities of 1-[2-amino-4-methylthiazol-5-yl]-3-arylpropenones 2-10. Methods. The in vitro anticancer activity of compounds 4, 6, 8-10 has been established by DTP(Developmental Therapeutics Program) of the National Cancer Institute. The antibacterial and antifungal activities of synthesized thiazole-based derivatives were evaluated in vitro with the agar diffusion and broth microdilution methods to wards Gram-positive, Gram-negative bacteria and yeasts. For the synthesized compounds, the in silico drug-likeness screening using SwissADME online server is reported. Results. The novel 1-[2-amino-4-methylthiazol-5-yl]-3-arylpropenones were synthesized from 1-[2-amino-4-methylthiazol-5-yl]ethanones and various aromatic aldehydes in the Claisen–Schmidt condensation. The synthesized compound 9 was moderately active
against the leukemia CCRF-CEM and HL-60(TB), renal cancer UO-31 and breast cancer MCF7 cell lines. The antimicrobial screening led to identification of the active compound 10 against Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans. Conclusions. The results obtained herein provide a platform for structure-based optimization of these newly identified thiazole-based compounds for the anticancer and antibacterial drug design. K e y w o r d s: thiazoles, Claisen-Schmidt condensation, anticancer activity, antimicrobial activity, SwissADME

Nonsteroidal anti-inflammatory drugs (NSAIDs), used in the treatment of numerous diseases, can cause a number of side effects, the main of which is an ulcerogenic effect on the mucous membranes of the gastrointestinal tract. NSAIDs can also cause side effects in the hepato-biliary, cardiovascular, excretory systems, affect the functioning of the liver and lungs [1]. The mechanism of action of NSAIDs is based on the inhibition of the activity of cyclooxygenase (COX), which exists in two main isoforms COX-1 and COX-2, differ structurally and functionally [2, 3]. COX-1 is a constitutive isoform that is expressed throughout the body and synthesizes prostaglandins involved in numerous physiological processes. In particular, with the participation of COX-1, prostaglandins are formed. They regulate the secretion of hydrochloric acid and stimulate the formation of protective mucus in the stomach, influence the process of proliferation and intercellular integration in various organs, regulate vascular homeostasis, platelet aggregation, and kidney function. COX-2 is an inducible form of the enzyme, which expression increases during inflammation, ensuring the synthesis of relatively large concentrations of prostaglandins, that act as the inflammation mediators [4, 5]. Considering the numerous side effects of currently existing NSAIDs, the development of new anti-inflammatory drugs devoid of side effects is actively underway. In this sense, the compounds capable of simultaneous inhibiting the cyclooxygenase and lipoxygenase (LOX) pathways of arachidonic acid metabolism are of significant interest. Dual-acting COX/LOX inhibitors could provide multiple...