Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Abstract

Currently, the development of anticancer drug resistance is significantly restricted the clinical efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely prevalent and considered to be the major challenges of this century, which concerns the medical community all over the world. Consequently, investigating small molecule antitumor agents, which could decrease drug resistance and reduce unpleasant side effect is more desirable. 2-aminothiazole scaffold has emerged as a promising scaffold in medicinal chemistry and drug discovery research. This nucleus is a fundamental part of some clinically applied anticancer drugs such as dasatinib and alpelisib. Literature survey documented that different 2aminothiazole analogs exhibited their potent and selective nanomolar inhibitory activity against a wide range of human cancerous cell lines such as breast, leukemia, lung, colon, CNS, melanoma, ovarian, renal, and prostate. In this paper, we have reviewed the progresses and structural modification of 2-aminothiazole to pursuit potent anticancers and also highlighted in vitro activities and in silico studies. The information will useful for future innovation.

Docking and synthesis of some 2-aminothiazole derivatives as antimicrobial agents

“…Chloroacetyl chloride (0.01 mol) was added dropwise with cooling to the corresponding hydrazones (6,8,9,11,12,13,15) (0.005mol) in a (0.01 mol) triethylamine in 40 ml of dioxane with stirring at room temperature for 20 minutes, then the mixture was refluxed for 8 hours. The reaction mixture was concentrated then poured into ice water; crude compounds were isolated, filtered, dried, and recrystallized from absolute ethanol, physical, and IR data for compounds (21)(22)(23)(24)(25)(26)(27)…”

“…While the physical properties and infrared data of the synthetic compounds (16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27) were listed in Table .5. The 1 H-NMR of the corresponding hydrazone compounds (6)(7)(8)(9)(10)(11)(12)(13)(14)(15) show the following peaks δ (ppm):…”

“…The monolactam ring of the 2-amino thiazole derivative compound 23 showed partial activity against Ca fungal species. Further studies of the 2aminothiazole derivatives as anticancer activity [26].…”

Biological Evaluation of 3-Aminoisoquinolin-1(2H)-one Derivatives as Potential Anticancer Agents Authors Lyudmyla Potikha

“…In essence, the aim of molecular hybridization is to produce a single chemical entity through combination of two or more distinct pharmacophore subunits present in the structures of two or more known bioactive derivatives. For example, pyrazole and thiazole derivatives can be cited as examples of the successful application of this strategy [2][3][4][5][6]. 5) is also based on 3-(pyrazol-3ylamino)-isoquinolin-1(2H)-ones [12].…”

“…The strong activity in suppressing proliferation and growth of glioblastoma cells [13], colorectal (SW620, HT29, GI50 = 23.8÷24.13 M) [14] and CNS (SF-295, GI = 55%) [15] human cancer cell lines was found for condensed derivatives having a 3-aminoisoquinolinone moiety (6). The unsaturated 5H-benzo [4,5]imidazo [1,2b]isoquinolin-1-one (7) exhibited significant Cdc25B inhibition (IC50 = 5.3 M) [11]. In this context, the consolidation of the 3aminoisoquinolinone template and novel carbo/heteroaromatic rings as novel pharmacophores seems to be promising for obtaining highly effective anticancer drugs.…”