engleski

Sinteza i antiproliferativna aktivnost novih amidino-supstituiranih arilnih bisbenzotiazola

2-Arylbenzothiazole derivatives are of considerable interest due to their diverse pharmaceutical properties and have emerged as a privileged scaffold in drug discovery bearing remarkable activity profiles in non-invasive diagnosis of Alzheimer's disease and antitumour effects. Strong anti-proliferative effects on some tumour cell lines were previously shown for isomeric imidazolinyl-substituted phenylene-bisbenzothiazole, and imidazolinyl- substituted phenyl- and naphtyl-benzothiazoles. These findings have led us to further investigate this class of compounds by introducing different types of amidinic substituents with the aim of improving activity and selectivity on different human tumour cell lines. Additionally, we explored reaction conditions for sustainable approach to synthesis of amidino-substituted phenylene- bisbenzothyazoles by condensation reaction from the corresponding bis(2-aminophenyl) disulfide and aldehyde using glycerol as a green solvent. We found new efficient and sustainable synthetic method for preparation of isomeric amidino-substituted derivatives of bisbenzothiazolyl-phenylenes and naphtalenes. Generally, the in vitro anti-proliferative screening of novel diamidino-bisbenzothiazolyl derivatives revealed strong activity on tested tumour cell lines (SW620, HepG2, CFPAC-1 and HeLa) depending on the type of amidinic substituent as well as positions of benzothiazolyl moieties.

synthesis, amidino-substituted benzothiazoles, anti-proliferative activity

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