Synthesis and anticancer activity of novel 3,6-disubstituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives
| Autor: | Vasiliki Sarli, Constantinos Potamitis, Panayiotis Dalezis, Charalambos Camoutsis, Georgios Charitos, Panagiotis Zoumpoulakis, Dimitrios T. Trafalis |
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| Rok vydání: | 2019 |
| Předmět: |
Chemistry(all)
Stereochemistry Research areas Cytotoxicity General Chemical Engineering Triazole Heterocycles 01 natural sciences Anticancer activity lcsh:Chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Thiadiazoles In vivo 010405 organic chemistry Chemistry Kinase General Chemistry Triazoles Combinatorial chemistry In vitro 3. Good health 0104 chemical sciences lcsh:QD1-999 030220 oncology & carcinogenesis Chemical Engineering(all) 1 3 4 thiadiazole derivatives |
| Zdroj: | Arabian Journal of Chemistry, Vol 12, Iss 8, Pp 4784-4794 (2019) |
| ISSN: | 1878-5352 |
| DOI: | 10.1016/j.arabjc.2016.09.015 |
| Popis: | The development of new antitumor agents is one of the most pressing research areas in medicinal chemistry and medicine. The importance of triazole and thiadiazole rings as scaffolds present in a wide range of therapeutic agents has been well reported and has driven the synthesis of a large number of novel antitumor agents. The presence of these heterocycles furnishes extensive synthetic possibilities due to the presence of several reaction sites. Prompted by these data we designed, synthesized and evaluated a series of novel 3,6-disubstituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives as potential anticancer agents. We emphasized in the strategy of combining two chemically different but pharmacologically compatible molecules (the 1,2,4-triazole and 1,3,4 thiadiazole) in one frame. Several of the newly synthesized 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives showed substantial cytostatic and cytotoxic antineoplastic activity invitro, while they have produced relatively low acute toxicities invivo, giving potentially high therapeutic ratios. Insilico screening has revealed several protein targets including apoptotic protease-activating factor 1 (APAF1) and tyrosine-protein kinase HCK which may be involved in the biological activities of active analogues. Keywords: Triazoles, Thiadiazoles, Heterocycles, Anticancer activity, Cytotoxicity |
| Databáze: | OpenAIRE |
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