Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles

One of the promising methods of creating antitumor drugs is the screening of potential antitumor agents among synthesized compounds. Nitrogen-based heterocycle analogues are an extremely important class of organic substances that are widely used in medical chemistry. [1,2,4]Triazolo[3,4-b][1,3,4] th...

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Autores principales:	I. І. Myrko, Yu. І. Horak, T. I. Chaban, І. V. Drapak, V. S. Matiychuk
Formato:	article
Lenguaje:	UK
Publicado:	The State Expert Center of the Ministry of Health of Ukraine 2021
Materias:	organic synthesis 3-r-6-(5-arylfuran-2-yl-[1 2 4]triazolo[3 4-b][1 3 4]thiadiazole antitumor activity Therapeutics. Pharmacology RM1-950 Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/f18de5a227b44a108103d684ac4cf43d
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spelling	oai:doaj.org-article:f18de5a227b44a108103d684ac4cf43d2021-11-04T12:10:50ZSynthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles10.32352/0367-3057.5.21.040367-30572617-9628https://doaj.org/article/f18de5a227b44a108103d684ac4cf43d2021-10-01T00:00:00Zhttps://pharmj.org.ua/index.php/journal/article/view/1250/1173https://doaj.org/toc/0367-3057https://doaj.org/toc/2617-9628One of the promising methods of creating antitumor drugs is the screening of potential antitumor agents among synthesized compounds. Nitrogen-based heterocycle analogues are an extremely important class of organic substances that are widely used in medical chemistry. [1,2,4]Triazolo[3,4-b][1,3,4] thiadiazoles are among the little-studied and hard-to-reach members of this class of compounds. The aim of our work was to synthesize some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, as well as the study of their antitumor activity. The objects of study were 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The composition and structure of the synthesized compounds were confirmed by the data of elemental analysis and 1H NMR spectroscopy. The antitumor activity of the synthesized compounds was studied in the framework of the international scientific program of the National Cancer Institute (Bethesda, Maryland, USA) DTP NCI (Developmental Therapeutic Program). The synthesis of 11 derivatives of 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles was carried out. These substances are obtained by the interaction of 5-arylfuran-2-carboxylic acids with 5-substituted 4-amino-4H-1,2,4-triazolo-3-thiols. Primary screening revealed individual 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, which showed pronounced selective antitumor activity. The most active among the tested compounds were 3 d, 3 e and 3 j, which were further investigated during secondary screening. The results of these studies confirm the high antitumor activity of these compounds. The proposed approaches and the developed synthesis protocols made it possible to obtain a series of new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The results of studies of the antitumor activity of the synthesized compounds made it possible to single out 3 highly active compounds with high antitumor activity, which gives reason to consider this condensed system as a promising molecular framework for the design of potential antitumor agents.I. І. MyrkoYu. І. HorakT. I. ChabanІ. V. DrapakV. S. MatiychukThe State Expert Center of the Ministry of Health of Ukrainearticleorganic synthesis3-r-6-(5-arylfuran-2-yl-[124]triazolo[34-b][134]thiadiazoleantitumor activityTherapeutics. PharmacologyRM1-950Pharmacy and materia medicaRS1-441UKФармацевтичний журнал, Vol 5, Pp 37-49 (2021)
institution	DOAJ
collection	DOAJ
language	UK
topic	organic synthesis 3-r-6-(5-arylfuran-2-yl-[1 2 4]triazolo[3 4-b][1 3 4]thiadiazole antitumor activity Therapeutics. Pharmacology RM1-950 Pharmacy and materia medica RS1-441
spellingShingle	organic synthesis 3-r-6-(5-arylfuran-2-yl-[1 2 4]triazolo[3 4-b][1 3 4]thiadiazole antitumor activity Therapeutics. Pharmacology RM1-950 Pharmacy and materia medica RS1-441 I. І. Myrko Yu. І. Horak T. I. Chaban І. V. Drapak V. S. Matiychuk Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
description	One of the promising methods of creating antitumor drugs is the screening of potential antitumor agents among synthesized compounds. Nitrogen-based heterocycle analogues are an extremely important class of organic substances that are widely used in medical chemistry. [1,2,4]Triazolo[3,4-b][1,3,4] thiadiazoles are among the little-studied and hard-to-reach members of this class of compounds. The aim of our work was to synthesize some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, as well as the study of their antitumor activity. The objects of study were 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The composition and structure of the synthesized compounds were confirmed by the data of elemental analysis and 1H NMR spectroscopy. The antitumor activity of the synthesized compounds was studied in the framework of the international scientific program of the National Cancer Institute (Bethesda, Maryland, USA) DTP NCI (Developmental Therapeutic Program). The synthesis of 11 derivatives of 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles was carried out. These substances are obtained by the interaction of 5-arylfuran-2-carboxylic acids with 5-substituted 4-amino-4H-1,2,4-triazolo-3-thiols. Primary screening revealed individual 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, which showed pronounced selective antitumor activity. The most active among the tested compounds were 3 d, 3 e and 3 j, which were further investigated during secondary screening. The results of these studies confirm the high antitumor activity of these compounds. The proposed approaches and the developed synthesis protocols made it possible to obtain a series of new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The results of studies of the antitumor activity of the synthesized compounds made it possible to single out 3 highly active compounds with high antitumor activity, which gives reason to consider this condensed system as a promising molecular framework for the design of potential antitumor agents.
format	article
author	I. І. Myrko Yu. І. Horak T. I. Chaban І. V. Drapak V. S. Matiychuk
author_facet	I. І. Myrko Yu. І. Horak T. I. Chaban І. V. Drapak V. S. Matiychuk
author_sort	I. І. Myrko
title	Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
title_short	Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
title_full	Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
title_fullStr	Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
title_full_unstemmed	Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
title_sort	synthesis and antitumor properties of some new 3-r-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
publisher	The State Expert Center of the Ministry of Health of Ukraine
publishDate	2021
url	https://doaj.org/article/f18de5a227b44a108103d684ac4cf43d
work_keys_str_mv	AT iímyrko synthesisandantitumorpropertiesofsomenew3r65arylfuran2yl124triazolo34b134thiadiazoles AT yuíhorak synthesisandantitumorpropertiesofsomenew3r65arylfuran2yl124triazolo34b134thiadiazoles AT tichaban synthesisandantitumorpropertiesofsomenew3r65arylfuran2yl124triazolo34b134thiadiazoles AT ívdrapak synthesisandantitumorpropertiesofsomenew3r65arylfuran2yl124triazolo34b134thiadiazoles AT vsmatiychuk synthesisandantitumorpropertiesofsomenew3r65arylfuran2yl124triazolo34b134thiadiazoles
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Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles

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