In the present work, we presented an efficient synthesis and anticancer activity evaluation of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. We have shown that the proposed synthetic protocols provided the possibility to design triazolothiadiazoles diversity with a considerable chemical novelty. The structures of target substances were confirmed by using 1H NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds were selected by the National Cancer Institute Developmental Therapeutic Program for the in vitro cell line screening. Among all the substances tested, three compounds exhibited significant cytotoxic activity.

The synthesis, anticancer and antimicrobial properties of novel N-aryl-2-(5-aryltetrazol-2-yl)acetamides were discussed. Novel N-aryl-2H-tetrazoles were synthesized and modified in order to obtain the compounds with a satisfactory pharmacological profile. The structures of target substances were confirmed by using 1 H spectroscopy, mass spectrometry and elemental analysis. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA).
The compounds with significant levels of anticancer activities have been found that can be used for further optimization. The antimicrobial activity of the synthesized substances was evaluated by the value of the MIC and minimum fungicidal and bactericidal concentration. The findings exhibited that the compounds possessed moderate antimicrobial potential

By the reaction of (4-furan-2-yl-thiazol-2-yl)- 3a and (4-thiophen-2-yl-thiazol-2-yl)- 3b acetonitriles with furfural 4 and 5-arylfurfyrals 5a-g 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives 6a-i were obtained. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was found out that (2E)-3-(2-furyl)-2-[4-(2-furyl)-1,3-thiazol-2-yl]acrylonitrile (6a) and 2-(4-thiophen-2-yl-thiazol-2-yl)-acrylonitriles 6h,i possessed low activity and 2-(4-furan-2-yl-thiazol-2-yl)acrylonitrile derivatives 6b-g showed moderate action. Compounds 6b-g were sensitive to cell lines of MDA-MB-468 and T-47D Breast Cancer. In this case cytotoxic effect was observed with a range of GP = -38.24 –1.28%.

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

The 18 new thiazolo[4,5-b]pyridin-2-one derivatives have been synthesized using alkylation, cyanethylation, hydrolysis, and acylation reactions. The structures of the obtained compounds have been confirmed by 1H NMR spectroscopy, mass spectrometry, and elemental analysis. The study of the in vivo anti-inflammatory activity of the synthesized substances was assessed by using the functional model of carrageenan-induced rat paw edema. The present results of anti-inflammatory activity have shown that the synthesized compounds demonstrated considerable anti-inflammatory effects. Some of them approach or exceed the comparative drug Ibuprofen in terms of activity.