Novel anthraquinone-based derivatives as potent inhibitors for receptor tyrosine kinases

Stasevych, Maryna; Zvarych, Viktor; Лунин, В.В.; Halenova, Tetiana; Savchuk, Olexiy; Dudchak, O; Vovk, M. V.; Novikov, Volodymyr

doi:10.4103/0250-474x.169062

Cited by 14 publications

(10 citation statements)

References 12 publications

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“…The kinase assay was performed according to published procedures [18]. The reaction was carried out in 96-well plates precoated with polyGlu/Tyr substrate (Sigma, USA; product No.…”

Section: Analysis Of Tyrosine Protein Kinase (Tpkase) Activitymentioning

confidence: 99%

Hypoglycemic activity of Phaseolus vulgaris (L.) aqueous extract in type 1 diabetic rats

Halenova

Raksha

Kravchenko

et al. 2019

Current Issues in Pharmacy and Medical Sciences

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The aim of the present study was to evaluate the hypoglycemic activity of the aqueous extract from the fruit walls of Phaseolus vulgaris pods and to examine the potential mechanism underlying the improvement of the glycemic level. In the course of the study, diabetes mellitus was induced in rats with a single intraperitoneal injection of streptozotocin (45 mg·kg−1 b.w.). Diabetic and control rats were then orally administered with a single-dose or repeated-dose (28 day) of P. vulgaris extract (200 mg·kg−1). Results show that the extract was found to possess significant hypoglycemic activity, and the study of glucose utilization by isolated rat hemidiaphragm suggests that the aqueous extract may enhance the peripheral utilization of glucose. The subsequent experiments have revealed that the P. vulgaris extract could increase glucose transporter 4 (GLUT-4) content in skeletal muscle cells of control and diabetic rats. Our data also indicate that the P. vulgaris extract did not affect the content of the insulin receptor, but significantly reduced the total tyrosine kinase activity in skeletal muscle cells of both experimental groups of rats. The present results clearly indicated that P. vulgaris extract may be beneficial for reducing hyperglycemia through its potency in regulation of glucose utilization via GLUT-4, but the current mechanism remains to be unidentified.

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“…The kinase assay was performed according to published procedures [18]. The reaction was carried out in 96-well plates precoated with polyGlu/Tyr substrate (Sigma, USA; product No.…”

Section: Analysis Of Tyrosine Protein Kinase (Tpkase) Activitymentioning

confidence: 99%

Hypoglycemic activity of Phaseolus vulgaris (L.) aqueous extract in type 1 diabetic rats

Halenova

Raksha

Kravchenko

et al. 2019

Current Issues in Pharmacy and Medical Sciences

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“…Derivatives of the 9,10-anthraquinone of both natural and synthetic origin are well known for their wide range of biological effects. Of particular interest, compounds with an antibacterial effect are known among them [14][15][16][17]. The 1,2,3-triazinone ring is an important biophore fragment for the creation of new promising antimicrobial agents based on the 9,10-anthraquinone platform.…”

Section: Introductionmentioning

confidence: 99%

Anthra[1,2-d][1,2,3]triazine-4,7,12(3H)-triones as a New Class of Antistaphylococcal Agents: Synthesis and Biological Evaluation

et al. 2019

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The development and spread of resistance of human pathogenic bacteria to the action of commonly used antibacterial drugs is one of the key problems in modern medicine. One of the especially dangerous and easily developing antibiotic resistant bacterial species is Staphylococcus aureus. Anthra[1,2-d][1,2,3]triazine-4,7,12(3H)-triones 22–38 have been developed as novel effective antistaphylococcal agents. These compounds have been obtained by sequential conversion of 1-amino-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid (1) and 1-amino-4-bromo-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid (2) into the corresponding amides 5–21, followed by subsequent endo-cyclization under the influence of sodium nitrite in acetic acid. Evaluation of the antimicrobial activity of the synthesized compounds against selected species of Gram-positive and Gram-negative bacteria as well as pathogenic yeasts of the Candida genus has been carried out by the serial dilution method. It has been established that anthra[1,2-d][1,2,3]triazine-4,7,12(3H)-triones exhibit selective antibacterial activity against Gram-positive bacteria. Eight, six and seven, out of seventeen compounds tested, effectively inhibited the growth of S. aureus ATCC 25923, S. aureus ATCC 29213 and S. epidermidis ATCC12228, respectively, at a concentration equal to 1 µg/mL or lower. The high antistaphylococcal potential of the most active compounds has been also confirmed against clinical isolates of S. aureus, including the MRSA strains. However, bacteria of the Staphylococcus genus have demonstrated apparent resistance to the novel compounds when grown as a biofilm. None of the four selected compounds 3234 and 36 at a concentration of 64 µg/mL (128 or 256 × MIC—against planktonic cells) has caused any decrease in the metabolic activity of the staphylococcal cells forming the biofilm. The kinetic time–kill assay revealed some important differences in the activity of these substances. Compound 33 is bacteriostatic, while the other three demonstrate bactericidal activity.

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“…Since 1,2,3-triazole systems based on the 9,10-anthracenediones have not been known in the literature, the construction of new structures with 9,10-anthracenedione and 1,2,3-triazole moieties is very promising from the standpoint of expanding a series of previously investigated derivatives of 9,10-anthracenedione [8][9][10][11][12].…”

Section: Introductionmentioning

confidence: 99%

“…The structure of triazoles 3-12, 15-17 was confirmed by Approach in silico has been used to continue preliminary results of correlation "structure-prediction computer-experimental studies" [8,12] and to identify the most promising directions of experimental studies of new functionalized 1(2)amino-9,10-anthracendiones with triazole fragment. It included a prediction of possible pharmacological activity by the program PASS Online [21] and determination of mechanisms for possible implementation of biological activity using a software package Schrödinger Suite 2014 [22].…”

mentioning

confidence: 99%

The New 1,2,3-Triazolylantracene-9,10-Diones: Synthesis and ComputerBioactivity Screening

Stasevych¹,

Zvarych²,

Лунин³

et al. 2017

ChChT

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Abstract. 1 The reactions of 1,4(1,5)-diazido-9,10-anthracenediones with phenylacetylene and methyl propiolate under copper(I)-catalyzed reaction of the azidealkyne cycloaddition conditions have been studied and a series of new 1,2,3-triazole derivatives of 9,10-anthracendione have been obtained. The computer screening of synthesized compounds was carried out using the PASS Online software to identify areas of experimental biomedical researches. Compounds with high affinity to the receptors family of tyrosine kinases of the epidermal growth factor EGFR have been found among the newly synthesized 1,2,3-triazoles of 9,10-anthracenedione using molecular docking. The results of molecular docking indicate a probable mechanism for the realization of antitumor activity.

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Novel anthraquinone-based derivatives as potent inhibitors for receptor tyrosine kinases

Cited by 14 publications

References 12 publications

Hypoglycemic activity of Phaseolus vulgaris (L.) aqueous extract in type 1 diabetic rats

Hypoglycemic activity of Phaseolus vulgaris (L.) aqueous extract in type 1 diabetic rats

Anthra[1,2-d][1,2,3]triazine-4,7,12(3H)-triones as a New Class of Antistaphylococcal Agents: Synthesis and Biological Evaluation

The New 1,2,3-Triazolylantracene-9,10-Diones: Synthesis and ComputerBioactivity Screening

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