Yaroslav V Faletrov

Yaroslav V Faletrov
Belarusian State University | BSU · Research Institute of Physico-Chemical Problems

PhD

About

43
Publications
4,514
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163
Citations

Publications

Publications (43)
Article
The article provides the route to trifluoroacetylated fluorescent boron dipyrromethene dye (2). The compound performs intensive absorption and emission bands in near‐red wavelength region. Photophysical properties of 2 are investigated in different solvents. A notable increase of fluorescence quantum yield after trifluoroacetyl group insertion conn...
Article
4-methyl-7-methoxycoumarin (CumOMe) has been synthesized and in silico calculations demonstrated localization of methoxy group within 0.4 nm from Fe ion of hem groups for some structures of human CYP19 & CYP46 as well as CYP152 S. paucimobilis , CYP158 St. coelicolor , HMUO C. diphtheriae , XPLA R. rhodochrous , CYP199A4 Rh. palustris , CYP101A1 Ps...
Article
A fluorescent molecular rotor (FMR) based on boron dipyrromethene core was obtained. Fluorescence emission properties of the compound strongly depend on the medium viscosity. The emission intensity increases 27 times after viscosity changing from ethanol to glycerol medium. At the same time, the compound appeared almost insensitive to solvatochromi...
Article
In this work we examined the synthesized N-alkynyl-17-aminosteroids and N-alkynyl-20-aminosteroids (based on dehydroepiandrosterone and pregnenolone, respectively) for their effect on C6 rat glioma cell functions. At 10 μM, the compounds had an insignificant effect on C6 glioma mitochondrial membrane potential, but increased cell autophagy by 70-90...
Article
A 3-acetyl analogue of 5-hydroxyindole was synthesised and evaluated for its effects on rat C6 glioma cell functions. It was found that 3-acetyl-5-hydroxy-2-methylindole at 10 μmol/L led to a sharp reduction of mitochondrial membrane potential, induction of autophagy and decrease of proliferation of C6 glioma cells. The compound’s effect was compar...
Preprint
Computer-aided docking-based inverse high-throughput virtual screening (inv HTVS) was applied for a quick evaluation of compounds as new affine ligands for SARS-CoV-2 proteins. We performed Autodock Vina-based inv HTVS using more than 450 structures of the virus proteins from Protein Data Bank (PDB) and totally ~ 2000 structures of compound with el...
Article
An efficient procedure has been developed for the synthesis of 1,4-dihydropyridines containing aliphatic and 2-(1-hydroxycyclopropyl)methyl substituents via multicomponent Hantzsch reaction using europium(III) chloride hexahydrate as catalyst. The synthesized compounds were evaluated for their potential biological activity by simulation of phosphol...
Article
An effective method of synthesis thiazolo[3,2-a]pyrimidine derivatives was developed and the compounds with n-pentyl or β-acetoxycyclopropyl as well as fluorescent benzo[f]coumarin substituents were obtained with yields 60 % and more. Using computational (in silico) approaches we demonstrated the ability of the obtained compounds to permeate lipid...
Article
Full-text available
A hydrophobic derivative of ciprofloxacin, hexanoylated ciprofloxacin (CPF-hex), has been used as a photoinitiator (PI) for two-photon polymerization (2PP) for the first time. We present, here, the synthesis of CPF-hex and its application for 2PP of methacrylate-terminated star-shaped poly (D,L-lactide), as well a systematic study on the optical, p...
Article
Albumin is a globular protein of plasma of mammalian blood participating in transport of hydrophobic metabolites and drugs. Thus, studies devoted to its binding are valuable as a part of evaluation of new potential drugs or fluorescent probes for in vivo usage. Here we describe results concerning synthesis and bovine serum albumin binding assay bot...
Article
In silico analysis of “protein-ligand” complexes of human CYP7 enzymes with modified borondipyrrome-tene (BODIPY) and steroids, containing photo-activated crosslinking groups, wasperformed in order to identify structural peculiarities of their interaction. It was found that BODIPY molecules and DHEA derivative with diazirine group are able to bind...
Article
Four novel indole steroids based on dehydroepiandrosterone (IS-1), estrone (IS-2) and pregnenolone (IS-3) were obtained and studied for their ability to inhibit C6 glioma proliferation. A reduction in cell proliferation by 52±13% was observed for IS-1 at 10 μM, whereas IS-3 and abiraterone acetate at 10 μM caused a 36±8% decrease. Surprisingly, the...
Article
Molecular docking of four hydrazones of isoniazid with steroids (dehydroepiandrosterone, pregnenolone, 16α,17α-epoxypregnenolone, cholestenone) — IDHEA, IPRE, IEP5, ICHN, to mycobacterial cytochromes P450 was performed. The in silico study has shown than these hydrazones can be effectively bound to CYP121, CYP124, CYP125, CYP126A1, CYP130, and CYP5...
Article
20-hydroxycholesterol is a signaling oxysterol with immunomodulating functions and, thus, structural analogues with reporter capabilities could be useful for studying and modulating the cellular processes concerned. We have synthesized three new 20-hydroxycholesterol-like pregn-5-en-3β-ol derivatives with fluorescent 7-nitrobenzofurazan (NBD) or Ra...
Article
Four isomeric dehydroepiandrosterone- and pregnenolone-based N-alkynylaminosteroids were synthesized and tested in vitro for inhibition of heterologously expressed CYP17A1. The highest inhibitory activity was observed when the optimal number of side chain atoms was met. The conjugate based on pregnenolone containing an N-propynyl moiety was found t...
Poster
Full-text available
Two novel 20­hydroxy­pregn­5­en­3β­ols with NBD­label in their side­chains, attached to C20 via ­NH 2 ­CH 2 CH 2 ­ (1) and ­NH 2 ­CH 2 CH 2 CC­ (2) linkers, were synthesized aiming to create fluorescent probes with 20­hydroxycholesterol­like scaffold. We estimated their interactions with whole cells of yeasts Yarrowia lipolytica and Saccharomyces c...
Article
Full-text available
Steroidogenic acute regulatory protein (StAR, STARD1) is a key factor of intracellular cholesterol transfer to mitochondria, necessary for adrenal and gonadal steroidogenesis, and is an archetypal member of the START protein family. Despite the common overall structural fold, START members differ in their binding selectivity toward various lipid li...
Article
Background: The use of antimicrobial agents affecting several biological targets at a time is one of the promising ways to fight multidrug-resistant bacterial strains, and hence it may serve to increase the efficiency of chemotherapy. Among the potential antimicrobial agents acting in this manner are redox-active complexes of transition metals with...
Preprint
Intracellular cholesterol transfer to mitochondria, a bottleneck of adrenal and gonadal steroidogenesis, relies on the functioning of the steroidogenic acute regulatory protein (StAR, STARD1), for which many disease-associated mutations have been described. Despite significant progress in the field, the exact mechanism of cholesterol binding and tr...
Article
Fluorescent steroids BODIPY-cholesterol (BPCh) and 7-nitrobenzoxadiazole-4-amino-(NBD)-labeled 22-NBD-chelesterol (22NC) as well as synthesized 20-(NBD)-pregn-5-en-3β-ol (20NP) were found to undergo bioconversions by Mycobacterium tuberculosis H37Rv and M. smegmatis mc(2) 155. The major fluorescent products were determined to be 4-en-3-one derivati...
Article
Full-text available
Steroidogenic acute regulatory protein (StAR) is responsible for the rapid delivery of cholesterol to mitochondria where the lipid serves as a source for steroid hormones biosynthesis in adrenals and gonads. Despite many successful investigations, current understanding of the mechanism of StAR action is far from being completely clear. StAR was mos...
Conference Paper
Previously we have found that fluorescent N-alkylarylamine Nile Red (NR) is converted by mammalian cytochrome P450 steroid 17a-hydroxylase CYP17A1. Mycobacteria possess various P450s, so we tested of the dye with M. smegmatisandM. tuberculosis. It has been found that fluorescent oxidized derivatives of NR form during long incubations of the dye wit...
Chapter
Novel redox-active metallotherapeutic agents were used to develop effective antimicrobial remedies differing from standard antibiotics in their mechanism of action with participation of free-radical intermediates. For this purpose redox-active compounds carrying sterically hindered 1,2-dihydroxybenzene moieties along with metal ions in a single sca...
Article
Full-text available
Ag(I) complexes formed by polydentate phenolic derivatives of thioglycolic and thiopropionic acids with Ag(I) ions could be a promising field of search for potential chemotherapeutic agents. Convenient synthetic methods to prepare these ligands have been developed on the basis of addition reactions occurring between S-nucleophiles and obenzoquinone...
Article
Fluorescent probes Nile Red (non-steroidal dye) and 25-NBD-cholesterol (a cholesterol analogue) have been evaluated as novel substrates for steroid-converting oxidoreductases. Docking simulations with AutoDock show that Nile Red fits well the substrate-binding site of CYP17A1 (binding energy value = -8.3 kcal/mol). Recombinant yeasts Saccharomyces...
Chapter
Convenient synthetic methods to prepare sulphur-and phosphorus-containing 1,2- dihydroxybenzene derivatives have been developed on the basis of addition reactions occurring between S-nucleophiles or dialkylphosphites and o-benzoquinones. A series of o-aminophenol derivatives has been prepared by reactions of sterically hindered 1,2- dihydroxybenzen...
Article
The synthesis and physico-chemical characterization of Fe(II) and Mn(II) complexes of 2-[4,6-di(tert-butyl)-2,3-dihydroxyphenylsulfanyl]acetic acid (HLI) and 2-[4,6-di(tert-butyl)-2,3-dihydroxyphenylsulfinyl]acetic acid (HLII) were carried out. The investigation of the molecular and electronic structure of Cu(II), Ni(II), Zn(II), Fe(II) and Mn(II)...
Conference Paper
Full-text available
The synthesis and physico-chemical characterization of Fe(II) and Mn(II) complexes of 2-[4,6-di(tert-butyl)-2,3-dihydroxyphenylsulfanyl]acetic acid (HLI) and 2-[4,6-di(tert-butyl)- 2,3-dihydroxyphenylsulfinyl]acetic acid (HLII) were carried out. Antibacterial activity of the Fe(II) and Mn(II) complexes was evaluated in comparison with Cu(II), Co...
Article
The synthesis and physico-chemical characterization of Fe(II) and Mn(II) complexes of 4,6-di-tert-butyl-3[(2-hydroxyethyl)sulphanyl]-1,2-dihydroxybenzene (HL I) and 2-amino-4,6-di-tert-butylphenol (HL II) were carried out. Antibacterial activity of the Co(II), Fe(II) and Mn(II) complexes was evaluated in comparison with Cu(II) complexes and three c...
Article
Full-text available
Abstract (3/4) This review summarizes data about structural and functional organization of steroidogenic P450-dependent enzymatic systems. Problems of catalysis of steroid substrate transformation, special features of mitochondrial type P450scc topogenesis, and abilities of some microbial electron transport proteins to support P450 activity in vitr...
Article
Full-text available
The relationship between 17α-hydroxylation and 20-oxidation-reduction of progesterone and some of its derivatives was studied in yeast strains Saccharomyces cerevisiae YEp51α, Yarrowia lipolytica E129A15, and expressing cytochrome P450c17. The key metabolites were found to be 17α-hydroxyprogester-one and 17α,20(α,β)-dihydroxypregn-4-ene-3-ones. The...
Article
Escherichia coli cells producing the mature form of adrenal cytochrome P450scc were used as a model for study of cytochrome P450scc topogenesis. By disruption of transformed E. coli cells and centrifugation of the homogenate under conventional conditions, we obtained membrane and soluble (high-speed supernatant) fractions both containing the recomb...

Questions

Question (1)
Question
Dear colleagues! I am a biochemist who has faced with a problem of detection of methyl thiol, dimethyl sulfide and also some other volatile sulfur cmpds in air. I have asked to develope a method suitable for GC-MS (electron impact ionization) in stead of GC-SCD (the last seems to allow lower LODs). Studing literature I have found examples of similar tasks' performance, e.g. Talanta 148 (2016) 472–477, Talanta 74 (2008) 562–569.
Could you recomend approaches and devices for concentration of the analytes from air? Also I kindly ask you to help with information about maximal sorbtion capacity of thermodesorber tubes, such as Tenax cartridges. Thank all in advance for attention and advices, which are appreciated in advance.

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