Viktor O. Iaroshenko

Bio: Viktor O. Iaroshenko is an academic researcher from Polish Academy of Sciences. The author has contributed to research in topics: Trifluoromethyl & Chromone. The author has an hindex of 13, co-authored 48 publications receiving 429 citations. Previous affiliations of Viktor O. Iaroshenko include Taras Shevchenko National University of Kyiv & University of Helsinki.

Synthesis of fluorinated purine and 1-deazapurine glycosides as potential inhibitors of adenosine deaminase.

Abstract: The synthesis of 2- and 6-trifluoromethylated purines and 1-deazapurines was performed by formal [3 + 3]-cyclization reactions of 5-aminoimidazoles with a set of trifluoromethyl-substituted 1,3-CCC- and 1,3-CNC-dielectrophiles. The corresponding fluorinated nucleosides were synthesized by glycosylation of 9-unsubstituted purines and 1-deazapurines with peracetylated β-ribose, β-glucose, and rhamnose and subsequent deprotection. These scaffolds can be considered as potential inhibitors of adenosine deaminase (ADA) and inosine monophosphate dehydrogenase (IMPDH) enzymes.

One-pot, three-component synthesis of 7-azaindole derivatives from N-substituted 2-amino-4-cyanopyrroles, various aldehydes, and active methylene compounds.

Abstract: An efficient and practical route to 7-azaindole framework has been developed by one-pot, three-component cyclocondensation of N-substituted 2-amino-4-cyanopyrroles, various aldehydes, and active methylene compounds in ethanol or acetic acid at reflux. Reactions involving tetronic acid, indane-1,3-dione, dimedone, and 5-phenylcyclohexane-1,3-dione gave carbocyclic fused 7-azaindoles, whereas Meldrum’s acid, benzoylacetonitrile, and malononitrile resulted in the highly substituted 7-azaindole derivatives, making this strategy very useful in diversity-oriented synthesis (DOS).

3-Methoxalylchromone—a novel versatile reagent for the regioselective purine isostere synthesis

Abstract: The first synthesis of 3-methoxalylchromone was described. The reaction of the latter with electron-rich aminoheterocycles afforded a set of heteroannelated pyridines bearing a CO2Me substituent located at the α-position of the pyridine core.

Synthesis of Some FluorinatedHeteroannulated Pyrimidines - Purine Isosteres - viaInverse-Electron-Demand Diels-Alder Protocol

Abstract: The inverse-electron-demand Diels―Alder reaction of electron excessive systems such as enamines, electron-enriched amino heterocycles, and anilines with 2,4,6-tris(polyfluoroalkyl)-1,3,5-triazines was investigated. This study results in the synthesis of a set of polyfluoroalkyl containing pyrimidines, heteroannulated pyrimidines, and quinazolines. Following the elaborated synthetic pathway, 1-(β-D-ribofuranosyl)-4,6-bis(polyfluoroalkyl)-1H-pyrazolo[3,4-d]pyrimidines were prepared starting from iso-AIRs.

Reactions of 3-acylchromones with dimethyl 1,3-acetonedicarboxylate and 1,3-diphenylacetone: one-pot synthesis of functionalized 2-hydroxybenzophenones, 6H-benzo[c]chromenes and benzo[c]coumarins.

Abstract: Reactions of 3-methoxalyl-, 3-polyfluoroacyl- and 3-aroylchromones with dimethyl 1,3-acetonedicarboxylate and 1,3-diphenylacetone in the presence of DBU proceed at the C-2 atom of the chromone system with pyrone ring-opening and subsequent formal [3 + 3] cyclocondensation to functionalized 2-hydroxybenzophenones, 6H-benzo[c]chromenes and benzo[c]coumarins, depending on the substituent at the 3-position. An NMR study and X-ray crystallographic analysis are reported. The compounds synthesized can be considered as promising scaffolds for the design of the novel UV-A/B and UV-B filters.

疟原虫var基因转换速率变化导致抗原变异[英]／Paul H, Robert P, Christodoulou Z, et al//Proc Natl Acad Sci U S A

Abstract: 抗原变异可使得多种致病微生物易于逃避宿主免疫应答。表达在感染红细胞表面的恶性疟原虫红细胞表面蛋白1（PfPMP1）与感染红细胞、内皮细胞、树突状细胞以及胎盘的单个或多个受体作用，在黏附及免疫逃避中起关键的作用。每个单倍体基因组var基因家族编码约60种成员，通过启动转录不同的var基因变异体为抗原变异提供了分子基础。

Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances

Abstract: The use of privileged structures in drug discovery has proven to be an effective strategy, allowing the generation of innovative hits/leads and successful optimization processes Chromone is recognized as a privileged structure and a useful template for the design of novel compounds with potential pharmacological interest, particularly in the field of neurodegenerative, inflammatory, and infectious diseases as well as diabetes and cancer This perspective provides the reader with an update of an earlier article entitled “Chromone: A Valid Scaffold in Medicinal Chemistry” (Chem Rev 2014, 114, 4960−4992) and is mainly focused on chromones of biological interest, including those isolated from natural sources Moreover, as drug repurposing is becoming an attractive drug discovery approach, recent repurposing studies of chromone-based drugs are also reported

Tandem inverse-electron-demand hetero-/retro-Diels-Alder reactions for aromatic nitrogen heterocycle synthesis.

Abstract: The merged inverse-electron-demand hetero-Diels–Alder (ihDA)/retro-Diels–Alder (rDA) reaction sequence can be used to rapidly synthesise highly functionalised nitrogen heteroaromatics. The reaction offers many advantages: high atom economy, high levels of regioselectivity, it rarely requires a catalyst and, in some cases, can be performed in the absence of solvent. In this tutorial review we discuss the range of commonly used dienophiles and aza-dienes for this process whilst highlighting the reactivity trends, and illustrating their applications.