Hydrazones of poorly studied fluorine-containing oxamic acid thiohydrazides were synthesized by t... more Hydrazones of poorly studied fluorine-containing oxamic acid thiohydrazides were synthesized by the reaction with salicylaldehydes. Tests showed that the newly synthesized compounds were effective low-toxic inhibitors of type III secretion system in Chlamydia trachomatis.
The monograph describes monothiooxamides and thiohydrazides of oxamic acids, methods of their syn... more The monograph describes monothiooxamides and thiohydrazides of oxamic acids, methods of their synthesis, chemical properties and physico-chemical methods for studying their structure; describes heterocyclic, steroid-heterocyclic, amino acid and peptide derivatives, metal complexes and supramolecular complexes obtained on the basis of monothiooxamides and thiohydrazides of oxamic acids, as well as their structural studies. The range of issues covered includes diverse topics related to those areas of organic chemistry, organic synthesis, structural chemistry, bioorganic and medical chemistry, as well as technical applications that have received their fruitful development on the basis of these classes of compounds. For specialists in the field of organic chemistry, organic synthesis, analytical, bioorganic and medical chemistry.
Related Article: Ksenia A. Myannik, Vladimir N. Yarovenko, Elena K. Beloglazkina, Anna A. Moiseev... more Related Article: Ksenia A. Myannik, Vladimir N. Yarovenko, Elena K. Beloglazkina, Anna A. Moiseeva, Mikhail M. Krayushkin|2018|Polyhedron|139|208|doi:10.1016/j.poly.2017.10.027
The reaction of amidoximes with cyanoguanidine in the presence of Lewis acids affords 3-substitut... more The reaction of amidoximes with cyanoguanidine in the presence of Lewis acids affords 3-substituted 5-guanidino-1,2,4-oxadiazoles. A study of the reaction of15N-labeled chloroacetamidoxime with cyanoguanidine showed that the formation of the oxadiazole ring occursvia the elimination of the amino group from the amidoxime fragment. 1,2,4-Oxadiazoles bearing the imidazole or pyrimidine moiety were synthesized.
Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform that is overexpressed in sev... more Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform that is overexpressed in several cancers and has been implicated in drug resistance. Currently, no small-molecule drug targeting GSTO1 is under clinical development. Here we show that silencing of GSTO1 with siRNA significantly impairs cancer cell viability, validating GSTO1 as a potential new target in oncology. We report on the development and characterization of a series of chloroacetamide-containing potent GSTO1 inhibitors. Co-crystal structures of GSTO1 with our inhibitors demonstrate covalent binding to the active site cysteine. These potent GSTO1 inhibitors suppress cancer cell growth, enhance the cytotoxic effects of cisplatin and inhibit tumour growth in colon cancer models as single agent. Bru-seq-based transcription profiling unravelled novel roles for GSTO1 in cholesterol metabolism, oxidative and endoplasmic stress responses, cytoskeleton and cell migration. Our findings demonstrate the therapeutic uti...
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance t... more ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Hydrazones of poorly studied fluorine-containing oxamic acid thiohydrazides were synthesized by t... more Hydrazones of poorly studied fluorine-containing oxamic acid thiohydrazides were synthesized by the reaction with salicylaldehydes. Tests showed that the newly synthesized compounds were effective low-toxic inhibitors of type III secretion system in Chlamydia trachomatis.
The monograph describes monothiooxamides and thiohydrazides of oxamic acids, methods of their syn... more The monograph describes monothiooxamides and thiohydrazides of oxamic acids, methods of their synthesis, chemical properties and physico-chemical methods for studying their structure; describes heterocyclic, steroid-heterocyclic, amino acid and peptide derivatives, metal complexes and supramolecular complexes obtained on the basis of monothiooxamides and thiohydrazides of oxamic acids, as well as their structural studies. The range of issues covered includes diverse topics related to those areas of organic chemistry, organic synthesis, structural chemistry, bioorganic and medical chemistry, as well as technical applications that have received their fruitful development on the basis of these classes of compounds. For specialists in the field of organic chemistry, organic synthesis, analytical, bioorganic and medical chemistry.
Related Article: Ksenia A. Myannik, Vladimir N. Yarovenko, Elena K. Beloglazkina, Anna A. Moiseev... more Related Article: Ksenia A. Myannik, Vladimir N. Yarovenko, Elena K. Beloglazkina, Anna A. Moiseeva, Mikhail M. Krayushkin|2018|Polyhedron|139|208|doi:10.1016/j.poly.2017.10.027
The reaction of amidoximes with cyanoguanidine in the presence of Lewis acids affords 3-substitut... more The reaction of amidoximes with cyanoguanidine in the presence of Lewis acids affords 3-substituted 5-guanidino-1,2,4-oxadiazoles. A study of the reaction of15N-labeled chloroacetamidoxime with cyanoguanidine showed that the formation of the oxadiazole ring occursvia the elimination of the amino group from the amidoxime fragment. 1,2,4-Oxadiazoles bearing the imidazole or pyrimidine moiety were synthesized.
Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform that is overexpressed in sev... more Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform that is overexpressed in several cancers and has been implicated in drug resistance. Currently, no small-molecule drug targeting GSTO1 is under clinical development. Here we show that silencing of GSTO1 with siRNA significantly impairs cancer cell viability, validating GSTO1 as a potential new target in oncology. We report on the development and characterization of a series of chloroacetamide-containing potent GSTO1 inhibitors. Co-crystal structures of GSTO1 with our inhibitors demonstrate covalent binding to the active site cysteine. These potent GSTO1 inhibitors suppress cancer cell growth, enhance the cytotoxic effects of cisplatin and inhibit tumour growth in colon cancer models as single agent. Bru-seq-based transcription profiling unravelled novel roles for GSTO1 in cholesterol metabolism, oxidative and endoplasmic stress responses, cytoskeleton and cell migration. Our findings demonstrate the therapeutic uti...
ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance t... more ABSTRACT ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
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