Search Results - "Khvat, Alexander"

Development and Prospects of Furin Inhibitors for Therapeutic Applications by Ivachtchenko, Alexandre V, Khvat, Alexander V, Shkil, Dmitrii O

“…Furin, a serine protease enzyme located in the Golgi apparatus of animal cells, plays a crucial role in cleaving precursor proteins into their mature, active…”
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Discovery of 2‑[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro‑1H‑isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP‑1 Inhibitor for Cancer Therapy by Papeo, Gianluca, Posteri, Helena, Borghi, Daniela, Busel, Alina A., Caprera, Francesco, Casale, Elena, Ciomei, Marina, Cirla, Alessandra, Corti, Emiliana, D’Anello, Matteo, Fasolini, Marina, Forte, Barbara, Galvani, Arturo, Isacchi, Antonella, Khvat, Alexander, Krasavin, Mikhail Y., Lupi, Rosita, Orsini, Paolo, Perego, Rita, Pesenti, Enrico, Pezzetta, Daniele, Rainoldi, Sonia, Riccardi-Sirtori, Federico, Scolaro, Alessandra, Sola, Francesco, Zuccotto, Fabio, Felder, Eduard R., Donati, Daniele, Montagnoli, Alessia

“…The nuclear protein poly­(ADP-ribose) polymerase-1 (PARP-1) has a well-established role in the signaling and repair of DNA and is a prominent target in…”
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Synthesis and biological evaluation of novel γ-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists by IVACHTCHENKO, Alexandre V, FROLOV, Eugene B, MITKIN, Oleg D, KYSIL, Volodymyr M, KHVAT, Alexander V, OKUN, Ilya M, TLCACHENKO, Sergey E

“…Synthesis, biological evaluation and structure-activity relationships for a series of novel gamma-carboline analogues of Dimebon are described. Among the…”
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A novel synthetic smoothened antagonist transiently inhibits pancreatic adenocarcinoma xenografts in a mouse model by Strand, Martin F, Wilson, Steven R, Dembinski, Jennifer L, Holsworth, Daniel D, Khvat, Alexander, Okun, Ilya, Petersen, Dirk, Krauss, Stefan

“…Hedgehog (Hh) signaling is over-activated in several solid tumors where it plays a central role in cell growth, stroma recruitment and tumor progression. In…”
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A new insight into the Pfitzinger reaction. A facile synthesis of 6-sulfamoylquinoline-4-carboxylic acids by Ivachtchenko, Alexandre V, Khvat, Alexander V, Kobak, Vladimir V, Kysil, Volodymir M, Williams, Caroline T

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Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance by Fang, Sungsoon, Suh, Jae Myoung, Reilly, Shannon M, Yu, Elizabeth, Osborn, Olivia, Lackey, Denise, Yoshihara, Eiji, Perino, Alessia, Jacinto, Sandra, Lukasheva, Yelizaveta, Atkins, Annette R, Khvat, Alexander, Schnabl, Bernd, Yu, Ruth T, Brenner, David A, Coulter, Sally, Liddle, Christopher, Schoonjans, Kristina, Olefsky, Jerrold M, Saltiel, Alan R, Downes, Michael, Evans, Ronald M

“…Restriction of FXR agonism to the gut improves obesity and diabetes. The systemic expression of the bile acid (BA) sensor farnesoid X receptor (FXR) has led to…”
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Multicomponent approach to unique 1,4-diazepine-2-amines by Kysil, Volodymyr, Khvat, Alexander, Tsirulnikov, Sergey, Tkachenko, Sergey, Ivachtchenko, Alexandre

“…Isocyanide-based multicomponent reaction (IMCR) has been developed as an efficient strategy for the 1,4-diazepine-2-amines synthesis. Isocyanide-based…”
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General Multicomponent Strategy for the Synthesis of 2-Amino-1,4-diazaheterocycles: Scope, Limitations, and Utility by Kysil, Volodymyr, Khvat, Alexander, Tsirulnikov, Sergey, Tkachenko, Sergey, Williams, Caroline, Churakova, Marina, Ivachtchenko, Alexandre

“…Multicomponent reactions of primary 1,2‐ and 1,3‐diamines with carbonyl compounds and isocyanides resulting in the formation of diverse…”
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TMSCl-promoted isocyanide-based MCR of ethylenediamines: an efficient assembling of 2-aminopyrazine core by Kysil, Volodymyr, Tkachenko, Sergey, Khvat, Alexander, Williams, Caroline, Tsirulnikov, Sergey, Churakova, Marina, Ivachtchenko, Alexandre

“…New trimethylchlorosilane (TMSCl) promoted multicomponent reaction (MCR) of ethylenediamine(s), diverse carbonyl compounds, and isocyanides is proposed for the…”
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Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1 H -isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy by Papeo, Gianluca, Posteri, Helena, Borghi, Daniela, Busel, Alina A., Caprera, Francesco, Casale, Elena, Ciomei, Marina, Cirla, Alessandra, Corti, Emiliana, D’Anello, Matteo, Fasolini, Marina, Forte, Barbara, Galvani, Arturo, Isacchi, Antonella, Khvat, Alexander, Krasavin, Mikhail Y., Lupi, Rosita, Orsini, Paolo, Perego, Rita, Pesenti, Enrico, Pezzetta, Daniele, Rainoldi, Sonia, Riccardi-Sirtori, Federico, Scolaro, Alessandra, Sola, Francesco, Zuccotto, Fabio, Felder, Eduard R., Donati, Daniele, Montagnoli, Alessia

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Screening for caspase-3 inhibitors: effect of a reducing agent on identified hit chemotypes by Okun, Ilya, Malarchuk, Sergei, Dubrovskaya, Elena, Khvat, Alexander, Tkachenko, Sergey, Kysil, Volodymyr, Kravchenko, Dmitry, Ivachtchenko, Alexandre

“…When studying cysteinyl proteases in general and caspases in particular, it is generally accepted that a reaction buffer must contain a reducing agent to…”
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Synthesis and Biological Evaluation of Novel 5,8-Disubstituted-2-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b] indoles as 5-HT6 and H1 Receptors Antagonists by Ivachtchenko, Alexandre V., Frolov, Eugene B., Mitkin, Oleg D., Kysil, Volodymyr M., Khvat, Alexander V., Tkachenko, Sergey E.

“…Synthesis, biological evaluation, and structure‐activity relationships (SAR) for a series of novel γ‐carboline analogues of Dimebon are described. Among the…”
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5,7-Substituted thiazolo[2,3- a]pyrimidines: Synthesis, stereochemistry and crystal structure by Yaremenko, Fedor, Beryozkina, Tetyana, Khvat, Alexander, Svidlo, Irina, Shishkin, Oleg, Shishkina, Svetlana, Orlov, Valeriy

“…Reaction of 2-aminothiazoline ( 1) with α,β-unsaturated carbonyl compounds 2 under mild conditions (acetone, room temperature) gives two diastereomers…”
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Synthesis and biological evaluation of novel [gamma]-carboline analogues of Dimebon as potent 5-HT[sub]6 receptor antagonists by Ivachtchenko, Alexandre V, Frolov, Eugene B, Mitkin, Oleg D, Kysil, Volodymyr M, Khvat, Alexander V, Okun, Ilya M, Tkachenko, Sergey E

“…Synthesis, biological evaluation and structure-activity relationships for a series of novel [gamma]- carboline analogues of Dimebon[super][TM] are described…”
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Liquid-Phase Parallel Synthesis of Combinatorial Libraries of Substituted 6-Carbamoyl-3,4-dihydro-2H-benzo[1,4]thiazines by Trifilenkov, Andrey S, Kobak, Vladimir V, Salina, Marina A, Kusovkova, Julya A, Ilyin, Alexey P, Khvat, Alexander V, Tkachenko, Sergey E, Ivachtchenko, Alexandre V

“…In this work, we explored several original combinatorial derivatization patterns for the 3,4-dihydro-2H-1,4-benzothiazine scaffold. The synthesis begins with…”
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A Parallel Solution-Phase Synthesis of Substituted 3,7-Diazabicyclo[3.3.1]nonanes by Ivachtchenko, Alexander V, Tkachenko, Sergey E, Sandulenko, Yuriy B, Vvedensky, Vladimir Y, Khvat, Alexander V

“…The parallel solution-phase synthesis of a series of building blocks and combinatorial libraries based on natural bispidine scaffold has been accomplished. Key…”
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Synthesis and biological evaluation of novel γ-carboline analogues of Dimebon as potent 5-HT 6 receptor antagonists by Ivachtchenko, Alexandre V., Frolov, Eugene B., Mitkin, Oleg D., Kysil, Volodymyr M., Khvat, Alexander V., Okun, Ilya M., Tkachenko, Sergey E.

“…Synthesis, biological evaluation and structure–activity relationships for a series of novel γ-carboline analogues of Dimebon ™. Synthesis, biological…”
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Synthesis and Biological Evaluation of Novel 5,8‐Disubstituted‐2‐methyl‐2,3,4,5‐tetrahydro‐1 H ‐pyrido[4,3‐ b ] indoles as 5‐HT 6 and H 1 Receptors Antagonists by Ivachtchenko, Alexandre V., Frolov, Eugene B., Mitkin, Oleg D., Kysil, Volodymyr M., Khvat, Alexander V., Tkachenko, Sergey E.

“…Abstract Synthesis, biological evaluation, and structure‐activity relationships (SAR) for a series of novel γ‐carboline analogues of Dimebon are described…”
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Parallel Liquid-Phase Synthesis of N-Substituted 6-Aminosulfonyl-2-oxo-1,2-dihydroquinoline-4-carboxamide and 6-Aminosulfonylquinoline-4-carboxamide Derivatives by Ivachtchenko, Alexandre V, Kobak, Vladimir V, Ilyn, Alexey P, Khvat, Alexander V, Kysil, Volodymir M, Williams, Caroline T, Kuzovkova, Julia A, Kravchenko, Dmitry V

“…Two efficient strategies for solution-phase parallel synthesis of libraries of quinoline derivatives are described. The first synthetic pathway features the…”
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Microwave-mediated reactions of 3-aminomethylpyridines with acetylenedicarboxylates. A novel synthetic route to dihydronaphthyridines and naphthyridine-1-ones by Vvedensky, Vladimir Y., Ivanov, Yury V., Kysil, Volodymyr, Williams, Caroline, Tkachenko, Sergei, Kiselyov, Alexander, Khvat, Alexander V., Ivachtchenko, Alexandre V.

“…[Display omitted] Reaction of 3-(1-alkylamino)pyridines with electron deficient acetylenes in the presence of acids yields…”
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