Verubulin (Azixa) Analogues with Increased Saturation: Synthesis, SAR and Encapsulation in Biocompatible Nanocontainers Based on Ca

apoptosis inducer aromatic nucleophilic substitution cross-linked alginate nanocontainer pyrimidine tetrahydroquinazoline tubulin polymerization inhibitor verubulin

Journal

Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453

Informations de publication

Date de publication:
21 Oct 2023
Historique:
received: 14 09 2023
revised: 09 10 2023
accepted: 19 10 2023
medline: 28 10 2023
pubmed: 28 10 2023
entrez: 28 10 2023
Statut: epublish

Résumé

Tubulin-targeting agents attract undiminished attention as promising compounds for the design of anti-cancer drugs. Verubulin is a potent tubulin polymerization inhibitor, binding to colchicine-binding sites. In the present work, a series of verubulin analogues containing a cyclohexane or cycloheptane ring 1,2-annulated with pyrimidine moiety and various substituents in positions 2 and 4 of pyrimidine were obtained and their cytotoxicity towards cancer and non-cancerous cell lines was estimated. The investigated compounds revealed activity against various cancer cell lines with IC

Identifiants

pubmed: 37895970
pii: ph16101499
doi: 10.3390/ph16101499
pmc: PMC10610134
pii:
doi:

Types de publication

Journal Article

Langues

eng

Subventions

Organisme : Ministry of Science and Higher Education of the Russian Federation
ID : Agreement with Zelinsky Institute of Organic Chemistry RAS No 075-15-2020-803
Organisme : Russian Science Foundation
ID : 22-14-00099
Organisme : RF State Program for IBCP RAS
ID : Project №122041400114-2

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Auteurs

Kseniya N Sedenkova (KN)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Denis N Leschukov (DN)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Yuri K Grishin (YK)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Nikolay A Zefirov (NA)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Yulia A Gracheva (YA)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Dmitry A Skvortsov (DA)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Yanislav S Hrytseniuk (YS)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Lilja A Vasilyeva (LA)

Faculty of Bioengineering and Bioinformatics, Lomonosov Moscow State University, 119991 Moscow, Russia.

Elena A Spirkova (EA)

Institute of Physiologically Active Compounds at Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences (IPAC RAS), 142432 Chernogolovka, Russia.

Pavel N Shevtsov (PN)

Institute of Physiologically Active Compounds at Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences (IPAC RAS), 142432 Chernogolovka, Russia.

Elena F Shevtsova (EF)

Institute of Physiologically Active Compounds at Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences (IPAC RAS), 142432 Chernogolovka, Russia.

Alina R Lukmanova (AR)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Vasily V Spiridonov (VV)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Alina A Markova (AA)

Emanuel Institute of Biochemical Physics, Russian Academy of Sciences, 119334 Moscow, Russia.

Minh T Nguyen (MT)

Emanuel Institute of Biochemical Physics, Russian Academy of Sciences, 119334 Moscow, Russia.

Alexander A Shtil (AA)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.
Institute of Cyber Intelligence Systems, National Research Nuclear University MEPhI, 115409 Moscow, Russia.

Olga N Zefirova (ON)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Alexander A Yaroslavov (AA)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Elena R Milaeva (ER)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Elena B Averina (EB)

Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.

Classifications MeSH