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Identification of Spiro-Fused Pyrrolo[3,4-a]pyrrolizines and Tryptanthrines as Potential Antitumor Agents: Synthesis and In Vitro Evaluation.
Latypova, Diana K; Shmakov, Stanislav V; Pechkovskaya, Sofya A; Filatov, Alexander S; Stepakov, Alexander V; Knyazev, Nickolay A; Boitsov, Vitali M.
Afiliação
  • Latypova DK; Saint-Petersburg National Research Academic University of the Russian Academy of Sciences, 194021 Saint-Petersburg, Russia.
  • Shmakov SV; Saint-Petersburg National Research Academic University of the Russian Academy of Sciences, 194021 Saint-Petersburg, Russia.
  • Pechkovskaya SA; Institute of Cytology, Russian Academy of Sciences, 194064 Saint-Petersburg, Russia.
  • Filatov AS; Department of Chemistry, Saint-Petersburg State University, 199034 Saint Petersburg, Russia.
  • Stepakov AV; Department of Chemistry, Saint-Petersburg State University, 199034 Saint Petersburg, Russia.
  • Knyazev NA; Department of Organic Chemistry, Saint Petersburg State Institute of Technology, 190013 Saint-Petersburg, Russia.
  • Boitsov VM; Institute of Cytology, Russian Academy of Sciences, 194064 Saint-Petersburg, Russia.
Int J Mol Sci ; 22(21)2021 Nov 05.
Article em En | MEDLINE | ID: mdl-34769424
A series of heterocyclic compounds containing a spiro-fused pyrrolo[3,4-a]pyrrolizine and tryptanthrin framework have been synthesized and studied as potential antitumor agents. Cytotoxicity of products was screened against human erythroleukemia (K562) and human cervical carcinoma (HeLa) cell lines. Among the screened compounds. 4a, 4b and 5a were active against human erythroleukemia (K562) cell line, while 4a and 5a were active against cervical carcinoma (HeLa) cell line. In agreement with the DNA cytometry studies, the tested compounds have achieved significant cell-cycle perturbation with higher accumulation of cells in G2/M phase and induced apoptosis. Using confocal microscopy, we found that with 4a and 5a treatment of HeLa cells, actin filaments disappeared, and granular actin was distributed diffusely in the cytoplasm in 76-91% of cells. We discovered that HeLa cells after treatment with compounds 4a and 5a significantly reduced the number of cells with filopodium-like membrane protrusions (from 63 % in control cells to 29% after treatment) and a decrease in cell motility.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirrolidinas / Quinazolinas / Compostos de Espiro / Leucemia Eritroblástica Aguda / Neoplasias do Colo do Útero / Antineoplásicos Tipo de estudo: Diagnostic_studies / Evaluation_studies Limite: Female / Humans Idioma: En Revista: Int J Mol Sci Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Federação Russa

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirrolidinas / Quinazolinas / Compostos de Espiro / Leucemia Eritroblástica Aguda / Neoplasias do Colo do Útero / Antineoplásicos Tipo de estudo: Diagnostic_studies / Evaluation_studies Limite: Female / Humans Idioma: En Revista: Int J Mol Sci Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Federação Russa