Synthetic cyclopenta[b]indoles exhibit antineoplastic activity by targeting microtubule dynamics in acute myeloid leukemia cells

Vicari, Hugo Passos; Lima, Keli; Gomes, Ralph da Costa; Fernandes, Daniara Cristina; Silva, Jean Carlos Lipreri da; Rodrigues, Manoel T.; Oliveira, Aline Silva Barroso de; Santos, Ricardo Nascimento dos; Andricopulo, Adriano D.; Coelho, Fernando; Costa-Lotufo, Letı́cia V.; Machado-Neto, João Agostinho

doi:10.1016/j.ejphar.2021.173853

Cited by 6 publications

(2 citation statements)

References 48 publications

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“…Microtubules are directly involved in the division process, forming the division spindle and thus, are involved in tumor pathogenesis [41,42]. Reducing the formation of microtubules significantly improves the prognosis in cancer [43,44]. In addition to inhibiting polymerization, a decrease in the content of tubulin monomers can lead to a decrease in microtubule formation.…”

Section: Discussionmentioning

confidence: 99%

Organization of the Cytoskeleton in Ectopic Foci of the Endometrium with Rare Localization

Toniyan

Povorova²,

Gorbacheva³

et al. 2021

Biomedicines

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(1) Background: Endometriosis is a common pathology of the female reproductive system, often accompanied by pain and decreased fertility. However, its pathogenesis has not been sufficiently studied regarding the role of the cytoskeleton. In this study, we describe two clinical cases involving rare localization of extragenital endometriosis (umbilicus) and compare them with genital endometriosis of different localization (ovaries and uterus), as well as eutopic endometrium obtained with separate diagnostic curettage without confirmed pathology. (2) Methods: The relative content of actin and tubulin cytoskeleton proteins was determined by Western blotting, and the expression of genes encoding these proteins was determined by RT-PCR in the obtained intraoperative biopsies. The content of 5hmC was estimated by dot blot experiments, and the methylase/demethylase and acetylase/deacetylase contents were determined. (3) Results: The obtained results indicate that the content of the actin-binding protein alpha-actinin1 significantly increased (p < 0.05) in the groups with endometriosis, and this increase was most pronounced in patients with umbilical endometriosis. In addition, both the mRNA content of the ACTN1 gene and 5hmC content increased. It can be assumed that the increase in 5hmC is associated with a decrease in the TET3 demethylase content. Moreover, in the groups with extragenital endometriosis, alpha- and beta-tubulin content was decreased (p < 0.05) compared to the control levels. (4) Conclusions: In analyzing the results, further distance of ectopic endometrial foci from the eutopic localization may be associated with an increase in the content of alpha-actinin1, probably due to an increase in the expression of its gene and an increase in migration potential. In this case, a favorable prognosis can be explained by a decrease in tubulin content and, consequently, a decrease in the rate of cell division.

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Section: Discussionmentioning

confidence: 99%

Organization of the Cytoskeleton in Ectopic Foci of the Endometrium with Rare Localization

Toniyan

Povorova²,

Gorbacheva³

et al. 2021

Biomedicines

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“…To investigate the cytotoxic activity of the indanone derivatives, in total 20 compounds were tested at a concentration of 5 and 50 μg/mL for 72 h in a panel of four histologically unrelated tumor lines, HCT116 (colon adenocarcinoma), MCF7 (breast adenocarcinoma), SK-MEL-28 (melanoma), and NB4 (acute leukemia) by methylthiazol tetrazolium (MTT) assay, as previously described [ 85 ]. Among the tested cells, NB4 cells were the most sensitive ones, with 7 compounds ( 10aa , bk and 11aa , ad , ae , dc , bj ) being active at 5 μg/mL, using a 75% cutoff inhibition at each concentration.…”

Section: Resultsmentioning

confidence: 99%

Bismuth(III) triflate: an economical and environmentally friendly catalyst for the Nazarov reaction

Rodrigues Jr.,

de Oliveira,

Gomes

et al. 2024

Beilstein J. Org. Chem.

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We describe the use of bismuth(III) triflate as an efficient and environmentally friendly catalyst for the Nazarov reaction of aryl vinyl ketones, leading to the synthesis of 3-aryl-2-ethoxycarbonyl-1-indanones and 3-aryl-1-indanones. By changing the temperature and reaction time, it was possible to modulate the reactivity, allowing the synthesis of two distinct product classes (3-aryl-2-ethoxycarbonyl-1-indanones and 3-aryl-1-indanones) in good to excellent yield. The reaction did not require additives and was insensitive to both air and moisture. Preliminary biological evaluation of some indanones showed a promising profile against some human cancer line cells.

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STMN1 is highly expressed and contributes to clonogenicity in acute promyelocytic leukemia cells

et al. 2021

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Synthetic cyclopenta[b]indoles exhibit antineoplastic activity by targeting microtubule dynamics in acute myeloid leukemia cells

Cited by 6 publications

References 48 publications

Organization of the Cytoskeleton in Ectopic Foci of the Endometrium with Rare Localization

Organization of the Cytoskeleton in Ectopic Foci of the Endometrium with Rare Localization

Bismuth(III) triflate: an economical and environmentally friendly catalyst for the Nazarov reaction

STMN1 is highly expressed and contributes to clonogenicity in acute promyelocytic leukemia cells

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