Microtubule Dynamics and Cancer

Ritter, Andreas; Kreis, Nina-Naomi

doi:10.3390/cancers14184368

Cited by 2 publications

(1 citation statement)

References 11 publications

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“…In this regard, tubulin‐microtubule dynamics have proven to be indispensable target for therapeutic intervention targeting, resulting in a significant breakthrough in the field of breast cancer [4,5] . α and β tubulin heterodimers, which are the building block of microtubules, play a crucial role in the separation of chromosomes during mitosis and have been associated with the regulation of cellular growth and functioning [6,7] . The abnormal activation of tubulin polymerization gives rise to excessive microtubule formation and contributed oncogenesis [8] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Biological Evaluation of New Enamide Fluorinated‐Schiff Base Derivatives as Potential Cytotoxic and Apoptosis‐Inducing Agents

Abd El‐Lateef,

Toson,

Abu Almaaty

et al. 2023

ChemistrySelect

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In search for new anticancer candidates, a new series of enamide fluorinated‐Schiff base derivatives were synthesized and confirmed by spectroscopic techniques as well as elemental microanalyses. The newly prepared compounds were evaluated for their cytotoxic activity on MCF‐7 breast adenocarcinoma cell line. The benzaldehyde Schiff base and furfural Schiff base derivatives (IC50=3.67±0.15 and 2.06±0.08 μM, respectively) were found to be the most potent molecules of all the tested derivatives against the MCF‐7 cancer cells. Additionally, the furfural Schiff base compound was more potent than colchicine by 1.74‐fold, while benzaldehyde Schiff base compound was nearly equipotent with colchicine as standard drug. In addition to tubulin inhibition activity, enamide‐furfural Schiff base molecule caused cell cycle arrest in MCF‐7 cells at the G2/M phase (2.62‐fold more than control MCF‐7) and induced apoptotic death (48.97‐fold compared to untreated MCF‐7 control) as indicated by FACS analysis. Furthermore, apoptotic studies conducted by enamide‐furfural Schiff base derivative were accomplished by downregulation of mitochondrial membrane potential by 1.56‐fold relative to control untreated cells.

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Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Biological Evaluation of New Enamide Fluorinated‐Schiff Base Derivatives as Potential Cytotoxic and Apoptosis‐Inducing Agents

Abd El‐Lateef,

Toson,

Abu Almaaty

et al. 2023

ChemistrySelect

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Design, Synthesis, and Investigation of Cytotoxic Activity of cis-Vinylamide-Linked Combretastatin Analogues as Potential Anticancer Agents

et al. 2022

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The combretastatins (cis-stilbenoid molecules) have received significant interest because of their simple chemical structures, excellent antiproliferative activity, and novel anti-tubulin molecular mechanism of action. Significant efforts have been carried out aiming at stabilizing the active cis-isomers. A new series of cis-vinylamide derivatives containing trimethoxyphenyl moiety were synthesized and characterized. Their anticancer activities were evaluated in vitro against MCF-7 breast cancer cell line. Compounds 2f, 3, and 5 displayed potent cytotoxic activity against the breast cancer cell line compared with CA-4 as the reference compound. The microtubule polymerization assay and flow cytometry analysis confirmed that the cytotoxic activity of compound 3 was related to inhibitory activity against tubulin polymerization. Compound 3 showed pro-apoptotic activity by inducting a significant increase in the percentage of pre-G1 phase in DNA flow cytometry compared to untreated control. The pro-apoptotic activity of compound 3 was inferred by a significant increase in the percentage of fluorescent annexin V/PI positive apoptotic cells. It also increased the level of caspase 3 compared to the untreated control.

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Microtubule Dynamics and Cancer

Abstract: Microtubules (MTs) are highly dynamic key components of the cytoskeleton composed of alpha- and beta-tubulin heterodimers [...]

Cited by 2 publications

References 11 publications

Synthesis, Characterization and Biological Evaluation of New Enamide Fluorinated‐Schiff Base Derivatives as Potential Cytotoxic and Apoptosis‐Inducing Agents

Synthesis, Characterization and Biological Evaluation of New Enamide Fluorinated‐Schiff Base Derivatives as Potential Cytotoxic and Apoptosis‐Inducing Agents

Design, Synthesis, and Investigation of Cytotoxic Activity of cis-Vinylamide-Linked Combretastatin Analogues as Potential Anticancer Agents

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