Synthesis and in vitro biological evaluation of new polyamine conjugates as potential anticancer drugs

Szumilak, Marta; Szulawska-Mroczek, Agata; Koprowska, Kamila; Stasiak, Marta; Lewgowd, Wiesława; Stańczak, Andrzej; Czyż, Małgorzata

doi:10.1016/j.ejmech.2010.09.032

Cited by 61 publications

(49 citation statements)

References 36 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Therefore, we were interested in examining the effect of 6 d and 6 p on cell-cycle progression by FACS analysis. [27] A549 cells were treated with conjugates 6 d or 6 p at 2 mm, along with the reference standard E7010 at 2 mm, and incubated for 48 h. The data obtained shows that these compounds caused greater accumulation of cells in the G 2 /M phase than control.…”

Section: Cell-cycle Analysis and Apoptosismentioning

confidence: 96%

Retracted: Synthesis and Cytotoxic Activity of 2‐Anilinopyridine‐3‐Acrylamides as Tubulin Polymerization Inhibitors

Kamal

Ashraf²,

Khan³

et al. 2014

ChemMedChem

View full text Add to dashboard Cite

The following article Synthesis and Cytotoxic Activity of 2‐Anilinopyridine‐3‐Acrylamides as Tubulin Polymerization Inhibitors, by A. Kamal, Md. Ashraf, M. N. A. Khan, V. D. Nimbarte, S. Faazil, N. V. Subba Reddy, S. Taj, ChemMedChem, DOI: , published online on March 28, 2014 in Wiley Online Library (wileyonlinelibrary.com), has been retracted by agreement between the authors, the journal Editor‐in‐Chief, Natalia Ortúzar, and Wiley‐VCH Verlag GmbH & Co. KGaA. The retraction has been agreed due to concern over the reproducibility of the Western blot results reported in the article.

show abstract

Section: Cell-cycle Analysis and Apoptosismentioning

confidence: 96%

Retracted: Synthesis and Cytotoxic Activity of 2‐Anilinopyridine‐3‐Acrylamides as Tubulin Polymerization Inhibitors

Kamal

Ashraf²,

Khan³

et al. 2014

ChemMedChem

View full text Add to dashboard Cite

show abstract

“…Cell-cycle phase determination was performed by flow cytometry (Becton Dickinson FACS Caliber) as previously described. [55] Two independent experiments were performed in triplicate. Statistical analysis was performed using GraphPad Prism software version 5.01.…”

Section: Cell-cycle Analysismentioning

confidence: 99%

Design and Synthesis of Imidazo[2,1‐b]thiazole–Chalcone Conjugates: Microtubule‐Destabilizing Agents

et al. 2014

View full text Add to dashboard Cite

A series of chalcone conjugates featuring the imidazo[2,1-b]thiazole scaffold was designed, synthesized, and evaluated for their cytotoxic activity against five human cancer cell lines (MCF-7, A549, HeLa, DU-145 and HT-29). These new hybrid molecules have shown promising cytotoxic activity with IC50 values ranging from 0.64 to 30.9 μM. Among them, (E)-3-(6-(4-fluorophenyl)-2,3-bis(4-methoxyphenyl)imidazo[2,1-b]thiazol-5-yl)-1-(pyridin-2-yl)prop-2-en-1-one (11 x) showed potent antiproliferative activity with IC50 values ranging from 0.64 to 1.44 μM in all tested cell lines. To investigate the mechanism of action, the detailed biological aspects of this promising conjugate (11 x) were carried out on the A549 lung cancer cell line. The tubulin polymerization assay and immunofluoresence analysis results suggest that this conjugate effectively inhibits microtubule assembly in A549 cells. Flow cytometric analysis revealed that this conjugate induces cell-cycle arrest in the G2/M phase and leads to apoptotic cell death. This was further confirmed by Hoechst staining, activation of caspase-3, DNA fragmentation analysis, and Annexin V-FITC assay. Moreover, molecular docking studies indicated that this conjugate (11 x) interacts and binds efficiently with the tubulin protein.

show abstract

“…In recent years, a large number of cinnoline compounds were found to own interesting pharmacological properties including anticancer [3], anti-in ammatory and antibacterial [4].…”

Section: Discussionmentioning

confidence: 99%

Crystal structure of 4-(4-((3-bromophenyl)amino)-6-(tert-butyl)-3-(2-hydroxypropan-2-yl)cinnolin-8-yl)-2-methylbut-3-yn-2-ol, C₂₆H₃₀BrN₃O₂

Yuan

Yin

Tian

et al. 2016

Zeitschrift Für Kristallographie - New Crystal Structures

View full text Add to dashboard Cite

show abstract

Synthesis and in vitro biological evaluation of new polyamine conjugates as potential anticancer drugs

Cited by 61 publications

References 36 publications

Retracted: Synthesis and Cytotoxic Activity of 2‐Anilinopyridine‐3‐Acrylamides as Tubulin Polymerization Inhibitors

Retracted: Synthesis and Cytotoxic Activity of 2‐Anilinopyridine‐3‐Acrylamides as Tubulin Polymerization Inhibitors

Design and Synthesis of Imidazo[2,1‐b]thiazole–Chalcone Conjugates: Microtubule‐Destabilizing Agents

Crystal structure of 4-(4-((3-bromophenyl)amino)-6-(tert-butyl)-3-(2-hydroxypropan-2-yl)cinnolin-8-yl)-2-methylbut-3-yn-2-ol, C₂₆H₃₀BrN₃O₂

Contact Info

Product

Resources

About

Synthesis and in vitro biological evaluation of new polyamine conjugates as potential anticancer drugs

Cited by 61 publications

References 36 publications

Retracted: Synthesis and Cytotoxic Activity of 2‐Anilinopyridine‐3‐Acrylamides as Tubulin Polymerization Inhibitors

Retracted: Synthesis and Cytotoxic Activity of 2‐Anilinopyridine‐3‐Acrylamides as Tubulin Polymerization Inhibitors

Design and Synthesis of Imidazo[2,1‐b]thiazole–Chalcone Conjugates: Microtubule‐Destabilizing Agents

Crystal structure of 4-(4-((3-bromophenyl)amino)-6-(tert-butyl)-3-(2-hydroxypropan-2-yl)cinnolin-8-yl)-2-methylbut-3-yn-2-ol, C26H30BrN3O2

Contact Info

Product

Resources

About

Crystal structure of 4-(4-((3-bromophenyl)amino)-6-(tert-butyl)-3-(2-hydroxypropan-2-yl)cinnolin-8-yl)-2-methylbut-3-yn-2-ol, C₂₆H₃₀BrN₃O₂