Design, synthesis and biological evaluation of novel 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines as tubulin polymerization inhibitors.

doi:10.1248/cpb.c20-00575

Paper

Design, synthesis and biological evaluation of novel 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines as tubulin polymerization inhibitors.

Published Sep 26, 2020 · Wenjing Liu, Guangcheng Wang, Zhiyun Peng

Chemical & pharmaceutical bulletin

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Abstract

A novel series of 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2- amines were designed, synthesized, and evaluated for their anticancer activities. Most of the synthesized compounds exhibited moderate to high antiproliferative activity in comparison to the standard drug cisplatin. Among them, 5i bearing ethoxy at the 4-position of the phenyl was found to be the most active on MCF-7 and HepG2 cancer cell lines, with IC50 values of 3.77±0.36 μM and 3.83±0.26, respectively. Further mechanism study shown that 5i potently inhibited tubulin polymerization, induced cell cycle arrest at G2/M phase and cell apoptosis in MCF-7 cell line. Furthermore, molecular modeling study suggested that 5i probably binds to the colchicine site of tubulin.

In Vitro Study

Study Snapshot

Novel 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines show moderate to high anticancer activity, with 5i showing the most activity on MCF-7 and HepG2 cancer cell lines, inhibiting tubulin polymerization and causing cell

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Design, synthesis and biological evaluation of novel 4-(4-methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines as tubulin polymerization inhibitors.

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References

Citations

Development of pyrazolo[1,5-a]pyrimidine-grafted coumarins as selective carbonic anhydrase inhibitors and tubulin polymerization inhibitors with potent anticancer activity.

Coumarin-based compounds show potential anticancer activity by inhibiting cancer-related carbonic anhydrase IX and XII and tubulin polymerization.

Design, Synthesis, Molecular Docking, and Biological Evaluation of Pyrazole Hybrid Chalcone Conjugates as Potential Anticancer Agents and Tubulin Polymerization Inhibitors

Pyrazole hybrid Chalcone conjugates show potential as anticancer agents and tubulin polymerization inhibitors, with compound 5o showing excellent cytotoxicity against cancer cell lines.

Aminopyrimidines: Recent synthetic procedures and anticancer activities

Aminopyrimidine derivatives show promising anticancer properties, with recent advances in organic and heterocyclic chemistry guiding their development and use as medicinal agents.