Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents.

doi:10.1016/j.bmcl.2018.12.050

Paper

Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents.

Published Mar 1, 2019 · S. Sengmany, Mathilde Sitter, Eric Léonel

Bioorganic & medicinal chemistry letters

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Abstract

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In Vitro Study

Study Snapshot

3-amino-, 3-alkoxy-, and 3-aryloxy-6-(hetero)arylpyridazines show potent antitumor activity against various cancer cell lines and inhibit oncogenicity in human breast cancer cell line MDA-MB 468-Luc.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents.

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References

MEK and PI3K catalytic activity as predictor of the response to molecularly targeted agents in triple-negative breast cancer.

MEK and PI3K catalytic activity may predict the response of triple-negative breast cancer to targeted agents trametinib and wortmannin.

Design and Synthesis of Pyridazine Containing Compounds with Promising Anticancer Activity.

Pyridazine-containing compounds show promising anticancer activity, with compound 5b showing the highest inhibition of VEGFR kinase (92.2%) in vitro.

Pyridazine Based Scaffolds as Privileged Structures in anti-Cancer Therapy

Pyridazine-based scaffolds show potential in anti-cancer therapy, particularly for targeting protein kinase inhibition, due to their diverse properties, improved ADME, and toxicity profile.

Synthesis and cytotoxic activities of some pyrazoline derivatives bearing phenyl pyridazine core as new apoptosis inducers.

Compound 8k shows promising antiproliferative activities against cancer cell lines, inducing apoptosis through caspase-3 activation.

Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.

Increasing the polarity of pyridazines can improve selectivity over related GPCRs, hERG inhibition, and phospholipidosis in MCH-R1 antagonists for obesity treatment.

Citations

Cross-Electrophile Coupling: Principles, Methods, and Applications in Synthesis

Cross-electrophile coupling (XEC) is a rapidly developing synthetic approach, with potential applications in various chemical reactions, but optimal catalysts, ligands, additives, and reductants remain in flux.

Preparation of Some New Pyrazine and Triazine Derivatives and Study of their Antimicrobial and Anticancer activities

New 1,2,4-triazine and 1,2-diazine derivatives show promising antimicrobial and anticancer activities against prostate cancer PC3.

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

Synthetic compounds with promising anti-breast cancer activity are being developed, offering a promising alternative to current treatments and addressing multidrug resistance and side effects.

Discovery of 3,6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico insights

3,6-disubstituted pyridazines show promising anticancer activity by targeting CDK2, with potential for further development into efficient and safe CDK inhibitors.