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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

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Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides.

Yogesh Yadav^1,2,3, Deepti Sharma^4,5, Kumar Kaushik⁶

¹Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India. yogeshyadav77@gmail.com.

Molecules (Basel, Switzerland)

|November 2, 2019

Summary

Novel pyrazolylnucleosides were synthesized and tested for anticancer properties. Compound 6e demonstrated significant anticancer activity, particularly against lung and breast cancer cell lines.

Keywords:

NCI-60 NOESY study anticancer modified nucleosides pyrazolylnucleosides

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Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides

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Published on: July 26, 2018

Area of Science:

Medicinal Chemistry
Organic Synthesis
Pharmacology

Background:

Pyrazolylnucleosides represent a class of heterocyclic compounds with potential biological activities.
Developing novel nucleoside analogs is crucial for identifying new anticancer agents.

Purpose of the Study:

To synthesize and characterize novel pyrazolylnucleosides.
To evaluate the in vitro anticancer activity of these synthesized compounds against a panel of human tumor cell lines.

Main Methods:

Synthesis of pyrazolylnucleosides 3a-e, 4a-e, 5a-e, and 6a-e.
Structure elucidation of regioisomers using extensive Nuclear Magnetic Resonance (NMR) studies.
Anticancer screening of compounds 5a-e and 6a-e against sixty human tumor cell lines.

Main Results:

Successful synthesis of a series of novel pyrazolylnucleosides.
Compound 6e exhibited significant anticancer activity, showing efficacy against 39 human tumor cell lines.
Specifically, compound 6e demonstrated potent inhibition against the Hop-92 lung cancer cell line (GI50 9.3 µM) and the HS 578T breast cancer cell line (GI50 3.0 µM).

Conclusions:

The synthesized pyrazolylnucleosides represent a promising scaffold for anticancer drug discovery.
Compound 6e is a potent lead compound with significant activity against lung and breast cancer.
Further investigation into the mechanism of action and in vivo efficacy of compound 6e is warranted.