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Comparison between conventional, grinding, and microwave synthesis of methylpyrazoles as VEGFR-2/HSP90 dual

Ebtehal M Husseiny¹, Rana M Abdelnaby², Najla Altwaijry³

¹Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Nasr City, Cairo, Egypt.

Future Medicinal Chemistry

|March 31, 2025

Abstract

Aim:

Embracing structure extension and substitution variation, methylpyrazolones 2-6 and dimethylpyrazoles 8-14 were synthesized as VEGFR-2/HSP90 dual inhibitors.

Materials And Methods:

The eco-friendly synthesis of the desired analogs was performed by conventional, grinding, and microwave-assisted methods.

Results:

All entities have been tested for their antitumor action against three carcinomas, whereas compounds 6, 12, and 13 showed significant cytotoxicity and selectivity toward the examined carcinomas. The consecutive molecular mechanistic studies proved that 6 and 12 exhibited dual inhibition of VEGFR-2 and HSP90 and prompted MCF-7 cycle arrest at G2/M phase followed by apoptosis stimulation.

Conclusion:

Molecular docking revealed strong interaction between the potent analogs and VEGFR-2/HSP90 active sites inspiring these congeners to be potential drug candidates in cancer treatment.

Keywords:

Anticancer HSP90 VEGFR-2 methylpyrazole synthesis

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