Convenient One‐Pot Synthesis and Biological Evaluation of New 3,5‐Dimethyl‐1H‐pyrazole‐1‐carbothiohydrazide Derivatives as Anti‐Tumor Agents

Author:

Fouad Marwa M.1ORCID,Elaasser Mahmoud M.2

Affiliation:

1. Basic Science Department Modern Academy for Engineering & Technology 11439 Cairo Egypt

2. The Regional Center for Mycology and Biotechnology Al-Azhar University 11371 Cairo Egypt

Abstract

AbstractPyrazole compounds have garnered attention due to their potential biological and medicinal qualities. Therefore, the purpose of the research being described is to utilize 3,5‐dimethyl‐1H‐pyrazole‐1‐carbothiohydrazide (1) as a starting material in a one‐pot synthesis to create novel pyrazole derivatives with potential biological applications. When either ethanol or acetic acid was added, components 1 and 1,3‐diphenylpropane‐1,3‐dione (2) reacted to produce derivative 3. Compound 1, when combined with ethanol, chemical 2, or acetyl acetone 5 and triethylamine, yielded chemicals 4 and 6 respectively. When ingredient 1 was mixed with ethyl cyanoacetate (7), stearic acid (10), or carboxylic acids 12 ac, 9, 11, and 13 ac were formed as a result. The equivalent 1,3,4‐thiadiazine derivatives, 15 and 17, were produced when 1 was mixed with either 14 or 16. The developed compounds′ cytotoxic properties were evaluated against lung and liver cancer. Our research identified a number of interesting bioactive chemicals, among which chemical 17 exhibited the greatest effectiveness against lung and liver cancer as well as the highest selectivity index measurements. It indicated a strong IC50 value of 5.35 and 8.74 μM, accordingly, when compared with 3.78 and 6.39 μM for the reference medication cisplatin. Additionally, its safety for use has been confirmed.

Publisher

Wiley

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