Objective: Pyrazolopyrimidines are heterocyclic molecules containing nitrogen as the main composition, and hence, they exhibit pharmacological efficacy. They are analogs of purines so that possessing wide applications in the field of medicinal chemistry. The main objective of this study is to synthesize different derivatives of pyrazole-pyrimidine classes by adopting simple methodology as well as by employing green chemistry. The purpose of the synthesis of these molecules is to study the antitumor activity against Ehrlich ascites carcinoma (EAC) cell lines.
Methods: After literature studies, it makes us to involve in the research of synthetic organic chemistry, especially to synthesize new compounds of pyrazolopyrimidines. We are reported solvent-free synthesis of pyrazolo [3,4-d]-pyrimidine-thiones through ethyl acetoacetate, hydrazine hydrate, thiourea, and different benzaldehydes. An ionic liquid 2-methyl-imidazolium-oxalate catalyzed the reactions under ultrasonication bath. Both conventional and ultrasonic methods were employed and comparison studies have been made. It was found that ultrasonic method completed the reaction quicker than the conventional method. All the synthesized compounds were confirmed their structures by 1HNMR, Fourier transform infrared, 13C-NMR, and elemental analysis spectra. The compounds were tested for in vitro anticancer activity against EAC cell lines. Most compounds revealed significant anticancer activity relative to doxorubicin as a positive control with inhibitory concentration (IC50) values.
Results: Ultrasonication method is a simple method under which all the reactions were completed at faster time (<7 min) compared to the convention method. Among eight molecules, 8a and 8d completed the reactions at a faster rate. We reported IC50 values of all the molecules, in which 8e and 8g were exhibited excellent potency against EAC cell lines at different concentrations .
Conclusions: Ultrasonication method is an excellent method for the organic synthesis. We are herein reported that under this method, all the reactions are completed within 7 min. Hence, it is superior method than the conventional method. All synthesized molecules have shown good inhibitor potency against EAC cell lines. Among them, two molecules 8e and 8g have shown excellent inhibitor potency.
Pyrazolo-Pyrimidines are Heterocycles having nitrogen based hetero atom which is the main composition to exhibit pharmacological efficacy. Since they resemble purine, have a great role in the field of medicinal chemistry. After thorough literature survey, we planned to synthesize the new compounds of Pyrazolo-Pyrimidines by different synthetic methodology followed the green chemistry approach. We are herein reported that one pot solvent-free syntheses of Pyrazolo-Pyrimidines met green chemistry via Ethyl acetoacetate, Hydrazine. hydrate, thiourea & different benzaldehydes by using Ionic liquid 2-methyl-imidazolium-Oxalate under Ultrasonicator. Both Conventional and Ultrasonic methods were employed & Comparisonal studies have been done. It was found that Ultrasonic method completed the reaction quicker than the Conventional method. The Ionic liquid 2-methyl-imidazolium-Oxalate is proved to be a good catalyst for the organic syntheses by attaining good yield. All the synthesized compounds were confirmed by 1 HNMR, IR & 13 C-NMR spectra. The compounds were tested for in-vitro anticancer activity against Ehrlich Ascites Carcinoma (EAC) cell line. Most compounds revealed significant anticancer activity relative to doxorubicin as positive control with IC50 values.
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