Design, Synthesis and Biological Evaluation of Novel Diaryl Pyrazole Derivatives as Anticancer Agents

Abstract

Cancer is one of the major causes of mortality all around the world. Globally, nearly 1 in 6 deaths is due to cancer. Researchers are trying to synthesize new anticancer agents. Previous studies demonstrated that some pyrazole derivatives could be considered as potential anticancer agents. Herein, ten novel derivatives of 1,5-diarylpyrazole were synthesized in four step reactions and cytotoxic activity was investigated by MTT cell viability assay. All of the compounds were characterized by 1H NMR and 13C NMR and their purity was confirmed by elemental analysis. The cytotoxicity was determined against three cancerous cell lines (HT-29, U87MG and MDA-MB 468) and AGO1522 as a normal cell line. Compound 5a showed the best cytotoxic activity on cancerous cell lines in comparison to paclitaxel. Annexin V/ PI staining assay also showed that compounds 5a and 5i would lead to significant apoptosis induction in MDA-MB 486 cell line.

Synthesis and Biological Evaluation of New 3-Substituted-pyrazolo[3,4-b]pyridine Derivatives as Antimicrobial Agents and DHFR Inhibitors

“…Also, n-butyl-urea derivative 6a showed potent activity equal to that of Gentamicin against most of the tested strains. However, the thiourea derivatives 7a-d revealed dramatic lowering in the antibacterial activity, the cyclohexyl thiourea derivative 7a gave moderate activity with MIC values range (16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29)(30)(31)(32) μg/mL and the other derivatives 7b-c showed weak or no activity (NA). The cyclization of the thiazolidin-4-one ring enhanced the inhibition potency against both grampositive and gram-negative strains.…”

“…On the other hand, pyrazoles are an important class of nitrogen heterocyclic compounds, regarding to their vital role in the field of medicinal chemistry. Pyrazole derivatives have a variety of biological activities such as antimicrobial [19][20][21], anticancer [22][23][24], antiinflammatory [25,26], antidiabetic [27,28] and antimalarial [29,30] activities. Also, pyridine-based compounds have a broad spectrum of pharmacological properties include, antimicrobial [31][32][33], anticancer [34,35], antimalarial [36] and antidiabetic [37] activities.…”