Development of Unique Pyrazoline Analogues for Screening Anticancer and Anti-inflammatory Studies

Abstract

Cancer is a major threat to human society in the world, which results in a maximum probability of death. In the present scenario, chemotherapy is the main cancer treatment, but still, it has its limitations. Hence, cytotoxic and chemotherapy medicines are the main focus of research for medicinal chemists. So, it is the need of the hour to explore the possibility of effective and safe anticancer drugs. The current research involves the synthesis of pyrazoline derivatives (PYR1-PYR8), which are novel cytotoxic agents developed from recently formulated chalcones (CHL1-CHL8). Title compounds were prepared by subjecting the chalcones with by hydrazine hydrate in ethanolic acetic acid. The purified synthesized compounds were characterized by IR, 1H-NMR, and mass spectroscopic evaluation. Using in-vitro models, cytotoxicity evaluations were conducted on cell lines associated with lung cancer by MTT and SRB methods using doxorubicin as standard, which revealed differing levels of cytotoxic effects among the compounds. The egg albumin denaturation and protein denaturation methods were used to access in-vitro anti-inflammatory activity. Compound PYR4 and PYR6 showed significant anti-inflammatory efficacy in relation to diclofenac sodium as the reference drug. Compound PYR3, PYR4, and PYR6 displayed noteworthy anticancer activity matched to doxorubicin, which is a reference drug. The current research asserts that the newly developed pyrazoline derivatives exhibit high levels of cytotoxicity and anti-inflammatory effects. However, their preclinical and clinical significance needs a thorough evaluation.