Anticancer Screening and Structure Activity Relationship Study of Some Semicarbazides and 1,2,4-Triazolin-5-ones

Abstract

In this paper some semicarbazide and 1,2,4-triazolin-5-one derivatives are evaluated in vitro for their anticancer activity towards human tumour cell line: ovary (TOV 112D), lung (A 549), breast (T47D) and uterus (Hela). Compounds 2-4 have been found to show the most effective in vitro activity against ovary cancer cell line. For compound 4 the growth inhibition (80% and 70%) is observed in two concentrations (100 µg/ml and 50 µg/ml). The cytotoxic effect of examined compounds seems to be dose-dependent and time-dependent. Compound 7 has GI=80% values towards the breast cancer cell line in concentration of 100 µg/ml. Structure-activity relationship (SAR) studies are carried out for all the compounds of the series. Compounds 2-4 show an activity profile that can be improved through medicinal chemistry strategies.

Cytotoxic Activity against A549 Human Lung Cancer Cells and ADMET Analysis of New Pyrazole Derivatives

“…There are many different types of compounds, both natural and synthetic, with potential medical properties. Substances, such as imidazoles, oxadiazoles, pyrroles, and many of their derivatives, are well studied and described in the literature [1][2][3][4][5]. The main goal of medicinal chemistry is to synthesize compounds with promising activity and therapeutic agents that exhibit lower toxicity.…”

Recent advances in antifungal drug development targeting lanosterol 14α‐demethylase (CYP51): A comprehensive review with structural and molecular insights

“…Reported literature showed that derivatives of the semicarbazide displayed different therapeutic potentials (Mohan et al, 2020; Pitucha & Rzymowska, 2012; Rane et al, 2014). To explore the theses potentials of the semicarbazide Morcoss et al (2020) synthesized a series of benzimidazole derivatives and identified their antifungal potential.…”

Synthesis and Antimicrobial Evaluation of Novel Derivatives of Semicarbazide and 1,2,4‐triazole

“…It follows from the literature survey, derivatives of semicarbazide and 1,2,4‐triazole can be used as anti‐inflammatory , antioxidant , antiparasitic , analgesic , anti‐HIV , antiviral , anticonvulsant , and antitumor agents. In addition, some of them also show antitubercular , antifungal , and antibacterial properties .…”

“…Our team is also interested in search, synthesis, and investigation of bioactive derivatives of thio/semicarbazide and 1,2,4‐triazole . Among them, there were derivatives of 1‐phenoxyacetyl‐4‐substituted thiosemicarbazide and 3‐phenoxymethyl‐4‐substituted‐1,2,4‐triazoline‐5‐thione, which were obtained by our team .…”