Work

Design and Synthesis of Propargyloxy Functionalized Pyrazole‐Based Aurones: Exploring Their Potent Anticancer Properties Against AGS and MCF‐7 Cell Lines

Year: 2024

Type: article

Abstract: ABSTRACT FDA‐approved numerous commercial and natural drugs used in cancer treatment feature either pyrazole or alkyne moieties. On the basis of this, we designed and synthesized 20 novel propargyloxy‐substituted pyrazole‐based aurones (10a–j and 11a–j) and evaluated for their anticancer potential against cancerous MCF‐7 and human gastric adenocarcinoma (AGS) cell lines, as well as normal cell line human embryonic kidney 293 (HEK‐293), through MTT assay. Among these tested compounds, five (10d–f, 11e, and 11f) displayed potent cytotoxic properties for AGS cancer cell line with IC50 values ranging from 19.7 to 28.5 µM, better than the reference drugs leucovorin (IC50 = 30.8 µM) and oxaliplatin (IC50 = 29.8 µM). Furthermore, compounds 10b, 10c, 11a, 11c, and 11d demonstrated a significant cytotoxic potential against the MCF‐7 cancer cell line with a single‐digit micromolar IC50 potency (4.8–8.5 µM) compared to the standard drug paclitaxel (IC50 = 19.7 µM). The cytotoxic studies of above selected potent active hybrid compounds, against HEK‐293, normal cell line, further highlight the potential use of 10c molecule (IC50 = 4.8 µM against MCF‐7 cells) as an anticancer agent for breast cancer with a selectivity index of 2.597. The cytotoxic results were further supported by the molecular docking studies.

Source: Chemistry & Biodiversity

DOI: 10.1002/cbdv.202402186