NOVEL CHALCONE DERIVATIVES AS ANTICANCER AGENTS: SYNTHESIS, CHARACTERIZATION, AND IN VITRO EVALUATION

Km. Hemlata, Mr. Ravi Kumar Saini*, Mrs. Renu, Dr. Omprakash Goshain, Mr. Gurjeet Singh

ABSTRACT

Background: Cancer remains a leading cause of morbidity and mortality worldwide, necessitating the continuous
development of novel therapeutic agents with improved efficacy and safety profiles (Bray et al., 2020). Chalcones,
a class of open-chain flavonoids, have emerged as promising anticancer agents due to their structural flexibility and
ability to interact with multiple molecular targets (Zhuang et al., 2017). Objective: The present study aimed to
design, synthesize, and evaluate novel chalcone derivatives for their in vitro anticancer activity, along with
characterization and structure–activity relationship (SAR) analysis. Methods: A series of chalcone derivatives
were synthesized via Claisen–Schmidt condensation using substituted acetophenones and aromatic aldehydes. The
synthesized compounds were characterized using FT-IR, ¹H NMR, ¹³C NMR, and mass spectrometry. Anticancer
activity was evaluated against human cancer cell lines (MCF-7, HeLa, A549) using the MTT assay (Mosmann,
1983). Results: Several synthesized compounds exhibited significant cytotoxic activity, with IC₅₀ values in the low
micromolar range. Compounds containing electron-withdrawing substituents such as nitro and halogens showed
enhanced anticancer activity. SAR analysis indicated that substitution patterns significantly influence cytotoxic
potential. Conclusion: The study demonstrates that chalcone derivatives are promising scaffolds for anticancer
drug development. Further in vivo and mechanistic studies are warranted.

Keywords: Chalcone, Anticancer activity, SAR, Cytotoxicity, MTT assay, Flavonoids.