SYNTHESIS AND BIOLOGICAL EVALUATION OF CHALCONE DERIVATIVES OF ACRIDINES AS ANTICANCER AGENTS

Abstract

A novel series of chalcone fused acridine derivatives (10a-j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and mass 
spectral data. Further, these derivatives were screened for their biological activities towards three different human cancer cell lines such as MCF-7, 
A549 and MDA MB-231. Among the tested derivatives, five compounds, 10a (MCF-7 = 1.89 ± 0.17 µM, A549 = 0.12 ± 0.01 µM and MDA MB-231 
= 2.89 ± 1.78 µM), 10b (MCF-7 = 0.24 ± 0.018 µM, A549 = 0.35 ± 0.02 µM and MDA MB-231 = 0.11 ± 0.01 µM), 10g (MCF-7 = 2.45 ± 1.60 µM 
and A549 = 2.78 ± 1.66 µM), 10h MCF-7 = 1.22 ± 0.11 µM, A549 = 1.76 ± 0.16 µM and MDA MB-231 = 1.34 ± 0.13 µM) and 10j (MCF-7 = 2.67 ± 
1.63 µM, A549 = 1.67 ± 0.14 µM, MDA MB-231 = 0.56 ± 0.015 µM) were demonstrated more potent anticancer activity than positive control (MCF
7 = 3.12 ± 2.56 µM, A549 = 2.10 ± 2.11 µM, MDA MB-231= 3.41 ± 2.59 µM).