Record Details

Synthesis of novel anticancer coumarin-triazole-chalcone hybrids as potential AKT inhibitors

NOPR - NISCAIR Online Periodicals Repository

View Archive Info
 
 
Field Value
 
Title Synthesis of novel anticancer coumarin-triazole-chalcone hybrids as potential AKT inhibitors
 
Creator Mallikarjun, E
Suneesha, D
Kumar, A Niranjana
Singh, Akanksha
Dutta, Hashnu
Kumar, Kotesh
Srinivas, K V N Satya
Meena, Abha
Venkatesh, B
Jain, Nishant
Sravanthi
Radhika, T
 
Subject Coumarins
1,2,3-Triazole
Chalcones
Anticancer Activity
Molecular docking
 
Description 1162-1170
This research article presents the synthesis of a novel series of hybrid analogues of Coumarin-Triazole-Chalcone, which are potential bioactives with a novel mode of action for anticancer therapy. The compounds have been synthesized via aldol condensation and 1,3-dipolar cycloaddition, resulting in the generation of hybrid heterocyclic systems that combine two or more pharmacophores. The synthesized compounds have then been screened for anticancer activity against various human cancer cell lines, including A549 (lung cancer), HeLa (Cervix carcinoma), PANC1 (pancreatic cancer), HT1080 (Fibrosarcoma) and HEK293 (Human embryonic kidney cells), in vitro. One of the compounds, para-nitrile chalcone 9a, demonstrates significant IC50 values in the range of 3.1 to 7.02 μg/mL when compared to the others. All the compounds 9a-d have shown higher IC50 values towards HEK-293 cells indicating their non-toxic nature towards normal cells. Furthermore, in silico approaches have been employed to assess the efficacy of compounds that are active in the MTT assay against molecular targets. The authors conducted docking studies of the proteins PI3K and AKT, which are common target biomarkers in Pancreatic cancer, Lung cancer, Cervical cancer, and Fibrosarcoma, with compound 9a and some known inhibitors. The results show that compound 9a has a good binding affinity with AKT (–10.6) and PI3K (–10.3). However, it is found to be more specific for AKT as its binding site amino acid interactions are similar to those of known AKT inhibitors. These findings provide evidence that hybrid heterocyclic systems may be useful for developing potential bioactives with a novel mode of action for anticancer therapy.
 
Date 2023-11-17T06:10:43Z
2023-11-17T06:10:43Z
2023-11
 
Type Article
 
Identifier 2583-1321 (Online); 0019-5103 (Print)
http://nopr.niscpr.res.in/handle/123456789/62905
https://doi.org/10.56042/ijc.v62i11.2610
 
Language en
 
Publisher NIScPR-CSIR,India
 
Source IJC Vol.62(11) [November 2023]