TY - JOUR
T1 - Synthesis of 2-styrylchromones
T2 - In vitro and in silico anticancer activity evaluation
AU - Via Safitri, Brilliana
AU - Kristanti, Alfinda Novi
AU - Suwito, Hery
AU - Ul Haq, Kautsar
AU - Hendriyanto, Dicky
N1 - Funding Information:
The funding of this research was supported by Universitas Airlangga (Riset Mandat, 2018).
Funding Information:
The authors acknowledge the H.E.J. Research Institute of Chemistry, International Centre for Chemical and Biological Sciences, University of Karachi, Pakistan, for cytotoxicity screening on HeLa cells and HRMS analysis.
Publisher Copyright:
© 2021. Brilliana Via Safitri et al.
PY - 2021/1
Y1 - 2021/1
N2 - The efforts to obtain cancer drugs are still a topic of many research studies considering that cancer is one of the main causes of human death. 2-Styrylchromones are a group of compounds with potential anticancer activity. This research was conducted to synthesize some 2-styrylchromones which involved the formation of 2-methylchromone, followed by aldol condensation with various benzaldehydes. The compound structures were determined using spectroscopic methods, which included ultra violet-visible, Fourier-transform infrared, proton nuclear magnetic resonance, carbon nuclear magnetic resonance- attached proton test APT, and high-resolution mass spectrometry. The toxicity test of the synthesized compounds was carried out in vitro against Henrietta Lacks cancer cells and in silico by molecular docking of the human kinesin Eg5 receptor. The results showed that the synthesized compound substituted with three methoxy groups presented the best anticancer activity, both in vitro (inhibition 100%) and in silico tests (grid score −41,029 kcal/mol).
AB - The efforts to obtain cancer drugs are still a topic of many research studies considering that cancer is one of the main causes of human death. 2-Styrylchromones are a group of compounds with potential anticancer activity. This research was conducted to synthesize some 2-styrylchromones which involved the formation of 2-methylchromone, followed by aldol condensation with various benzaldehydes. The compound structures were determined using spectroscopic methods, which included ultra violet-visible, Fourier-transform infrared, proton nuclear magnetic resonance, carbon nuclear magnetic resonance- attached proton test APT, and high-resolution mass spectrometry. The toxicity test of the synthesized compounds was carried out in vitro against Henrietta Lacks cancer cells and in silico by molecular docking of the human kinesin Eg5 receptor. The results showed that the synthesized compound substituted with three methoxy groups presented the best anticancer activity, both in vitro (inhibition 100%) and in silico tests (grid score −41,029 kcal/mol).
KW - 2-styrylchromone
KW - aldol condensation
KW - HeLa cell
KW - human kinesin Eg5
KW - molecular docking
KW - MTT assay
UR - http://www.scopus.com/inward/record.url?scp=85099377481&partnerID=8YFLogxK
U2 - 10.7324/JAPS.2021.110114
DO - 10.7324/JAPS.2021.110114
M3 - Article
AN - SCOPUS:85099377481
SN - 2231-3354
VL - 11
SP - 121
EP - 128
JO - Journal of Applied Pharmaceutical Science
JF - Journal of Applied Pharmaceutical Science
IS - 1
ER -
