TY - JOUR
T1 - Synthesis, cytotoxic study and docking based multidrug resistance modulator potential analysis of 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamides
AU - Kumar, Rajesh
AU - Kaur, Maninder
AU - Bahia, Malkeet Singh
AU - Silakari, Om
PY - 2014/6/10
Y1 - 2014/6/10
N2 - The present study describes the synthesis of fifteen 2-(9-oxoacridin-10(9H) -yl)-N-phenyl acetamide derivatives (13a-o) through condensation of 2-chloro-N-phenyl acetamides (12a-o) with acridone molecule (10). All the synthesized compounds were screened for their anti-cancer activity against three diverse cell lines including breast (MCF-7), cervical (HeLa) and lung adenocarcinoma (A-549) employing standard MTT assay. Among synthesized molecules, 13k and 13l showed good cytotoxicity activity against considered three cancer cell lines. Additionally, in silico studies of multidrug resistance modulator (MDR) effects of these compounds was performed by docking simulation in the ATP binding site of P-gp. The results of docking simulation displayed important interactions of these molecules in the active site of this protein and predicted their MDR modulator behavior.
AB - The present study describes the synthesis of fifteen 2-(9-oxoacridin-10(9H) -yl)-N-phenyl acetamide derivatives (13a-o) through condensation of 2-chloro-N-phenyl acetamides (12a-o) with acridone molecule (10). All the synthesized compounds were screened for their anti-cancer activity against three diverse cell lines including breast (MCF-7), cervical (HeLa) and lung adenocarcinoma (A-549) employing standard MTT assay. Among synthesized molecules, 13k and 13l showed good cytotoxicity activity against considered three cancer cell lines. Additionally, in silico studies of multidrug resistance modulator (MDR) effects of these compounds was performed by docking simulation in the ATP binding site of P-gp. The results of docking simulation displayed important interactions of these molecules in the active site of this protein and predicted their MDR modulator behavior.
KW - Acridone derivatives
KW - Cytotoxicity
KW - Docking analysis
KW - MTT assay
KW - Multidrug resistance
UR - http://www.scopus.com/inward/record.url?scp=84899056158&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2014.04.030
DO - 10.1016/j.ejmech.2014.04.030
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C2 - 24769346
AN - SCOPUS:84899056158
SN - 0223-5234
VL - 80
SP - 83
EP - 91
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -