Synthesis, chemical characterization of novel 1,3-dimethyl acridones as cytotoxic agents, and their DNA-binding studies

Simple item page
dc.contributor.authorSathish, N.K.
dc.contributor.authorGopkumar, P.
dc.contributor.authorRajendra Prasad, V.V.S.
dc.contributor.authorShanta Kumar, S.M.
dc.contributor.authorMayur, Y.C.
dc.date.accessioned2026-02-05T09:36:14Z
dc.date.issued2010
dc.description.abstractA series of new 1,3-dimethyl acridone derivatives were synthesized with different alkyl side chain (propyl and butyl) substitution at N 10-position and highly basic amine groups at terminal end of alkyl side chain. All the synthesized molecules were screened for their cytotoxic activity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines. DNA binding constants (K<inf>i</inf>) of selected compounds were determined with calf-thymus DNA. Results showed that the molecules 7, 8, 10, 11, 12, 13, 14, and 15 exhibited good cytotoxic activity with IC<inf>50</inf> value <10 ?M. Compound 14 having (?- hydroxyethyl) piperazine butyl side chain exhibited potent cytotoxic activity against MCF-7 cell line and DNA-intercalating properties. Examination of the relationship between lipophilicity and acridone derivatives showed poor correlation. © Birkhäuser Boston 2009.
dc.identifier.citationMedicinal Chemistry Research, 2010, 19, 7, pp. 674-689
dc.identifier.issn10542523
dc.identifier.urihttps://doi.org/10.1007/s00044-009-9222-8
dc.identifier.urihttps://idr.nitk.ac.in/handle/123456789/27416
dc.subject1,3 dimethyl 10h acridinone
dc.subject10 (3 chloropropyl) 1,3 dimethyl 10h acridinone
dc.subject10 (3' n morpholinopropyl) 1,3 dimethyl 10h acridinone
dc.subject10 (3' n piperidinopropyl) 1,3 dimethyl 10h acridinone
dc.subject10 (3' n pyrrolidinopropyl) 1,3 dimethyl 10h acridinone
dc.subject10 (4' chlorobutyl) 1,3 dimethyl 10h acridinone
dc.subject10 (4' n [(beta hydroxyethyl)piperazine]butyl] 1,3 dimethyl 10h acridinone
dc.subject10 (4' n morpholinobutyl) 1,3 dimethyl 10h acridinone
dc.subject10 (4' n piperidinobutyl) 1,3 dimethyl 10h acridinone
dc.subject10 (4' n pyrrolidinobutyl) 1,3 dimethyl 10h acridinone
dc.subject10 [3' (n diethylamino)propyl] 1,3 dimethyl 10h acridinone
dc.subject10 [3' n (methylpiperazino)]propyl 1,3 dimethyl 10h acridinone
dc.subject10 [3' n [(beta hydroxyethyl)piperazine]propyl] 1,3 dimethyl 10h acridinone
dc.subject10 [4' (n diethylamine)butyl] 1,3 dimethyl 10h acridinone
dc.subject10 [4' n (methylpiperazino)butyl] 1,3 dimethyl 10h acridinone
dc.subjectacridone derivative
dc.subjectcyclophosphamide
dc.subjectcytotoxic agent
dc.subjectDNA
dc.subjectdoxorubicin
dc.subjectunclassified drug
dc.subjectalkylation
dc.subjectantineoplastic activity
dc.subjectarticle
dc.subjectbinding affinity
dc.subjectcatalysis
dc.subjectcell strain HL 60
dc.subjectcell strain MCF 7
dc.subjectcontrolled study
dc.subjectcyclization
dc.subjectcytotoxicity
dc.subjectdrug DNA binding
dc.subjectdrug synthesis
dc.subjecthuman
dc.subjecthuman cell
dc.subjecthydrophobicity
dc.subjectIC 50
dc.subjectlipophilicity
dc.subjectsubstitution reaction
dc.titleSynthesis, chemical characterization of novel 1,3-dimethyl acridones as cytotoxic agents, and their DNA-binding studies

Files

Collections

Journal Articles