Synthesis, Characterization, ADME Study and Anti-proliferative evaluation against MCF-7 breast cancer cell line of new analog of a 4-aminophenyl quinazolinone derivative

Zainab A. Jabbar; Monther F. Mahdi; Basma M.Abd Razik

doi:10.32947/ajps.v23i4.1096

Authors

Zainab A. Jabbar Department of Pharmaceutical Chemistry, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq
Monther F. Mahdi Department of Pharmaceutical Chemistry, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq
Basma M.Abd Razik Department of Pharmaceutical Chemistry, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq

DOI:

https://doi.org/10.32947/ajps.v23i4.1096

Keywords:

Human estrogen receptor-alpfa , MCF-7,quinazolinone

Abstract

New series of 4-aminophenyl quinazolinone attached to an aromatic aldehyde moiety has been designed. Compound (ZA) was synthesized by a reaction of benzene-1,4-diamine with 2-aminobenzoic acid.

The reaction between (ZA) intermediate and different substituted aromatic aldehydes (R1- R6) is considered one of the most common chemical reactions for the synthesis of imine compounds (Schiff bases) to produce compound (ZA1-ZA6). FTIR, ¹H-NMR, and ¹³C-NMR have been used to confirm the chemical structures of various substances. MTT assay was used to assess in vitro anti-proliferative action for estrogen receptor alpha. The anti-proliferative study discovered a dose-dependent effect on cell proliferation in breast cancer (MCF-7) with inhibitory concentration In comparison to the reference medication tamoxifen (IC₅₀ of 133.4µg\mL), IC₅₀ of the compounds (ZA1, ZA2, ZA3) was 0.07964, 57.43 & 0.002717 µg\mL, respectively at 72 hours on same cell line mentioned above, that also signifies that compound ZA1 has a significantly greater effect on this cell line type

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