SciELO - Scientific Electronic Library Online

vol.59 issue3Use of Psychopharmaceuticals in the Northeastern Argentine Region during the decade of 2004-2013Effective potential studies for some new hybrid molecules for their activity against prostate cancer author indexsubject indexarticles search
Home Pagealphabetic serial listing  

Services on Demand




Related links

  • On index processCited by Google
  • Have no similar articlesSimilars in SciELO
  • On index processSimilars in Google


Ars Pharmaceutica (Internet)

On-line version ISSN 2340-9894


NARA, Sukanya  and  GARLAPATI, Achaiah. Design, Synthesis and molecular docking study of hybrids of quinazolin-4(3H)-one as anticancer agents. Ars Pharm [online]. 2018, vol.59, n.3, pp.121-131.  Epub Oct 19, 2020. ISSN 2340-9894.

A series of 4-(2-(4-substituted phenyl)-4-oxoquinazolin-3(4H)-yl)-N-(2-(4-fluorophenyl)-4-oxo-5-(arylidene)thiazolidin-3-yl) benzamides (VIa-n) have been synthesized by condensation of N-(2-(4-fluorophenyl)-4-oxothiazolidin-3-yl)-4-(4-oxo-2-(4-substituted phenyl)quinazolin-3(4H)-yl)benzamides (Va-b) with various aryl/heteroaryl aldehydes using conventional methodology. All compounds were screened for their in vitro anticancer activity against the human breast cancer cell lines (MCF-7), human lung cancer cell lines (A549) using MTT assay method and doxorubicin is used as standard drug. Compound VId, VIk and VIn showed high potency against A549 cell lines with IC50 values 0.035±0.002 µM, 0.031±0.002 µM and 0.030±0.002 µM respectively compared to 0.023±0.002 µM showed by the standard. However, highest activity against MCF-7 cell lines was exhibited by Va, Vb, VIk and VIn with IC50 values between 0.040 - 0.050 µM. All the remaining compounds showed moderate anticancer activity against both the MCF-7 and A549 cell lines. To understand the interactions with active binding site of receptor, molecular docking study was also performed.

Keywords : Quinazolin-4(3H)-one; Thiazolidin-4-one; Anticancer activity; Molecular docking.

        · abstract in Spanish     · text in English     · English ( pdf )