Design, Synthesis and molecular docking study of hybrids of quinazolin-4(3H)-one as anticancer agents

ABSTRACT 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)benzamid...

Full description

Saved in:
Bibliographic Details
Main Authors: Sukanya Nara (Author), Achaiah Garlapati (Author)
Format: Book
Published: Facultad de Farmacia, Universidad de Granada.
Subjects:
Online Access:Connect to this object online.
Tags: Add Tag
No Tags, Be the first to tag this record!

MARC

LEADER 00000 am a22000003u 4500
001 doaj_491a6c3b399b4b478e8c5ed96e9de61d
042 |a dc 
100 1 0 |a Sukanya Nara  |e author 
700 1 0 |a Achaiah Garlapati  |e author 
245 0 0 |a Design, Synthesis and molecular docking study of hybrids of quinazolin-4(3H)-one as anticancer agents 
260 |b Facultad de Farmacia, Universidad de Granada. 
500 |a 2340-9894 
500 |a 10.30827/ars.v59i3.7360 
520 |a ABSTRACT 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. 
546 |a EN 
546 |a ES 
690 |a Quinazolin-4 (3H) -ona 
690 |a Thiazolidin-4-one 
690 |a Actividad anticancerosa 
690 |a Atraque molecular 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Ars Pharmaceutica, Vol 59, Iss 3, Pp 121-131 
787 0 |n http://scielo.isciii.es/scielo.php?script=sci_arttext&pid=S2340-98942018000300121&lng=en&tlng=en 
787 0 |n https://doaj.org/toc/2340-9894 
856 4 1 |u https://doaj.org/article/491a6c3b399b4b478e8c5ed96e9de61d  |z Connect to this object online.