Substituted quinazolines, part 3. Synthesis, in vitro antitumor activity and molecular modeling study of certain 2-thieno-4(3H)-quinazolinone analogs☆

Synthesis of 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and evaluation of their anticancer activity

“…Many researchers have also studied thiophenes extensively due to the fact that new effective compounds can be obtained by the bioisosteric replacement of benzene ring with thiophene 20,21 . Some studies have confirmed that compounds bearing thiophene moiety possess antitumor activity [22][23][24] .…”

Synthesis, antitumor and antimicrobial activity of some new 6-methyl-3-phenyl-4(3H)-quinazolinone analogues: in silico studies

“…Based on aforementioned rational and our studies on quinazoline derivatives as attractive candidates for antitumor 9,[23][24][25] and antimicrobial agents 10,11,21 , we have designed a number of new quinazoline derivatives containing a 3-phenyl substituent attached with different fragments at 2-position to identify the dual antitumor and antimicrobial activities. Moreover, an in silico study, ADME-T prediction and molecular docking studies were used to identify the structural features required for the antitumor properties of the designed compounds.…”

“…Such medical health problems have encouraged many medicinal chemists to search for novel antibacterial agents other than the analogs of existing antibiotics 7 . Quinazolines are frequently used in medicine because of their wide spectrum of biological activities [8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26] . Based on the good performances of quinazoline derivatives in anticancer application, development of novel quinazoline derivatives as anticancer drugs is a promising field 9 .…”

Utility of 2-Methyl-quinazolin-4(3H)-one in the Synthesis of Heterocyclic Compounds with Anticancer Activity

“…A systematic perpusal of literature, reveals that quinazoline derivatives encompass a broad spectrum of pharmaceutical activity profile such as antitumor [4]- [10], anti-HIV [11]- [13], antimicrobial [14]- [16], antibacterial, anti-inflammatory [17]- [20], CNS activity [21]- [23] and cardiovascular activity [24] [25]. The quinazoline nucleus is the scaffold of many antitumor drugs mainly acting as inhibitors of tyrosine kinase receptor (TKR) [26].…”