Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates

Synthesis of methyl [3-alkyl-2-(2,4-dioxo-3,4-dihydro-2H-quinazolin-1-yl)-acetamido] alkanoate

“…Anticancer agent Iressa (ZD1839) A is a clinically approved example of quinazoline-based inhibitors which is in phase III clinical trials for cancer used to inhibit the receptor tyrosine kinase of epidermal growth factor. also exhibit pronounced biological activities as antimicrobial, 7,8 anti-HIV (NNRTI), 9,10 anti-tumour, [11][12][13][14][15][16] potential analgesic and anti-inflammatory activity. 17 Non-proteinogenic amino acids are major component in a number of drugs including β-lactam antibiotics 18 and glutamate antagonists.…”

Design, Synthesis, Computer Modeling and Analgesic Activity of Some New Disubstituted Quinazolin-4(3H)-ones

“…All the newly synthesized compounds VIII [1][2][3][4][5][6][7][8][9][10][11][12] were preliminarily evaluated for their analgesic and Anti-inflammatory activities (using writhing test) using paracetamol as writhing protective stander. The analgesic activity of the newly synthesized compounds VIII [1][2][3][4][5][6][7][8][9][10][11][12] compared to paracetamol (Sigma Chemical Co., St. Louis, MO, USA) as a reference was measured after and 30, 60, 90, 120, 150, and 180 after p-benzoquinone (Aldrich) subcutaneous injection.…”

“…The solid product was obtained crystallized from ethanol 95% to afford the desired products VII 1-4 . Synthesis of substituted-2-Benzylamino-3-(substituted benzylidene amino) quinazolin-4(3H)-one VIII [1][2][3][4][5][6][7][8][9][10][11][12] General procedure: A mixture of 3-amino-2-benzylamino substituted quinazolin-4(3H)-one VII 1-4 (0.01 mol) and different aromatic aldehydes derivative (0.01 mol) in acetic acid was refluxed for 30 hrs. After completion of reaction (TLC) the reaction mixture was poured into crushed ice and the solid obtained was crystallized from ethanol 95% to obtain pure compounds VIII 1-12 .…”

“…Quinazolines derivatives exhibited a vital role in many pharmacological activities [1][2][3][4][5][6][7][8] including anti-inflammatory, [9] antibacterial, [10] and anticonvulsant, [11] activities. Schiff 's bases have generated a great deal of attention due to their interesting pharmaceutical activities include possess potent analgesic and antiinflammatory activities [12].…”

Synthesis and In Vitro Cytotoxic Properties of Polycarbo-Substituted 4-(Arylamino)quinazolines

“…Quinazolines constitute an important class of compounds with a wide-range of biological properties including anticancer [1][2][3], antibacterial [4], antimicrobial [5] and antihypertensive [6] activities. Among this class of heterocycles, the 4-anilinoquinazolines have established themselves as selective inhibitors of the epidermal growth factor receptor (EGFR) tyrosine kinase phosphorylation, which results from competitive binding at the ATP site [7].…”