الفهرس 
Synthesis and evaluation of novel compounds containing thiourea and 1,3-thiazolidinone derivatives as anticancer
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Abstract
New acetamides IVa-h and 1,3-thiazolidinone derivatives VIIa-h were designed, synthesized and evaluated for their cytotoxic activity over MCF-7 and A549 cell lines along with their lead compounds (erlotinib and gefitinib).The newly designed compounds were prepared according to the adopted procedures in schemes 1 and 2 from their quinazolinone parents. 2DQSAR, 3DQSAR pharmacophore and docking molecular modeling protocols using Discovery Studio program were conducted beside a full biological assay for these compounds. The cytotoxicity evaluation demonstrated that compounds IVc, IVd, VIIa, VIId, VIIg exhibited potent cytotoxic activities against both MCF-7 and A549 cell lines as well as the molecular modeling studies that corroborated to the affinity of the compounds towards EGFR, consequently these five compounds were then screened for their EGFR inhibition and as well evaluated for their toxicity over normal cells, which revealed that, the acetamide derivative IVd and the thiazolidinone derivative VIIa were the most potent and least toxic. DNA flow cytometry analysis was conducted for compounds IVd and VIIa, which indicated that both compounds induce arrest at G2/M phase of the cell cycle