The present study involves the design, synthesis, characterization and molecular docking studies of
biologically active quinazolin-4-ones, which were synthesized by condensing 2-amino-4-substituted
phenylthiazole with N-methylbenzoxazin-4-one. The N-methylbenzoxazin-4-one and 2-amino-4-
substituted phenylthiazole were synthesized from N-methylanthranilic acid and substituted ketones,
respectively. The ADME properties determined the synthetic accessibility of quinazolin-4-ones by in
silico Swiss ADME. The colorectal anticancer screening was done by using cell HT-29 human colorectal
adenocarcinoma based on molecular docking studies on 3GC7-the structure of p38alpha in complex
with dihydroquinazolinone. Finally, compounds 5Dh8, 5DF6, 5Db2 and 5Di9 exhibited better activity
at a concentration < 10 μg/mL when compared to 5-fluorouracil. The ADME properties revealed that
all the compounds were within the range and docking studies showed the highest binding with glide
score -7.19 and -7.027 Kcal/mol compared to the target protein -10.67 Kcal/mol.