الفهرس 
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Abstract
Background: The present study deals with the synthesis of new benzothiazole derivatives to be tested for their antitumor activity. Also, discusses the classification of anticancer drugs based on their mode of action, also includes different examples from recent literatures describing the antitumor activity of different series of piperazinoacetamides, arylidene thiazolidinone, arylidene carbohydrazide, acid hydrazide, thiosemicarbazide, triazole and sulfonyl derivatives. Method: includes the synthetic procedures of the designed compounds as well as the physicochemical and spectral data of the prepared compounds and the adopted procedure of MTT assay for antitumor screening and EGFR-TK assay. Results: compounds 84 and 85 proved to have the highest potency against the tested cancer cell lines. Compounds, 84, 85, 95, 101, 106 displayed strong activity against all tested cancer cells. Notably, the most active antitumor compounds 84 and 85 represented the most potent inhibitors to EGFR with IC50 values of 24.58 and 30.42 nM respectively in comparison with 17.38 nM for lapatinib as a standard drug. Conclusion: In the present study, different series of benzothiazole-based derivatives were synthesized. The most active antitumor compounds were the acid hydrazones 84 and 85 which also represented the most potent inhibitors to EGFR with IC50 values of 24.58 and 30.42 nM respectively in comparison with 17.38 nM for lapatinib as a standard drug. Docking studies into EGFR active site revealed that compounds 84 and 85 showed a pattern of binding similar to lapitinib as the reference ligand as they fulfilled the key interactions, where the hydrogen bonding with Lys745 was established. Compounds of interest, namely 84 and 85, were deeply buried into the active site and completely housed in its cavity which in turn has its impact on their higher inhibitory activity on EFGR enzyme. Surface mapping displayed a deep interaction with the hydrophobic pocket at ATP binding back site that could be in charge for perfect fitting at active site.