Molecular Modelling and Synthesis of Quinazoline-Based Compounds as Potential Antiproliferative Agents
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In this study, four series of 4-anilinoquinazoline derivatives were designed and synthesized as potential anti-proliferative agents. Mechanism of anticancer activity was explained through molecular docking of the target compounds into epidermal growth factor receptor tyrosine kinase (EGFR-TK) active site which displayed comparable binding mode of certain compounds to that of lapatinib. Moreover, the newly synthesized compounds were tested for their anti-proliferative activity on breast carcinoma cell line (MCF-7). 6-(4-Benzylpiperazin-1-ylsulfonyl)-4-(4-bromoanilino)quinazoline (14g) exhibited the most potent inhibitory activity (IC50=5.52 µ<span style="font-variant: small-caps;">M</span>).
- 公益社団法人 日本薬学会の論文
公益社団法人 日本薬学会 | 論文
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