Molecular modelling and synthesis of quinazoline-based compounds as potential antiproliferative agents
Yassen, Asmaa Said Ali; Elshihawy, Hosam Eldin Abd Elhamed Ahmed; Said, Mohamed Mokhtar Amin; Abouzid, Khaled;
Abstract
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 µM).
Other data
| Title | Molecular modelling and synthesis of quinazoline-based compounds as potential antiproliferative agents | Authors | Yassen, Asmaa Said Ali; Elshihawy, Hosam Eldin Abd Elhamed Ahmed; Said, Mohamed Mokhtar Amin; Abouzid, Khaled | Keywords | Anti-proliferative agent;Quinazoline;Tyrosine kinase | Issue Date | 2014 | Journal | Chemical and Pharmaceutical Bulletin | Volume | 62 | Issue | 5 | Start page | 454 | End page | 466 | ISSN | 00092363 | DOI | 10.1248/cpb.c14-00016 | PubMed ID | 24789927 | Scopus ID | 2-s2.0-84899761382 |
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