Mardia T. El Sayed, Alaadin E. Sarhan, Huriyyah A. Alturaifi, Selwan M. El-Sayed, Ghada S. Hassan, Nehal A. Hamdy, Shahenda M. El-Messery, Mamdouh M. Ali
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Design and synthesis of indole-based elipticine analogues as topoisomerase IIβ inhibitors
New ellipticine analogs with indole cores were synthesized. and evaluated for their anticancer activity. A new compound, scaffolds, revealed broad-spectrum anticancer potential in one-dose and five doses screening. against the full 60-cell line at NCI. Compounds 2a and 3c had been selected for five-dose screening, where they showed marked anticancer activity against the tested cell lines with an average GI50 (MG-MID) value of 2.23 and 0.98 mM, respectively. Compounds 2a, 2b, 2d, 3b, 3c, and 12 showed noted Topoisomerase Type IIβ inhibitory activity with inhibition records 85.45, 94.7, 93.5, 91.6, 89, and 94.5 percent, respectively. Molecular modeling studies and physicochemical parameter calculations of the most active compounds confirmed their safe. drug-like properties. as a promising anticancer class.
期刊介绍：
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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