Journal Article

Design and synthesis of indole-based elipticine analogues as topoisomerase IIβ inhibitors

Hassan, Ghada S., El-Sayed, Selwan M., El Sayed, Mardia T., Sarhan, Alaadin E., El-Messery, Shahenda M., Hamdy, Nehal A., Alturaifi, Huriyyah A., Ali, Mamdouh M.

2024

Overview

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 GI 50 (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.

• Publisher: Springer US,Springer Nature B.V
• Subject: Acids / Anticancer properties / Antitumor activity / Apoptosis / Biochemistry / Biomedical and Life Sciences / Biomedicine / Bioorganic Chemistry / Cancer / Cell lines / Drug dosages / Enzymes / Inorganic Chemistry / Medicinal Chemistry / Molecular modelling / Original Research Article / Pharmacology/Toxicology / Physicochemical properties / Screening / Single crystals / Toxicity