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

Authors :
El Sayed, Mardia T.
Sarhan, Alaadin E.
Alturaifi, Huriyyah A.
El-Sayed, Selwan M.
Hassan, Ghada S.
Hamdy, Nehal A.
El-Messery, Shahenda M.
Ali, Mamdouh M.
Source :
Medicinal Chemistry Research; Jun2024, Vol. 33 Issue 6, p885-902, 18p
Publication Year :
2024

Abstract

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<subscript>50</subscript> (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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
10542523
Volume :
33
Issue :
6
Database :
Complementary Index
Journal :
Medicinal Chemistry Research
Publication Type :
Academic Journal
Accession number :
177925672
Full Text :
https://doi.org/10.1007/s00044-024-03222-2