Dissemin is shutting down on January 1st, 2025

Published in

Newlands Press, Future Medicinal Chemistry, 10(10), p. 1159-1175, 2018

DOI: 10.4155/fmc-2017-0206

Links

Tools

Export citation

Search in Google Scholar

Design, synthesis, anticancer screening, docking studies and in silico ADME prediction of some β-carboline derivatives

Journal article published in 2018 by Mohamed A. Abdelsalam ORCID, Omaima M. AboulWafa, El-Sayed A. M. Badawey, Mai S. El-Shoukrofy, Mostafa M. El-Miligy, Noha Gouda, Mahmoud M. Elaasser
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

Full text: Unavailable

Green circle
Preprint: archiving allowed
Upload
Green circle
Postprint: archiving allowed
Upload
Red circle
Published version: archiving forbidden
Policy details
Data provided by SHERPA/RoMEO

Abstract

Background: Medicinal interest has focused on β-carbolines as anticancer agents. Methodology/Results: Several β-carbolines were designed, synthesized and evaluated for their cytotoxic activity against MCF-7 and A-549 cancer cell lines using MTT assay. Compounds 13a, 13c, 13d and 20a were the most promising showing high selectivity indices. Compounds 13c and 20a showed potent inhibition of topoisomerase (topo-I) and kinesin spindle protein (KSP/Eg5 ATPase) which was confirmed by their docking results into the active site of both enzymes. In silico physicochemical calculations predicted that compounds 13a, 13d and 20a obeyed Lipinski's rule of five. Conclusion: Compounds 13c and 20a are multitarget anticancer leads that act as potent inhibitors for both topo-I and/or KSP ATPase.