Evaluation of Alkylating and Intercalating Properties of Mannich Bases for Cytotoxic Activity

ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)

Volume 14, 12 Issues, 2017

Download PDF Flyer

Letters in Drug Design & Discovery

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Submit Abstracts Online Submit Manuscripts Online

G. Perry
University of Texas
San Antonio, TX

View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 0.974
5 - Year: 2.25

Evaluation of Alkylating and Intercalating Properties of Mannich Bases for Cytotoxic Activity

Letters in Drug Design & Discovery, 11(9): 1096-1106.

Author(s): Huseyin Istanbullu, Yalcin Erzurumlu, Petek Ballar Kirmizibayrak and Ercin Erciyas.

Affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, 35100, Izmir, Turkey.


A series of new “hybrid compounds”, Mannich base derivatives of planar polycyclic/heterocyclic starting materials, was designed and synthesized. The structures of the compounds were confirmed by spectroscopic methods and elemental analysis. Cytotoxicity of compounds was investigated in three cancer cell lines (PC3, HeLa, and MCF7) and one non-tumoral cell line (293 HEK). We tested the DNA-intercalating capability of the molecules by ethidium bromide (EtBr) fluorescence displacement experiment. Compounds' alkylation potency was investigated via in vitro incubation test using 2-mercaptoethanol, a biomimetic nucleophile. The five of the compounds (7s, 9d, 10b, 11b, 12c) are reported for first time in the literature. Our results suggest that compound 9d has a biological activity close to the reference compound doxorubicin, an intercalating agent in clinical use.


Alkylation, cytotoxicity, ethidium bromide displacement, intercalation, mannich bases, mercaptoethanol.

Purchase Online Order Reprints Order Eprints Rights and Permissions

Article Details

Volume: 11
Issue Number: 9
First Page: 1096
Last Page: 1106
Page Count: 11
DOI: 10.2174/1570180811666140529005029
Price: $58

Related Journals

Webmaster Contact: urooj@benthamscience.org Copyright © 2016 Bentham Science