<abstract xmlns="http://www.w3.org/1999/xhtml"><p>Four classes of aminoquinoline derivatives were prepared: primaquine ureas <bold>1a</bold>–<bold>f</bold>, primaquine bis-ureas <bold>2a</bold>–<bold>f</bold>, chloroquine fumardiamides <bold>3a</bold>–<bold>f</bold> and mefloquine fumardiamides <bold>4a</bold>–<bold>f</bold>. Their antiproliferative activities against breast adeno-carcinoma (MCF-7), lung carcinoma (H460) and colon carcinoma (HCT 116 and SW620) cell lines were evaluated <italic>in vitro</italic>, using MTT cell proliferation assay. The results revealed a low activity of primaquine urea and bis-urea derivatives and high activity of all fumardiamides, with <italic>IC</italic><sub>50</sub> values in low micromolar range against all tested cancer cell lines.</p></abstract>

Four classes of aminoquinoline derivatives were prepared: primaquine ureas 1a–f, primaquine bis-ureas 2a–f, chloroquine fumardiamides 3a–f and mefloquine fumardiamides 4a–f. Their antiproliferative activities against breast adeno-carcinoma (MCF-7), lung carcinoma (H460) and colon carcinoma (HCT 116 and SW620) cell lines were evaluated in vitro, using MTT cell proliferation assay. The results revealed a low activity of primaquine urea and bis-urea derivatives and high activity of all fumardiamides, with IC50 values in low micromolar range against all tested cancer cell lines.

Antiproliferative evaluation of various aminoquinoline derivatives

Faculty of Pharmacy and Biochemistry Department of Medicinal Chemistry

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

{"article-title":"Antiproliferative evaluation of various aminoquinoline derivatives"}

Four classes of aminoquinoline derivatives were prepared: primaquine ureas 1a–f, primaquine bis-ureas 2a–f, chloroquine fumardiamides 3a–f and mefloquine...

Antiproliferative evaluation of various aminoquinoline derivatives

Pubblicato online: 21 ott 2019

Pagine: 661 - 672

Accettato: 24 giu 2019

DOI: https://doi.org/10.2478/acph-2019-0048

Parole chiave
primaquine, chloroquine, mefloquine, fumardiamide, antiproliferative activity

© 2019 Branka Zorc et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Antiproliferative evaluation of various aminoquinoline derivatives

Pubblicato online: 21 ott 2019

Pagine: 661 - 672

Accettato: 24 giu 2019

DOI: https://doi.org/10.2478/acph-2019-0048

Parole chiaveprimaquine, chloroquine, mefloquine, fumardiamide, antiproliferative activity

© 2019 Branka Zorc et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Parole chiave
primaquine, chloroquine, mefloquine, fumardiamide, antiproliferative activity