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Synthesis, in vitro evaluation and molecular modelling of naphthalimide analogue as anticancer agents.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2013 Oct; Vol. 68, pp. 352-60. Date of Electronic Publication: 2013 Aug 11. - Publication Year :
- 2013
-
Abstract
- A series of amine substituted naphthalimide analogue were synthesized and evaluated for in vitro anti-tumour activities against 60 tumour cell lines at a single dose concentration of 10 μM. These new analogue showed potential anticancer activities against various cancer cell lines. Compound 5d exhibited significant growth inhibition and was evaluated as 60 cell panel at five dose concentration levels. Compound 5d proved to be fivefold more active than standard antitumour drug 5-fluorouracil (5-FU) with MG-MID GI50 and TGI values of 5.05 and 38.71 respectively. ct-DNA binding studies of most active compound 5d revealed strong interacting properties. Molecular docking studies in the active binding site provided complementary theoretical support for the experimental biological data acquired.<br /> (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Cell Line, Tumor
Cell Proliferation drug effects
Humans
Inhibitory Concentration 50
Structure-Activity Relationship
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Models, Molecular
Naphthalimides chemical synthesis
Naphthalimides chemistry
Naphthalimides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 68
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23994328
- Full Text :
- https://doi.org/10.1016/j.ejmech.2013.07.027