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Synthesis, structure-activity relationship and biological evaluation of novel nitrogen mustard sophoridinic acid derivatives as potential anticancer agents.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Oct 01; Vol. 25 (19), pp. 4092-6. Date of Electronic Publication: 2015 Aug 18. - Publication Year :
- 2015
-
Abstract
- A series of novel nitrogen mustard sophoridinic acid derivatives were designed, synthesized and evaluated for their cytotoxicity. Of the newly synthesized compounds, compound 6 exhibited a potent effect against hepatocellular carcinoma in vitro and in vivo. SAR analysis indicated that introduction of a nitrogen mustard group to the structure of sophoridinic acid significantly enhance the antitumor activity. Moreover, molecular docking study exhibited benzyl group introduced to the nitrogen atom at the 12-position and aryl nitrogen mustard group at the 4'-carboxyl region for compound 6 were beneficial for the higher anticancer activity. This work provides useful information for further structural modifications of these compounds and for the synthesis of new, potent antitumor agents.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemistry
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Hep G2 Cells
Humans
Molecular Docking Simulation
Molecular Structure
Nitrogen Mustard Compounds chemical synthesis
Nitrogen Mustard Compounds chemistry
Structure-Activity Relationship
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Nitrogen Mustard Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26299348
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.08.035