Back to Search
Start Over
Synthesis of mono Mannich bases of 2-(4-hydroxybenzylidene)-2,3-dihydroinden-1-one and evaluation of their cytotoxicities.
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2016 Oct; Vol. 31 (5), pp. 818-23. Date of Electronic Publication: 2015 Aug 06. - Publication Year :
- 2016
-
Abstract
- Chalcones and Mannich bases are a group of compounds known for their cytotoxicities. In this study restricted chalcone analogue, compound 2-(4-hydroxybenzylidene)-2,3-dihydroinden-1-one MT1, was used as a starting compound to synthesize new mono Mannich bases since Mannich bases may induce more cytotoxicity than chalcone analogue that they are derived from by producing additional alkylating center for cellular thiols. In this study, cyclic and acyclic amines were used to synthesize Mannich bases. All compounds were tested against Ca9-22 (gingival carcinoma), HSC-2, HSC-3 and HSC-4 (oral squamous cell carcinoma) as tumour cell lines and HGF (gingival fibroblasts), HPC (pulp cells) and HPLF (periodontal ligament fibroblasts) human normal oral cells as non tumour cell lines. Cytotoxicity, selectivity index (SI) values and potency selectivity expression (PSE) values expressed as a percentage were determined for the compounds. According to data obtained, the compound MT8 with the highest PSE value bearing N-methylpiperazine moiety seems to be a good candidate to develop new cytotoxic compounds and is suited for further investigation.
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents toxicity
Cell Line
Cell Line, Tumor
Cell Survival drug effects
Humans
Hydroxybenzoates chemical synthesis
Hydroxybenzoates chemistry
Hydroxybenzoates toxicity
Indenes chemistry
Mannich Bases chemistry
Molecular Structure
Neoplasms drug therapy
Indenes chemical synthesis
Indenes toxicity
Mannich Bases chemical synthesis
Mannich Bases toxicity
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 31
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26247355
- Full Text :
- https://doi.org/10.3109/14756366.2015.1070263