Literature DB >> 26247355

Synthesis of mono Mannich bases of 2-(4-hydroxybenzylidene)-2,3-dihydroinden-1-one and evaluation of their cytotoxicities.

Mehtap Tugrak1, Cem Yamali1, Hiroshi Sakagami2, Halise Inci Gul1.   

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.

Entities:  

Keywords:  1-indanone; Chalcone analogue; MTT; Mannich bases; cytotoxicity; dihydroinden-1-one; phenol; selectivity index; synthesis

Mesh:

Substances:

Year:  2015        PMID: 26247355     DOI: 10.3109/14756366.2015.1070263

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  4 in total

1.  Microwave-assisted synthesis and bioevaluation of new sulfonamides.

Authors:  Halise Inci Gul; Cem Yamali; Fatma Yesilyurt; Hiroshi Sakagami; Kaan Kucukoglu; Ilhami Gulcin; Mustafa Gul; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

2.  Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines.

Authors:  Halise Inci Gul; Ebru Mete; Parham Taslimi; Ilhami Gulcin; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-24       Impact factor: 5.051

3.  Designing, synthesis and bioactivities of 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]benzenesulfonamides.

Authors:  Halise Inci Gul; Ebru Mete; Sakip Emre Eren; Hiroshi Sakagami; Cem Yamali; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-23       Impact factor: 5.051

4.  Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones.

Authors:  Sinan Bilginer; Halise Inci Gul; Feyza Sena Erdal; Hiroshi Sakagami; Serkan Levent; Ilhami Gulcin; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.