Synthesis and Cytotoxicities of 2-[4-hydroxy-(3,5-bis-aminomethyl)-benzylidene]-indan-1-ones

TUĞRAK, Mehtap; Gül, Halise İnci; Sakagami, Hiroshi

doi:10.2174/1570180812666150430002002

Makale Tam Makale Uluslararası 2015

Synthesis and Cytotoxicities of 2-[4-hydroxy-(3,5-bis-aminomethyl)-benzylidene]-indan-1-ones

Mehtap TUĞRAK, Halise İnci Gül, Hiroshi Sakagami

LETTERS IN DRUG DESIGN & DISCOVERY Cilt 12 · Sayı 10 · ss. 806–812 · 01.01.2015

DOI ile aç

Özet

Chalcones and Mannich bases are bioactive compounds and known with their cytotoxicities. alpha,beta-Unsaturated ketones are reported with their alkylating potential to cellular thiols thereby inducing cytotoxicities. In this study; Mannich bases (MT2-MT7), which may generate two additional alkylating centers comparing with starting compound 2-(4-hydroxybenzylidene)-2,3-dihydroinden-1-one MT1, were designed and synthesized expecting the increased cytotoxicities in bis Mannich bases. Their cytotoxicities were tested against Ca9-22, HSC-2, HSC-3, and HSC-4 human oral squamous cell carcinoma as tumour cell lines and HGF, HPC, and HPLF human normal oral cells as non tumour cell lines. Amine parts were changed as N-methylpiperazine (MT2), pyrrolidine (MT3), morpholine (MT4), piperidine (MT5), dimethylamine (MT6), and dipropylamine (MT7).

Anahtar kelimeler

cytotoxicity BIOLOGICAL-ACTIVITY Synthesis DNA TOPOISOMERASE-I JURKAT CELLS HYDROCHLORIDES phenol BIS MANNICH-BASES CORRESPONDING AZINE DERIVATIVES ANTIINFLAMMATORY ACTIVITY CELLULAR GLUTATHIONE CANCER CELLS Chalcone analogue Indan-1-one tumour selectivity ANTIFUNGAL EVALUATION

Atıf için künye

TUĞRAK, M., Gül, H. İ., & Sakagami, H. (2015). Synthesis and Cytotoxicities of 2-[4-hydroxy-(3,5-bis-aminomethyl)-benzylidene]-indan-1-ones. LETTERS IN DRUG DESIGN & DISCOVERY, 12(10), 806–812. https://doi.org/10.2174/1570180812666150430002002

BibTeX

@article{tugrak2015-19968,
  author = {TUĞRAK, Mehtap and Gül, Halise İnci and Sakagami, Hiroshi},
  title = {Synthesis and Cytotoxicities of 2-[4-hydroxy-(3,5-bis-aminomethyl)-benzylidene]-indan-1-ones},
  journal = {LETTERS IN DRUG DESIGN & DISCOVERY},
  year = {2015},
  volume = {12},
  number = {10},
  pages = {806--812},
  issn = {1570-1808},
  doi = {10.2174/1570180812666150430002002},
  url = {https://akademik.atauni.edu.tr/yayinlar/19968-synthesis-and-cytotoxicities-of-2-4-hydroxy-35-bis-aminomethyl-benzylidene-indan}
}