2. Academic Validation
  3. Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives

Synthesis, antiproliferative activities and telomerase inhibition evaluation of novel asymmetrical 1,2-disubstituted amidoanthraquinone derivatives

  • Eur J Med Chem. 2012 Jan;47(1):323-36. doi: 10.1016/j.ejmech.2011.10.059.
Chia-Chung Lee 1,  Kuo-Feng Huang,  Pen-Yuan Lin,  Fong-Chun Huang,  Chun-Liang Chen,  Tsung-Chih Chen,  Jih-Hwa Guh,  Jing-Jer Lin,  Hsu-Shan Huang
Affiliations

Affiliation

  • 1 Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 114, Taiwan.
PMID: 22100139 DOI: 10.1016/j.ejmech.2011.10.059
Abstract

A series of diversely asymmetrical mono- or disubstituted 1,2-diamidoanthraquinone derivatives were synthesized and evaluated for drug-induced cytotoxicity by SRB assay, Telomerase inhibitory activity by TRAP assay, and hTERT expression by SEAP assay. Interestingly, compounds 4, 11, 21, 32 and 36 exhibited selective potent antiproliferative activities by NCI with IC(50) values in the micromolar range. Of these, only compound 8 showed an IC(50) value of 0.95 μM against PC-3 cell lines (human prostate Cancer) by SRB assay. All the synthesized compounds exhibited a poor or modest Telomerase inhibitory activity by TRAP assay suggesting another mode of action for these compounds. Compound 11 showed broad inhibition against different types of Cancer cell lines in the micromolar and submicromolar range.

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