2. Academic Validation
  3. Design, synthesis, and anti-tumor evaluation of novel symmetrical bis-benzimidazoles

Design, synthesis, and anti-tumor evaluation of novel symmetrical bis-benzimidazoles

  • Eur J Med Chem. 2009 Apr;44(4):1808-12. doi: 10.1016/j.ejmech.2008.07.021.
Yan-Hui Yang 1,  Mao-Sheng Cheng,  Qing-He Wang,  Han Nie,  Na Liao,  Jian Wang,  Hong Chen
Affiliations

Affiliation

  • 1 Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
PMID: 18762358 DOI: 10.1016/j.ejmech.2008.07.021
Abstract

A novel symmetrical bis-benzimidazole was designed as DNA minor groove binder. Molecular modeling study showed that it could DOCK into the minor groove of DNA. Several derivatives were synthesized and confirmed by IR, MS, and (1)H NMR. All these novel compounds were screened for cytotoxic activity on SKOV-3, HeLa, and BGC-823 cell lines in vitro. Some compounds showed IC(50)s in the single-digit micromolar range for cytotoxicity in several tumor cell lines.

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