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Bioorg Med Chem Lett. 2008 Oct 1;18(19):5272-6. doi: 10.1016/j.bmcl.2008.08.050. Epub 2008 Aug 22.

Synthesis of unsymmetrical biphenyls as potent cytotoxic agents.

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1
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.

Abstract

Twenty-six unsymmetrical biphenyls were synthesized and evaluated for cytotoxic activity against DU145, A549, KB and KB-Vin tumor cell lines. Three compounds 27, 35 and 40 showed very potent activity against the HTCL panel with an IC(50) value range of 0.04-3.23 microM. In addition, fourteen active compounds were all more potent against the drug-resistant KB-Vin cell line than the parental KB cell line. Preliminary SAR analysis indicated that two bulky substituents on the 2,2'-positions of unsymmetrical biphenyl skeleton are necessary and crucial for in vitro anticancer activity, thus providing a good starting point to develop unsymmetrical biphenyls as novel anticancer agents.

PMID:
18782668
PMCID:
PMC2577197
DOI:
10.1016/j.bmcl.2008.08.050
[Indexed for MEDLINE]
Free PMC Article
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