2. Academic Validation
  3. A facile synthesis and biological activity of novel tetrahydrobenzo[4',5']thieno[3',2':5,6]pyrido[4,3-d]pyrimidin-4(3H)-ones

A facile synthesis and biological activity of novel tetrahydrobenzo[4',5']thieno[3',2':5,6]pyrido[4,3-d]pyrimidin-4(3H)-ones

  • Bioorg Med Chem Lett. 2009 Dec 1;19(23):6713-6. doi: 10.1016/j.bmcl.2009.09.117.
Qingyun Ren 1,  Yong-Ju Liang,  Hongwu He,  Liwu Fu,  Yucheng Gu
Affiliations

Affiliation

  • 1 Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, PR China.
PMID: 19846302 DOI: 10.1016/j.bmcl.2009.09.117
Abstract

The synthesis and biological activity of 2-substituted-8,9,10,11-tetrahydrobenzo[4',5']thieno[3',2':5,6] pyrido[4,3-d]pyrimidin-4(3H)-ones are described. Bioassay results indicated that these compounds have Antifungal activity against Botrytis cinerea at a concentration of 50mg/L. In addition, compounds 5m and 5n were effective to both KB cells and their parent multidrug resistant KBv200 cells with the overexpression of ABCB1. For example, compound 5m showed the best inhibition against KB and KBv200 cells with IC(50) values of 17.4 and 25.4 microM, respectively.

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