2. Academic Validation
  3. Synthesis and cytotoxicity of 8-cyano-3-substitutedalkyl-5-methyl-4-methylene-7-methoxy-3,4-dihydropyrido[4,3-d]pyrimidines

Synthesis and cytotoxicity of 8-cyano-3-substitutedalkyl-5-methyl-4-methylene-7-methoxy-3,4-dihydropyrido[4,3-d]pyrimidines

  • Bioorg Med Chem Lett. 2011 Oct 1;21(19):5975-7. doi: 10.1016/j.bmcl.2011.07.067.
Wen-Yan Mo 1,  Yong-Ju Liang,  Yu-Cheng Gu,  Li-Wu Fu,  Hong-Wu He
Affiliations

Affiliation

  • 1 Key Lab of Pesticide and Chemical Biology, Ministry of Education, School of Chemistry, Central China Normal University, Wuhan 430079, PR China.
PMID: 21843939 DOI: 10.1016/j.bmcl.2011.07.067
Abstract

Synthesis and cytotoxicity of 11 4-methylene pyrido[4,3-d]pyrimidines 5a-k were described. Cytotoxicity assay results showed that some compounds had much stronger antitumor activity than Fluorouracil against KB cell lines. The most active compound 5i exhibited high potency against KB, CNE2, MGC-803 cell lines with IC(50) values of 0.48, 0.15, 0.59 μM, respectively. The preliminary structure-activity relationships indicated that the introduction of benzyl groups bearing electron-donating function groups is favorable for the activity.

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