Design, synthesis, and antitumor activities of some novel substituted 1,2,3-benzotriazines.

A series of novel substituted 1,2,3-benzotriazines based on the structures of vatalanib succinate (PTK787) and vandetanib (ZD6474) were designed and synthesized. The antiproliferative effects of these compounds were tested on microvascular endothelial cells (MVECs) using the MTT assay. Introduction of a methoxy and a 3-chloropropoxy group into the 1,2,3-benzotriazines increased the antiproliferative effects. 4-(3-Chloro-4- fluoroanilino)-7-(3-chloropropoxy)-6-methoxy-1,2,3-benzotriazine (8m) was the most effective compound. It was 4-10 fold more potent than PTK787 in inhibiting the growth of T47D breast cancer cells, DU145 and PC-3 prostate cancer cells, LL/2 murine Lewis lung cancer cells and B16F0 melanoma cells.
AuthorsJin-Ling Lv, Rui Wang, Dan Liu, Gang Guo, Yong-Kui Jing, Lin-Xiang Zhao
JournalMolecules (Basel, Switzerland) (Molecules) Vol. 13 Issue 6 Pg. 1427-40 ( 2008) ISSN: 1420-3049 [Electronic] Switzerland
PMID18596667 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Phthalazines
  • Pyridines
  • Triazines
  • vatalanib
  • Animals
  • Antineoplastic Agents
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Drug Screening Assays, Antitumor
  • Endothelial Cells (drug effects)
  • Humans
  • Phthalazines
  • Pyridines
  • Structure-Activity Relationship
  • Triazines (chemical synthesis, chemistry, pharmacology)

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