Abstract |
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.
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Authors | Jin-Ling Lv, Rui Wang, Dan Liu, Gang Guo, Yong-Kui Jing, Lin-Xiang Zhao |
Journal | Molecules (Basel, Switzerland)
(Molecules)
Vol. 13
Issue 6
Pg. 1427-40
(Jun 24 2008)
ISSN: 1420-3049 [Electronic] Switzerland |
PMID | 18596667
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Phthalazines
- Pyridines
- Triazines
- vatalanib
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Topics |
- 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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