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Design, Synthesis, and Antitumor Activities of Some Novel Substituted 1,2,3-Benzotriazines
Shenyang Pharmaceutical University, Shenyang, 110016, P.R. China
Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA
* Author to whom correspondence should be addressed.
Received: 2 June 2008; in revised form: 22 June 1995 / Accepted: 23 June 2008 / Published: 24 June 2008
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.
Keywords: 1; 2; 3-Benzotriazine; synthesis; antiproliferative activity; vatalanib succinate.
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MDPI and ACS Style
Lv, J.-L.; Wang, R.; Liu, D.; Guo, G.; Jing, Y.-K.; Zhao, L.-X. Design, Synthesis, and Antitumor Activities of Some Novel Substituted 1,2,3-Benzotriazines. Molecules 2008, 13, 1427-1440.
Lv J-L, Wang R, Liu D, Guo G, Jing Y-K, Zhao L-X. Design, Synthesis, and Antitumor Activities of Some Novel Substituted 1,2,3-Benzotriazines. Molecules. 2008; 13(6):1427-1440.
Lv, Jin-Ling; Wang, Rui; Liu, Dan; Guo, Gang; Jing, Yong-Kui; Zhao, Lin-Xiang. 2008. "Design, Synthesis, and Antitumor Activities of Some Novel Substituted 1,2,3-Benzotriazines." Molecules 13, no. 6: 1427-1440.