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1 Polish Journal of Chemistry

1 2007

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Synthesis of (3-Amino-7-chloro-8-methyl-1,1-dioxo-4H-1,5,2-benzo[f]dithiazepin-4-ylidene)acetic Acid De rivatives as Potential Antitumor Agents

Brzozowski Z., Sączewski F., Sławiński J.

Polish Journal of Chemistry

2007

Vol. 81, nr 12

2133-2142

Several 3-amino-7-chloro-8-methyl-1,1-dioxo-4H-1,5,2- benzo[f]dithiazepin- 4-yli - dene)acetic acid derivatives (2, 4-15) have been syn the sized. The in vi tro antitumor activity of the compounds 8, 10-12 and 14-15 have been evaluated in the US National Cancer Institute. Screening data indicated that compounds 10, 11 and 14 exhibited high activity against 1-28 human tumor cell lines (GI50 < 0.01 to 3.0 mM). [3-(Benzo-2,1,3-thiadiazol-4-ylamino)-7-chloro-8-methyl-1,1-dioxo-4H-1,5,2-benzo[f]dithiazepin-4--ylidene]acetic acid 11 is the prominent one due to remark able activity and selectivity toward CNS cancer SF-295 cell line of (GI50 < 0.01 mM; TGI = 0.05 mM) and BT-549 cell line of breast cancer (GI50 < 0.01 mM; TGI = 0.09 mM).