Search for new antitumor compounds among n-glycoside indolo[2,3-a]carbazole derivatives


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Abstract

The study investigated antitumor activity of 10 new compounds in the series of N-glycosides of indolo[2,3-a] carbazoles. The results identified strong antitumor activity of compounds LCS-1208, LCS -1054, LCS -999 and LCS-1006 against lymphocytic leukemia P-388 (ILS=85 - 119%). Glycosides LCS-1208, LCS-999 and LCS-1006 exhibited high antitumor activity immediately after treatment for Lewis epidermoid lung carcinoma LLC (TGI =90%). In addition, the antitumor effect after LCS-999 and LCS-1006 treatment kept on for 10 days, and LCS-1208 - for 15 days. Glycoside LCS-1208 had a therapeutic efficiency on melanoma B-16 for 7 days (TGI=91 - 58%). Thus, the study of relation «structure-activity» in a series of derivatives of N-glycosides of indolo[2,3-a]carbazoles allowed to select highly effective compound LCS-1208 for preclinical studies.

About the authors

Marina P. Kiseleva

N.N. Blokhin Russian Cancer Research Center

Email: marina-kiselyova@mail.ru
MD 115478, Moscow, Russian Federation

Z. S Smirnova

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

L. M Borisova

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

I. Yu Kubasova

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

L. V Ektova

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

T. D Miniker

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

I. L Plikhtiak

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

L. A Medvedeva

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

V. A Eremina

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

N. I Tikhonova

N.N. Blokhin Russian Cancer Research Center

115478, Moscow, Russian Federation

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