Biopolymers and cell. 2003; 19 (5): 467 - 471

Antitumor activity of 6-substituted derivatives of 4-alkylaminoquinazolines

SAPELKIN V. M., MAKOVENKO I. E., LUKASHOV S. S., DUBININA G. G., YARMOLUK S. M.

13 derivatives of 6-R-4-alkylaminoauinazoline were synthesized and tested for antitumor activity (in vivo). According to the resultes of testing with 56 human tumor cell lines four compounds 4.1, 4.9-4.11 were shown to inhibit the proliferation of cancer cells at low micromotor concentrations, l-phenylethylf 4 quinuzolinylfamine (4.1) exhibits antitumor activity: CI50 2.29 öÌ; LC50 46.7mkM (cell line SK-MFL-5 (Melanoma)); the 6-bromo4 auinazolinyKtert-butyDamine (4. to): GI50 3 82 uM; LC50 43.7 uM (cell line SK-MEl.-S (Melanoma)) and GI50 2 64 uM, LC50 44.2 fiM (cell line CAKI-l (Renal Cancer)).