6601-22-5Relevant articles and documents
Discovery of ortho-carborane-conjugated triazines as selective topoisomerase I/II inhibitors
Nakamura, Hiroyuki,Shoji, Atsushi,Takeuchi, Ayano,Ban, Hyun Seung,Lee, Jong-Dae,Yamori, Takao,Kang, Sang Ook
scheme or table, p. 1430 - 1437 (2012/02/06)
The cell growth inhibition profile of 2,4-(2-methyl-ortho-carboranyl)-4- (dimethylamino)-1,3,5-triazine (TAZ-6) was found to be similar to that of ICRF-193, a topoisomerase II inhibitor, as revealed by COMPARE analysis (correlation coefficient (r)≤0.724). Various mono-and di-ortho-carborane- substituted 1,3,5-triazines were synthesized based on the structure of TAZ-6 and tested for their ability to inhibit cell growth and the activities of topoisomerases I and II. Among the compounds synthesized, 3c, 4c, and 4f completely inhibited topoisomerase I activity without affecting topoisomerase II activity, whereas 3a and 3d completely inhibited topoisomerase II activity without affecting topoisomerase I activity, at 100μM.
2-CYANO-1,3,5-TRIAZINE-4,6-DIAMINE DERIVATIVES
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Page/Page column 14, (2010/02/10)
The invention relates to the use of a 2-cyano-1,3,5-triazine -4,6-diamine derivative having general formula (I), wherein R1 is (C1-6)alkyl, (C3-8)cycloalkyl, aryl, aryl(C1-4)alkyl, aryloxy(C1-4)alkyl, heteroaryl or heteroaryloxy(C1-4)alkyl; R2 is H or (C1-4)alkyl; or R1 and R2 together with the nitrogen to which they are bound form a 4-8 membered heterocyclic ring, optionally further comprising 1 or more heteroatoms selected from O, S or NR5, which ring may be substituted with (C1-4)alkyl, (C3-8)cycloalkyl, aryl, aryl(C1-4)alkyl or NR6R7,and which ring may be fused to a benzene ring; R3 is (C1-6)alkyl, (C3-8) cycloalkyl (optionally comprising 1 or more heteroatoms selected from O, S or NR8), aryl, aryl(C1-4)alkyl or heteroaryl; R4 is H or (C1-4)alkyl; or R3 and R4 together with the nitrogen to which they are bound form a 4-8 membered heterocyclic ring, optionally further comprising 1 or more heteroatoms selected from O, S or NR9; R5, R8 and R9 are independently H, (C1-4)alkyl, (C3-8) cycloalkyl, aryl or aryl(C1-4)alkyl; R6 and R7 are independently H or (C1-4)alkyl; or R6 and R7 form together with the nitrogen to which they are bound a 4-8 membered heterocyclic ring; or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of osteoporosis and atherosclerosis.