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초록
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 100 mu M.
키워드
NEUTRON-CAPTURE THERAPY; TUMOR-CELL-LINES; DNA TOPOISOMERASES; 2,4,6-TRISUBSTITUTED TRIAZINES; ANTITUMOR-ACTIVITY; I INHIBITORS; DERIVATIVES; DRUG; HEXAMETHYLMELAMINE; CAMPTOTHECINS
- 제목
- Discovery of ortho-Carborane-Conjugated Triazines as Selective Topoisomerase I/II Inhibitors
- 저자
- Nakamura, Hiroyuki; Shoji, Atsushi; Takeuchi, Ayano; Ban, Hyun Seung; Lee, Jong-Dae; Yamori, Takao; Kang, Sang Ook
- DOI
- 10.1071/CH11295
- 발행일
- 2011
- 유형
- Article
- 권
- 64
- 호
- 11
- 페이지
- 1430 ~ 1437