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Discovery of ortho-Carborane-Conjugated Triazines as Selective Topoisomerase I/II Inhibitors
- Authors
- Nakamura, Hiroyuki; Shoji, Atsushi; Takeuchi, Ayano; Ban, Hyun Seung; Lee, Jong-Dae; Yamori, Takao; Kang, Sang Ook
- Issue Date
- 2011
- Publisher
- CSIRO PUBLISHING
- Citation
- AUSTRALIAN JOURNAL OF CHEMISTRY, v.64, no.11, pp.1430 - 1437
- Indexed
- SCIE
SCOPUS
- Journal Title
- AUSTRALIAN JOURNAL OF CHEMISTRY
- Volume
- 64
- Number
- 11
- Start Page
- 1430
- End Page
- 1437
- ISSN
- 0004-9425
- Abstract
- 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.
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Collections - Graduate School > Department of Advanced Materials Chemistry > 1. Journal Articles
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