To investigate one possible mechanism of action of the cytotoxic activity of benzothiazoles, we synthesized 2-(substituted-phenyl)benzothiazoles and evaluated their ability to inhibit topoisomerase 11 activities. Solid phase combinatorial method using trityl resin was employed and benzothiazole derivatives with Various substitution on 2'-, 3'-, or 4'-position of phenyl group were obtained in ca. 30 mg scale (7-96% yield). Most of the compounds synthesized exhibited topoisomerase 11 inhibitory activity at 100 mu M. 2-(3-Amino-4-methylphenyl)benzothiazole showed high activity (IC50 = 71.7 mu M), comparable to etoposide (IC50 = 78.4 mu M). (c) 2005 Elsevier Ltd. All rights reserved.
Synthesis and characterization of new platinum(II) complexes containing thiazole and imidazole donors II. Tribromo(styrylheterazole)platinate(II) anionic complexes
作者:Mariel M. Muir、Grisell M. Gomez、Mayra E. Cadiz、James A. Muir
DOI:10.1016/s0020-1693(00)88016-0
日期:1990.2
Lokhande, S. B.; Rangnekar, D. W., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1986, vol. 25, p. 485 - 488
作者:Lokhande, S. B.、Rangnekar, D. W.
DOI:——
日期:——
Benzoheterazolo[3,2-a]quinolinium salts
申请人:Commonwealth of Puerto Rico
公开号:US04590275A1
公开(公告)日:1986-05-20
The preparation of the hitherto unknown benzoheterazolo[3,2-a]quinolinium salts via, the photochemically induced cyclization of 2-chlorostyrylbenzoheterazoles is described. The new products show cytotoxic, antitumor and antiviral activity.