Antitumour efficiency of novel fluoro substituted 6-amino-2-phenylbenzothiazole hydrochloride salts in vitro and in vivo (CROSBI ID 123158)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Stojković, Ranko ; Karminski-Zamola, Grace ; Racane, Livio ; Tralić-Kulenović, Vesna ; Glavaš-Obrovac, Ljubica ; Ivanković, Siniša ; Radačić, Marko
engleski
Antitumour efficiency of novel fluoro substituted 6-amino-2-phenylbenzothiazole hydrochloride salts in vitro and in vivo
The purpose of this study was to investigate antitumor activity of novel fluoro-substituted 6-amino-2-phenylbenzothiazole hydrochloride salts in vitro and in vivo. A novel series of hydrochloride or dihydrochloride salts of the novel 2-(fluoro-substituted phenyl)-6-aminobenzothiazoles (5-7) have been prepared in multistep synthesis starting from 3- or 4-fluorobenzaldehydes and 2-amino-5-nitrothiophenol and evaluated for their antiproliferative activity against human cervical (HeLa), breast (MCF-7), colon (CaCO-2), and laryngeal (Hep-2) carcinomas and against fibroblast cell lines (WI-38). Also, antitumor activity of these compounds was evaluated in vitro and in vivo against murine melanoma (B16-F10), fibrosarcoma (FsaR), and squamous cell carcinoma (SCCVII). The tested compounds were found to exert good cytotoxic activity in vitro. The cytotoxic effect was selective, cell specific, and dose dependent, between 33 mcM for MCF-7 and 110 mcM for WI-38. Benzothiazoles reduced de novo protein and DNA synthesis up to 75%. All examined benzothiazoles had significant antitumor activity in vivo against melanoma B16-F10, fibrosarcoma, and squamous cell carcinoma. The best therapeutic results were achieved when therapy started 7 days after tumor cell implantation and when benzothiazoles were given repeatedly five times every 2 days, i.e., on day 7, 9, 11, 13, and 15 after transplantation of tumor cells.
fluoro substituted 6-amino-2-phenyl benzothiazole derivatives; antiproliferative/antitumour activity; in vitro/in vivo
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Podaci o izdanju
28 (6)
2006.
347-354-x
objavljeno
0379-0355
Povezanost rada
Kemija, Temeljne medicinske znanosti, Veterinarska medicina