Naslov
New heterocyclic bis(phenylamidines)and their cytotoxic effect on solid tumor cell lines

Autori
Mišković, Katarina ; Stolić, Ivana ; Bajić, Miroslav ; Baus Lončar, Mirela ; Glavaš-Obrovac, Ljubica

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Abstracts of the Congress of the Croatian Society of Biochemistry and Molecular Biology with international participation / - , 2008

Skup
Congress of the Croatian Society of Biochemistry and Molecular Biology with international participation

Mjesto i datum
Osijek, Hrvatska, 17.09.2008. - 20.09.2008

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
bis(phenylamidines) derivatives; cytotoxic; Hoechst 33258; solid tumor

Sažetak
Constant need for more effective and less harmful anticancer drugs leads to intensive synthesis of novel small organic molecules with potential antitumor activity. We tested antiproliferative activity of new synthesized dicationic bis(phenylamidine) derivatives: 2, 5-bis(4-amidinophenyl)-3, 4-ethylenedioxythiophene dihydrochloride (MB-17), 2, 5-bis[4-(N-isopropylamidino)phenyl)]-3, 4- ethylenedioxythiophene dihydrochloride (MB-18) and 2, 5-bis[4-(2-imidazolino)phenyl]- 3, 4-ethylenedioxythiophene dihydrochloride (MB-19) on 7 solid tumor cell lines (MCF-7, NCI-H358, CaCo-2, HEp-2, HeLa, AGS, MiaPaCa) by colorimetric MTT assay. The cytotoxic effect of novel compounds was compared with DNA minor groove binder and antitumor drug Hoechst 33258 (2’ -(4-hydroxyphenyle)-5-(4-methyl-1-piperazinyl)-2, 5’ -bi(1H-benzimidazole) trihydrochloride). All three compounds were effective on tested cell lines in 10-4 M concentration. MB 17 and MB 18 compounds showed similar antiproliferative effect on MCF-7, HEp-2 and MiaPaCa in 10-5 M concentration suppressing cell growth approximately 50% compared to control. The best antiproliferative activity was exhibited by MB 19 at 10-5 M concentration showing more then 80% growth reduction for 6 tested cell lines. An exception was MiaPaCa cell line with 60% growth reduction compared to control. MB 19 has higher antiproliferative activity on tested cell lines compared with Hoechst 33258. As MB 19 is a fluorochrom its entrance into the cell was monitored by fluorescent microscopy. MB 19 enters the cell and localises in nucleus similar as Hoechst 33258. The mechanism of MB 19 still remains to be elucidated.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, Temeljne medicinske znanosti

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