Pregled bibliografske jedinice broj: 446631
Pyrazolone-fused combretastatins and their precursors : synthesis, cytotoxicity, antitubulin activity and molecular modeling studies
Pyrazolone-fused combretastatins and their precursors : synthesis, cytotoxicity, antitubulin activity and molecular modeling studies // Bioorganic & medicinal chemistry, 18 (2010), 7; 2375-2387 doi:10.1016/j.bmc.2010.03.006 (međunarodna recenzija, članak, znanstveni)
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Naslov
Pyrazolone-fused combretastatins and their precursors : synthesis, cytotoxicity, antitubulin activity and molecular modeling studies
Autori
Burja, Bojan ; Čimbora-Zovko, Tamara ; Tomić, Sanja ; Jelušić, Tihana ; Kočevar, Marijan ; Polanc, Slovenko ; Osmak, Maja
Izvornik
Bioorganic & medicinal chemistry (0968-0896) 18
(2010), 7;
2375-2387
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni
Ključne riječi
Combretastatin CA-4 derivatives ; Cytotoxicity ; Tubulin ; Molecular modeling
Sažetak
A series of pyrazolone-fused combretastatins and precursors were synthesized and their cytotoxicity as well as antitubulin potential was evaluated. The hydrazide 9f and the pyrazolone-fused combreta¬statins 12a, 12b and 12c were highly cytotoxic against various tumor cell lines including cisplatin resistant cells. The same compounds were also the best inhibitors of tubulin polymerization. Molecular modeling results showed that they bind the colchicine binding site at the tubulin heterodimer. The hydrazide 9f arrested HeLa cells in the G2/M phase of the cell cycle and strongly affected cell shape and microtubule network.
Izvorni jezik
Engleski
Znanstvena područja
Fizika, Kemija, Biologija
POVEZANOST RADA
Projekti:
098-0982913-2748 - Stanični odgovor na citotoksične spojeve i razvoj otpornosti (Osmak, Maja, MZOS ) ( CroRIS)
098-0982913-2850 - Povećanje transdukcije adenovirusnih vektora i otpornost stanica na citostatike (Ambriović Ristov, Andreja, MZOS ) ( CroRIS)
098-1191344-2860 - Proučavanje biomakromolekula računalnim metodama i razvoj novih algoritama (Tomić, Sanja, MZOS ) ( CroRIS)
Ustanove:
Institut "Ruđer Bošković", Zagreb
Citiraj ovu publikaciju:
Časopis indeksira:
- Current Contents Connect (CCC)
- Web of Science Core Collection (WoSCC)
- Science Citation Index Expanded (SCI-EXP)
- SCI-EXP, SSCI i/ili A&HCI
- Scopus
- MEDLINE