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Pregled bibliografske jedinice broj: 446631

Pyrazolone-fused combretastatins and their precursors : synthesis, cytotoxicity, antitubulin activity and molecular modeling studies


Burja, Bojan; Čimbora-Zovko, Tamara; Tomić, Sanja; Jelušić, Tihana; Kočevar, Marijan; Polanc, Slovenko; Osmak, Maja
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)


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


Projekt / tema
098-0982913-2748 - Stanični odgovor na citotoksične spojeve i razvoj otpornosti (Maja Osmak, )
098-0982913-2850 - Povećanje transdukcije adenovirusnih vektora i otpornost stanica na citostatike (Andreja Ambriović Ristov, )
098-1191344-2860 - Proučavanje biomakromolekula računalnim metodama i razvoj novih algoritama (Sanja Tomić, )

Ustanove
Institut "Ruđer Bošković", Zagreb

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


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