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Pregled bibliografske jedinice broj: 803581

The novel coumarin[3, 2-c]thiophene and its hydroxamic acid and ureido derivatives : synthesis and cytostatic activity evaluations


Wittine, Karlo; Ratkaj, Ivana; Benci, Krešimir; Suhina, Tomislav; Mandić, Leo; Ilić, Nataša; Kraljević Pavelić, Sandra; Pavelić, Krešimir; Mintas, Mladen
The novel coumarin[3, 2-c]thiophene and its hydroxamic acid and ureido derivatives : synthesis and cytostatic activity evaluations // Medicinal chemistry research, 25 (2016), 4; 728-737 doi:10.1007/s00044-016-1523-0 (međunarodna recenzija, članak, znanstveni)


Naslov
The novel coumarin[3, 2-c]thiophene and its hydroxamic acid and ureido derivatives : synthesis and cytostatic activity evaluations

Autori
Wittine, Karlo ; Ratkaj, Ivana ; Benci, Krešimir ; Suhina, Tomislav ; Mandić, Leo ; Ilić, Nataša ; Kraljević Pavelić, Sandra ; Pavelić, Krešimir ; Mintas, Mladen

Izvornik
Medicinal chemistry research (1054-2523) 25 (2016), 4; 728-737

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Coumarin[3; 2-c]thiophene; urea; hydroxamic acid; antitumour

Sažetak
In the present paper, we report on the synthesis and in vitro anti-tumour effects of novel hydroxamic acid (compounds 4 and 5) and ureido (compounds 7-11) derivatives containing coumarin[3, 2-c]thiophene moiety. The results of anti-proliferative assays performed on a panel of selected human tumour cell lines revealed stronger concentration-dependent anti-proliferative activity of coumarin[3, 2-c]thiophene (7-11) ureido derivatives in comparison with coumarin[3, 2-c]thiophene hydroxamic acid derivatives (4 and 5). Nevertheless, compounds 7-10 were cytotoxic on normal human fibroblasts as well. Importantly, the ureido derivative 11 and hydroxamic acid derivatives 4 and 5 showed pronounced and selective inhibitory activity towards cervical carcinoma (HeLa) cell line with concomitant low or no cytotoxicity on normal human fibroblasts. These compounds can therefore be considered as potential anti-tumour lead compounds for further structural optimization.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biotehnologija



POVEZANOST RADA


Projekt / tema
125-0982464-2922 - RAZVOJ NOVIH PROLIJEKOVA I LIJEKOVA PROTIV VIRUSA I RAKA (Mladen Mintas, )
13.11.1.1.11
13.11.1.2.01
335-0000000-3532 - Uloga IGF2 i signalni putovi nizvodno u karcinomima pluća čovjeka (Sandra Kraljević Pavelić, )
335-0982464-2393 - Molekularna obilježja miofibroblasta Dupuytrenove bolesti (Krešimir Pavelić, )

Ustanove
Fakultet kemijskog inženjerstva i tehnologije, Zagreb,
Sveučilište u Rijeci - Odjel za biotehnologiju

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


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