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Synthesis, antitumor activity and crystal structure of novel benzofuran-2-carboxanilides


Hranjec, Marijana; Sović, Irena; Ratkaj, Ivana; Kraljević Pavelić, Sandra; Pavlović, Gordana; Pavelić, Krešimir; Karminski-Zamola, Grace
Synthesis, antitumor activity and crystal structure of novel benzofuran-2-carboxanilides // International Symposium on Advances in Synthetic and Medicinal Chemistry : Abstracts / Nicolaou, K.C. (ur.).
St. Petersburg, 2011. str. 179-179 (poster, međunarodna recenzija, sažetak, znanstveni)


Naslov
Synthesis, antitumor activity and crystal structure of novel benzofuran-2-carboxanilides

Autori
Hranjec, Marijana ; Sović, Irena ; Ratkaj, Ivana ; Kraljević Pavelić, Sandra ; Pavlović, Gordana ; Pavelić, Krešimir ; Karminski-Zamola, Grace

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

Izvornik
International Symposium on Advances in Synthetic and Medicinal Chemistry : Abstracts / Nicolaou, K.C. - St. Petersburg, 2011, 179-179

Skup
International Symposium on Advances in Synthetic and Medicinal Chemistry

Mjesto i datum
St. Petersburg, Rusija, 21.-25.08.2011

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
Benzofuran-2-carboxanilides; amidines; antitumor activity; crystal structure

Sažetak
Since classical chemotherapy which uses small molecules or bioactive natural products is still the mainstay of cancer treatment, there has been tremendous growth in recent years in the number and types of new anticancer agents. Substituted heterocyclic amides exhibit wide range of pharmacological activities and have therefore attracted considerable attention from medicinal and synthetic organic chemists. We have previously reported synthesis and strong inhibitory activities on several human tumour cell lines of various amidino substituted benzobthiophene-2-carboxamides and benzo[b]thieno[2, 3-c]quionolones while it is well known that amidines are structural parts of numerous compounds of biological interest as various medical and biochemical agents. As a part of our continuing search for potential anticancer agents related to heterocyclic amides, we have synthesized novel cyano, nitro, acetamido, N, N-dimethylamino and 2-imidazolinyl substituted benzofuran-2-carboxanilides using classical linear and convergent organic synthesis reactions. Structures of prepared compounds were confirmed by means of 1H, 13C NMR, IR and UV spectroscopy. Crystal and molecular structures of two compounds were determined by X-ray diffractometry. All compounds were tested on their antitumor activity on human tumour cell lines, as well as on normal (diploid) human fibroblasts (control cell line). The in vitro screening revealed a rather strong and non-specific cytotoxic effect of all tested compounds. Some compounds exerted a highly selective concentration-dependent antiproliferative effects on certain cell lines and are thus suitable for further studies. References [1] Jarak I. ; Kralj, M. ; Šuman, L. ; Pavlović, G. ; Dogan J. ; Piantanida, I. ; Žinić, M. Pavelić, K. ; Karminski-Zamola, G. J. Med. Chem. 48 (2005) 2346-2360. [2] Ester, K. ; Hranjec, M. ; Piantanida, I. ; Ćaleta, I. ; Jarak, I. ; Pavelić, K. ; Kralj, M. ; Karminski-Zamola, G. J. Med. Chem. 52 (2009) 2482-2492. [3] Hranjec, M. ; Kralj, M. ; Piantanida, I. ; Sedić, M. ; Šuman, L. ; Pavelić, K. ; Karminski-Zamola, G. J. Med. Chem. 50 (2007) 5696-5711.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
09-1191344-2943
125-0982464-1356 - Novi heterocikli kao antitumorski i antivirusni ("pametni") lijekovi (Marijana Hranjec, )
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