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Pregled bibliografske jedinice broj: 326202

Novel C-6 Fluorinated Acyclic Side Chain Pyrimidine Derivatives: Synthesis, 1H and 13C NMR Conformational Studies, Antiviral and Cytostatic Evaluations

Prekupec, Svjetlana; Makuc, Damjan; Plavec, Janez; Šuman, Lidija; Kralj, Marijeta; Pavelić, Krešimir; Balzarini, Jan; De Clercq, Erik; Mintas, Mladen; Raić-Malić, Silvana
Novel C-6 Fluorinated Acyclic Side Chain Pyrimidine Derivatives: Synthesis, 1H and 13C NMR Conformational Studies, Antiviral and Cytostatic Evaluations // III Simposio Internacional de Quimica / P. Garciga (ur.).
Santa Clara (CA): Facultad de Química y Farmacia, Universidad Central, 2007. (poster, međunarodna recenzija, sažetak, znanstveni)

CROSBI ID: 326202 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Novel C-6 Fluorinated Acyclic Side Chain Pyrimidine Derivatives: Synthesis, 1H and 13C NMR Conformational Studies, Antiviral and Cytostatic Evaluations

Autori
Prekupec, Svjetlana ; Makuc, Damjan ; Plavec, Janez ; Šuman, Lidija ; Kralj, Marijeta ; Pavelić, Krešimir ; Balzarini, Jan ; De Clercq, Erik ; Mintas, Mladen ; Raić-Malić, Silvana

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

Izvornik
III Simposio Internacional de Quimica / P. Garciga - Santa Clara (CA) : Facultad de Química y Farmacia, Universidad Central, 2007

Skup
III International Symposium On Chemistry

Mjesto i datum
Santa Clara, Kuba, 05.06.2007. - 08.06.2007

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
C-6 fluorinated pyrimidine derivatives; 1H and 13C NMR conformational studies; antiviral and aytostatic evaluations

Sažetak
The synthetic route for introduction of a fluoroalkyl (7-12, 14), fluoroalkenyl (16 and 17), fluorophenylalkyl (18, 20, 21 and 23) and fluorophenylalkenyl (19, 22) side chain at C-6 of the pyrimidine involved the lithiation of the pyrimidine derivatives 3 and 3a and subsequent nucleophilic addition or substitution reactions of the organolithium intermediate thus obtained with various electrophiles (Figure).1 Conformational properties of the novel fluorinated pyrimidine derivatives were assessed by the use of 1D difference NOE enhancements and C-F coupling constants. The novel compounds were evaluated for their antiviral and cytostatic activities. Of all compounds evaluated, the 5-bromopyrimidine derivatives 5 and 6 showed the highest inhibitory activities. Among the series of fluoroalkylated pyrimidines that is generally more active than the series of fluorophenylalkylated pyrimidines, compounds 8 and 14 displayed moderate cytostatic activities against the tested tumor cell lines. Compounds 6, 8 and 15a are worth considering for further development because they afforded a limited specific activity against varicella zoster virus (VZV) and cytomegalovirus (CMV) at a  10-fold lower concentration than that required for cytotoxicity. 1. Raić-Malić, S., et al., Nucl. Nucl. & Nucl. Acids 2004, 23, 1707 ; Johayem, A., Raić-Malić, S., et al., Chemistry&Biodiversity 2006, 3, 274 ; Prekupec, S., Raić-Malić, S., et al., Antiviral Chem. & Chemother. 2005, 16, 327.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti



POVEZANOST RADA

Projekti:
098-0982464-2393 - Molekularna obilježja miofibroblasta Dupuytrenove bolesti
098-0982464-2514 - Uloga različitih mehanizama odgovora stanica na terapiju oštećenjem DNA (Kralj, Marijeta, MZOS ) ( CroRIS)
125-0982464-2922 - RAZVOJ NOVIH PROLIJEKOVA I LIJEKOVA PROTIV VIRUSA I RAKA (Mintas, Mladen, MZOS ) ( CroRIS)
125-0982464-2925 - Razvoj i primjena novih molekula u pozitron-emisijskoj tomografiji (PET) (Raić-Malić, Silvana, MZOS ) ( CroRIS)

Ustanove:
Institut "Ruđer Bošković", Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb

Profili:

Avatar Url Krešimir Pavelić (autor)

Avatar Url Lidija Šuman (autor)

Avatar Url Mladen Mintas (autor)

Avatar Url Svjetlana Krištafor (autor)

Avatar Url Marijeta Kralj (autor)

Avatar Url Silvana Raić-Malić (autor)

Citiraj ovu publikaciju:

Prekupec, Svjetlana; Makuc, Damjan; Plavec, Janez; Šuman, Lidija; Kralj, Marijeta; Pavelić, Krešimir; Balzarini, Jan; De Clercq, Erik; Mintas, Mladen; Raić-Malić, Silvana
Novel C-6 Fluorinated Acyclic Side Chain Pyrimidine Derivatives: Synthesis, 1H and 13C NMR Conformational Studies, Antiviral and Cytostatic Evaluations // III Simposio Internacional de Quimica / P. Garciga (ur.).
Santa Clara (CA): Facultad de Química y Farmacia, Universidad Central, 2007. (poster, međunarodna recenzija, sažetak, znanstveni)
Prekupec, S., Makuc, D., Plavec, J., Šuman, L., Kralj, M., Pavelić, K., Balzarini, J., De Clercq, E., Mintas, M. & Raić-Malić, S. (2007) Novel C-6 Fluorinated Acyclic Side Chain Pyrimidine Derivatives: Synthesis, 1H and 13C NMR Conformational Studies, Antiviral and Cytostatic Evaluations. U: P. Garciga (ur.)III Simposio Internacional de Quimica.
@article{article, author = {Prekupec, Svjetlana and Makuc, Damjan and Plavec, Janez and \v{S}uman, Lidija and Kralj, Marijeta and Paveli\'{c}, Kre\v{s}imir and Balzarini, Jan and De Clercq, Erik and Mintas, Mladen and Rai\'{c}-Mali\'{c}, Silvana}, year = {2007}, pages = {AP44}, keywords = {C-6 fluorinated pyrimidine derivatives, 1H and 13C NMR conformational studies, antiviral and aytostatic evaluations}, title = {Novel C-6 Fluorinated Acyclic Side Chain Pyrimidine Derivatives: Synthesis, 1H and 13C NMR Conformational Studies, Antiviral and Cytostatic Evaluations}, keyword = {C-6 fluorinated pyrimidine derivatives, 1H and 13C NMR conformational studies, antiviral and aytostatic evaluations}, publisher = {Facultad de Qu\'{\i}mica y Farmacia, Universidad Central}, publisherplace = {Santa Clara, Kuba} }
@article{article, author = {Prekupec, Svjetlana and Makuc, Damjan and Plavec, Janez and \v{S}uman, Lidija and Kralj, Marijeta and Paveli\'{c}, Kre\v{s}imir and Balzarini, Jan and De Clercq, Erik and Mintas, Mladen and Rai\'{c}-Mali\'{c}, Silvana}, year = {2007}, pages = {AP44}, keywords = {C-6 fluorinated pyrimidine derivatives, 1H and 13C NMR conformational studies, antiviral and aytostatic evaluations}, title = {Novel C-6 Fluorinated Acyclic Side Chain Pyrimidine Derivatives: Synthesis, 1H and 13C NMR Conformational Studies, Antiviral and Cytostatic Evaluations}, keyword = {C-6 fluorinated pyrimidine derivatives, 1H and 13C NMR conformational studies, antiviral and aytostatic evaluations}, publisher = {Facultad de Qu\'{\i}mica y Farmacia, Universidad Central}, publisherplace = {Santa Clara, Kuba} }

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