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Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives

Gazivoda Kraljević, Tatjana; Klika, Mateja; Kralj, Marijeta; Martin-Kleiner, Irena; Jurmanović, Stella; Milić, Astrid; Padovan, Jasna; Raić-Malić, Silvana (2012) Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives. Bioorganic and Medicinal Chemistry Letters, 22 (1). pp. 308-312. ISSN 0960-894X

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Abstract

The synthesis of the novel 5-alkyl pyrimidine derivatives, 5, 6-dihydrofuro[2, 3-d]pyrimidines and 5-alkyl N-methoxymethyl pyrimidine derivatives and evaluation of their cytostatic activities are described. The mechanism of antiproliferative effect of 5-(2-chloroethyl)-substituted pyrimidine 3 that exerted the pronounced cytostatic activity was studied in further details on colon carcinoma (HCT116) cells. The cell cycle perturbation analysis demonstrated severe DNA damage (G2/M arrest) pointing to a potential DNA alkylating ability of 3. Preliminary ADME data of 3 and its 6-methylated structural congener (6-Me-3) showed their high permeability and good metabolic stability.

Item Type: Article
Uncontrolled Keywords: 5-alkyl pyrimidine derivatives; cytostatic evaluations; cell cycle analysis; ADME properties
Subjects: NATURAL SCIENCES > Chemistry
Divisions: Division of Molecular Medicine
Projects:
Project titleProject leaderProject codeProject type
Razvoj i primjena novih molekula u pozitron-emisijskoj tomografiji (PET)-Silvana Raić-Malić125-0982464-2925MZOS
Uloga različitih mehanizama odgovora stanica na terapiju oštećenjem DNA-Marijeta Kralj098-0982464-2514MZOS
Depositing User: Irena Martin Kleiner
Date Deposited: 21 Dec 2016 13:27
Last Modified: 01 Feb 2017 14:28
URI: http://fulir.irb.hr/id/eprint/1976
DOI: 10.1016/j.bmcl.2011.11.009

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