UNIVERSITAS AIRLANGGA



Detail Article

Berkala Ilmiah Kimia Farmasi

ISSN 2302-8270

Vol. 2 / No. 1 / Published : 2013-06

Order : 3, and page :16 - 21

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Original Article :

Sintesis dan uji aktivitas antikanker senyawa 1-(2-klorobenzoiloksi)urea dan 1-(4-klorobenzoiloksi)urea

Author :

  1. Suko Hardjono*1
  1. Dosen Fakultas Farmasi

Abstract :

Hydroxyurea or (HU) is a compound that has antineoplastic activity through a mechanism of inhibiting ribonucleotide reductase enzyme. To design new drugs, the physicochemical properties of drug molecules can be predicted before they are synthesized and purified. In silico test is a method to predict the activity of the compound to be synthesized. Ribonucleotide reductase was the main target or receptor of anticancer compounds such as HU and their derivatives, namely  1-(2-chlorobenzoyl-oxy)urea or 2-ClBOU and 1-(4-chlorobenzoyloxy)urea or 4-ClBOU. These compounds formed a complex with crystal structure of ribonucleotide reductase I enzym which was 2EUD. Bond energy in the form of rerank scores from both complexes were calculated with Molegro program. Rerank score score 2-ClBOU -81,1349 and 4-ClBOU -82,7887 while HU - 43.3565. From the results obtained could be predicted that 2-ClBOU and 4-ClBOU have greater anticancer activity than HU. Synthesis of These compounds were performed by reacting hydroxyurea with 2-chlorobenzoyl chloride or 4-chlorobenzoyl chloride. Purity test was by TLC and melting point determination were performed.                                       The structure of compounds were confirmed using data from UV, IR, 1H-NMR, 13C-NMR, and MS/GC-MS spectra. In this study, 2-ClBOU and 4-ClBOU compounds have been succesfully synthesized and after in vitro anticancer activity was tested against HeLa cells, it was obtained             2-ClBOU IC50  94 µg/ml, 4-ClBOU IC50 84 µg/ml while IC50 HU 430 µg/ml. Can be concluded that     2-ClBOU and 4-ClBOU have greater anticancer activity than HU.  

Keyword :

1-(2-chlorobenzoyloxy)urea, 1-(4-chlorobenzoyloxy)urea in silico test, synthesis, anticancer activity test,


References :

Avendano C & Menendes J.C, ,(2008) Medicinal Chemistry of Anticancer Drugs Amsterdam : Elsevier





Archive Article

Cover Media Content

Volume : 2 / No. : 1 / Pub. : 2013-06
  1. Validasi spektrofotometri visible untuk penentuan kadar formalin dalam daging ayam
  2. Validasi metode kromatografi gas-spektrometri massa untuk penetapan kadar residu endosulfan dalam kubis
  3. Sintesis dan uji aktivitas antikanker senyawa 1-(2-klorobenzoiloksi)urea dan 1-(4-klorobenzoiloksi)urea
  4. Pengaruh gugus metoksi posisi orto (o) dan para (p) pada benzaldehida terhadap sintesis turunan khalkon dengan metode kondensasi aldol
  5. Modifikasi struktur n-fenilurea menjadi senyawa baru n-benzoilfenilurea dan 4-fluorobenzoilfenilurea serta uji aktivitasnya sebagai penekan susunan saraf pusat
  6. Aktivitas antinociceptiv dan uji in silico terhadap cyclooxygenase dari asam p-metoksisinamat dan asam m-metoksisinamat
  7. Docking dan modifikasi struktur senyawa baru turunan parasetamol

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