Sintesis dan uji aktivitas antikanker senyawa 1-(2-klorobenzoiloksi)urea dan 1-(4-klorobenzoiloksi)urea
| Main Author: | Suko Hardjono, |
|---|---|
| Format: | Article PeerReviewed Book |
| Bahasa: | eng |
| Terbitan: |
Fakultas Farmasi Universitas Airlangga
, 2013
|
| Subjects: | |
| Online Access: |
http://repository.unair.ac.id/51551/1/BIKF%20Vol-2%20No-1%202013%20Juni%20Sintesis%20dan%20Uji%20Aktivitas%20Antikanker.cover.pdf http://repository.unair.ac.id/51551/2/download-fullpapers-bikf2cbd804a532full.pdf http://repository.unair.ac.id/51551/12/Bukti%20C-12.pdf http://repository.unair.ac.id/51551/ http://journal.unair.ac.id/sintesis-dan-uji-aktivitas-antikanker-senyawa-1-(2-klorobenzoiloksi)urea-article-6439-media-96-category-15.html |
Daftar Isi:
- 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.