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Advanced Pharmaceutical Bulletin
ISSN: 2228-5881      eISSN: 2251-7308  
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Article History
Submitted: 05 Sep 2012
Revised: 07 Oct 2012
First published online: 07 Feb 2013

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Adv Pharm Bull. 2013;3(1):73-77 doi: 10.5681/apb.2013.012
PMID:24312815        PMCID:PMC3846042

Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines

Original Research

Saeed Ghasemi, Soodabeh Davaran, Simin Sharifi, Davoud asgari, Ali Abdollahi, Javid Shahbazi Mojarrad *


Abstract
Purpose: Farnesyltransferase (FTase) is a zinc-dependent enzyme that adds a farnesyl group to the Ras proteins. L778, 123 is a potent peptidomimetic imidazole-containing FTase inhibitor. Methods: L778123 was synthesized according to known methods and evaluated alone and in combination with doxorubicin against A549 (adenocarcinomic human alveolar basal epithelial cells) and HT29 (human colonic adenocarcinoma) cell lines by MTT assay. Results: L778123 showed weak cytotoxic activity with IC50 of 100 and 125 for A549 and HT-29 cell lines, respectively. The combination of doxorubicin and L778123 can decrease IC50 of doxorubicin in both cell lines significantly. Conclusion: It can be concluded that L778, 123 can be a good agent for combination therapy.





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