2. Academic Validation
  3. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines

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

  • Adv Pharm Bull. 2013;3(1):73-7. doi: 10.5681/apb.2013.012.
Saeed Ghasemi 1,  Soodabeh Davaran,  Simin Sharifi,  Davoud Asgari,  Ali Abdollahi,  Javid Shahbazi Mojarrad
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
PMID: 24312815 DOI: 10.5681/apb.2013.012
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.

Keywords

Combination therapy; Farnesyltransferase inhibitor; L-778123; MTT assay.

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