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Current Cancer Therapy Reviews


ISSN (Print): 1573-3947
ISSN (Online): 1875-6301

Research Article

In Silico Study and Cytotoxicity of the Synthesized Open-chain Analogues of Antimycin A3 Against HEP-2 Laryngeal Cancer Cells

Author(s): Ade Arsianti*, Fadilah Fadilah, Kusmardi Kusmardi, Gede Y. Sugiarta, Hiroki Tanimoto and Kiyomi Kakiuchi

Volume 13, Issue 2, 2017

Page: [129 - 136] Pages: 8

DOI: 10.2174/1573394713666170712113049

open access plus


Background: Laryngeal cancers affect one quarter of all head and neck cancers. Chemotherapy is a standard method in treatment laryngeal carcinoma. However, cancer chemotherapy is often a failure due to the appearance of drug resistance. This fact suggests that the search for novel, safe, and more effective laryngeal cancer drugs are required. Antimycin A3 is a fit ligand of anti-apoptotic Bcl-2. While Bcl-2 is known to be over-expressed in laryngeal cancer cell, it is quite reasonable to expect antimycin A3 and its analogue to induce apoptosis in those cells.

Methods: With this viewpoint, we decided to conduct research that is aimed to evaluate cytotoxic activity of the synthesized open-chain analogues of antimycin A3 against HEP-2 laryngeal cancer cells, as well as to conduct in silico study of the analogues on receptor binding target Bcl-2 of laryngeal cancer.

Results and Conclusion: Open-chain analogues of antimycin A3 were successfully synthesized in a good yield from Boc-L-Threonine by esterification, amidation, and Sharpless asymmetric dihydroxylation.

Consistent with in silico study, the analogues exhibited a greater anticancer activity against laryngeal HEP-2 cells than the original antimycin A3 with IC50 ranging of 31.6 µM to 46.3 µM. Our results clearly demonstrate that the open-chain analogues of antimycin A3 as a promising candidates of new anti-laryngeal cancer agents.

Keywords: Synthesis, in silico, cytotoxicity, opened-chain analogue, antimycin A3, HEP-2, laryngeal cancer.

Graphical Abstract

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