Synthesis of Iodoacetamide Compound Library for Developing Novel Anti-cancer Drugs
Date Issued
2010
Date
2010
Author(s)
Kuo, Wei-Chi
Abstract
ABSTRACT
Previous report has demonstrated the feasibility of targeting β-tubulin around Cys354 by iodoacetamide-Trp to disrupt β-tubulin/CCT-β complex as a new anti-cancer therapy, especially against drug-resistant cancers (Lin et al., Cancer Res. 2009). In the thesis, I have synthesized a series of iodoacetamides to investigate their structure-activity relationship of the cell apoptotic effect. The compounds were synthesized via the modified pathway from the reaction of starting materials containing free amino group with chloro-acetate to form a series of chloroacetamide compounds, followed by reaction with sodium iodine to form the final adducts. The compounds were evaluated for their cell apoptotic effect. Their binding ability with β-tubulin was predicted by computer modeling to rationalize their SAR against cells. The computer modeling revealed similar binding modes and affinity of these compounds with β-tubulin, and they also caused similar apoptotic effect against the HEK-293 cells.
Subjects
iodoacetamide
SDGs
Type
thesis
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