臺灣博碩士論文加值系統

Hydrazonoyl hydrochlorides與碳二亞胺 (carbodiimides) 在三乙胺 (triethylamine) 作為鹼性條件下經由1,3-dipolar 環化反應成功地合成出5-amino-1,2,4-triazoles。除了diphenyl carbodiimide其他飽和烷基皆能適用於新開發之1,3-dipolar環化反應。將所有5-amino-1,2,4-triazoles進行體外人類腫瘤細胞抑制活性之藥理活性測試，腫瘤細胞包括肺癌 (NCI-H266)、鼻咽癌 (NCP-TW01)與T-細胞白血病(Jurkat)。經由上列所述三株細胞所測得IC50藥理活性，其效果皆不佳。

An effective 1,3-dipolar cycloaddition was successfully developed for synthesis 5-amino-1,2,4-triazoles by reacting hydrazonoyl hydrochlorides (nitrilimines) with carbodiimides in the presence of triethylamine as a base catalyst. Carbodiimides can be adapted to the newly developed reaction condition, except for diphenyl carbodiimide. All of 5-Amino-1,2,4-triazoles were evaluated against a panel of human cancer cell lines in vitro, including lung carcinoma (NCI-H226), nasopharyngeal (NPC-TW01), and T-cell leukemia (Jurkat) cells. Based on the IC50, result, most of them provided the poor inhibitory potency.

Abbreviations..... I
Chart of Figure... IV
Chart of Scheme... VIII
Chart of Table.... IX
Chapter 1. Introduction.....1
Section 1.1 Bioactivity of 1,2,4-triazoles derivatives....1
Section 1.1.1 1,2,4-Triazoles derivatives as glycine transporter 1 inhibitors....2
Section 1.1.2 1,2,4-Triazoles derivatives were evaluated on antimicrobial activity..... 3
Section 1.2 Chemistry...... 4
Section 1.2.1 Chemistry of 1,2,4-triazoles....4
Section 1.2.2 Chemistry of Carbodiimides......7
Section 1.2.3 Chemistry of hydrazonoyl hydrochlorides..8
Chapter 2. Research Approach.........9
Chapter 3. Results & Discussion......11
Section 3.1 Chemistry.......11
Section 3.2 Inhibitory activities of 5-amino-1,2,4-triazoles......... 21
Chapter 4. Conclusion...... 24
Chapter 5. Experimental Section..... 27
Section 5.1 General Procedure....... 27
Section 5.2 Spectrum....... 29
Section 5.3 Cell lines..... 39
Section 5.4 Growth inhibition assay.....40
Reference .....41
Appendix.....52

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