Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline Derivatives
α-Carboline (pyrido[2,3-b]indole) was selected as the basic scaffold for development of antileukemic agents by structural modification. From the structure-activity study, it was found that sequential introduction of 6-acetyl and 9-substituted benzyl groups onto an α-Carboline scaffold resulted in 6-...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Wiley
2010-11-01
|
| Series: | Kaohsiung Journal of Medical Sciences |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1607551X10700917 |
| _version_ | 1818683021779271680 |
|---|---|
| author | Jui-Ying Tsai Yi-Chien Lin Mei-Hua Hsu Sheng-Chu Kuo Li-Jiau Huang |
| author_facet | Jui-Ying Tsai Yi-Chien Lin Mei-Hua Hsu Sheng-Chu Kuo Li-Jiau Huang |
| author_sort | Jui-Ying Tsai |
| collection | DOAJ |
| description | α-Carboline (pyrido[2,3-b]indole) was selected as the basic scaffold for development of antileukemic agents by structural modification. From the structure-activity study, it was found that sequential introduction of 6-acetyl and 9-substituted benzyl groups onto an α-Carboline scaffold resulted in 6-acetyl-9-(3,5-dimethoxybenzyl)-9H-pyrido[2,3-b]indole and 6-acetyl-9-(3,4,5-trimethoxybenzyl)-9H-pyrido[2,3-b]indole with potent cytotoxicity against the HL-60 cell line. These two compounds will be used as new lead compounds for further investigation. |
| first_indexed | 2024-12-17T10:28:07Z |
| format | Article |
| id | doaj.art-aa9f567099a945c493c6d3cb7de8241e |
| institution | Directory Open Access Journal |
| issn | 1607-551X |
| language | English |
| last_indexed | 2024-12-17T10:28:07Z |
| publishDate | 2010-11-01 |
| publisher | Wiley |
| record_format | Article |
| series | Kaohsiung Journal of Medical Sciences |
| spelling | doaj.art-aa9f567099a945c493c6d3cb7de8241e2022-12-21T21:52:35ZengWileyKaohsiung Journal of Medical Sciences1607-551X2010-11-01261159360210.1016/S1607-551X(10)70091-7Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline DerivativesJui-Ying TsaiYi-Chien LinMei-Hua HsuSheng-Chu KuoLi-Jiau Huangα-Carboline (pyrido[2,3-b]indole) was selected as the basic scaffold for development of antileukemic agents by structural modification. From the structure-activity study, it was found that sequential introduction of 6-acetyl and 9-substituted benzyl groups onto an α-Carboline scaffold resulted in 6-acetyl-9-(3,5-dimethoxybenzyl)-9H-pyrido[2,3-b]indole and 6-acetyl-9-(3,4,5-trimethoxybenzyl)-9H-pyrido[2,3-b]indole with potent cytotoxicity against the HL-60 cell line. These two compounds will be used as new lead compounds for further investigation.http://www.sciencedirect.com/science/article/pii/S1607551X10700917antileukemic agentsα-CarbolineHL-60 cellsstructure-activity relationships |
| spellingShingle | Jui-Ying Tsai Yi-Chien Lin Mei-Hua Hsu Sheng-Chu Kuo Li-Jiau Huang Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline Derivatives Kaohsiung Journal of Medical Sciences antileukemic agents α-Carboline HL-60 cells structure-activity relationships |
| title | Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline Derivatives |
| title_full | Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline Derivatives |
| title_fullStr | Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline Derivatives |
| title_full_unstemmed | Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline Derivatives |
| title_short | Synthesis and Cytotoxicity of 1,6,8,9-Substituted α-Carboline Derivatives |
| title_sort | synthesis and cytotoxicity of 1 6 8 9 substituted α carboline derivatives |
| topic | antileukemic agents α-Carboline HL-60 cells structure-activity relationships |
| url | http://www.sciencedirect.com/science/article/pii/S1607551X10700917 |
| work_keys_str_mv | AT juiyingtsai synthesisandcytotoxicityof1689substitutedacarbolinederivatives AT yichienlin synthesisandcytotoxicityof1689substitutedacarbolinederivatives AT meihuahsu synthesisandcytotoxicityof1689substitutedacarbolinederivatives AT shengchukuo synthesisandcytotoxicityof1689substitutedacarbolinederivatives AT lijiauhuang synthesisandcytotoxicityof1689substitutedacarbolinederivatives |