Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives
The focus of this study has been to investigate the in vitro cytotoxic effects of new β-carboline derivatives on the K562 human cancer cell line. Analysis using 3D-QSAR models has revealed the importance of derivatisation at position-2 and -9 of the β-carbolines. Two new series of N2-benzylated-β-ca...
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| Format: | Thesis |
| Language: | English |
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2018
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| Online Access: | http://eprints.usm.my/43676/1/MAZLIN%20MOHIDEEN.pdf |
| _version_ | 1797011049903292416 |
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| author | Mohideen, Mazlin |
| author_facet | Mohideen, Mazlin |
| author_sort | Mohideen, Mazlin |
| collection | USM |
| description | The focus of this study has been to investigate the in vitro cytotoxic effects of new β-carboline derivatives on the K562 human cancer cell line. Analysis using 3D-QSAR models has revealed the importance of derivatisation at position-2 and -9 of the β-carbolines. Two new series of N2-benzylated-β-carboline (M23-M46) and N2-N9-benzylated-1-substituted-β-carboline derivatives (M47-M113) were synthesised and characterised using four-step reaction and were produced in good yields (>70%). Compounds M23-M113 exhibited the most potent anticancer activity with IC50 values between 0.01-4 μM, except for compounds M88-M90 which produced IC50 values of more than 100 μM. |
| first_indexed | 2024-03-06T15:28:38Z |
| format | Thesis |
| id | usm.eprints-43676 |
| institution | Universiti Sains Malaysia |
| language | English |
| last_indexed | 2024-03-06T15:28:38Z |
| publishDate | 2018 |
| record_format | dspace |
| spelling | usm.eprints-436762019-04-12T05:24:50Z http://eprints.usm.my/43676/ Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives Mohideen, Mazlin RS200-201 Pharmaceutical dosage forms The focus of this study has been to investigate the in vitro cytotoxic effects of new β-carboline derivatives on the K562 human cancer cell line. Analysis using 3D-QSAR models has revealed the importance of derivatisation at position-2 and -9 of the β-carbolines. Two new series of N2-benzylated-β-carboline (M23-M46) and N2-N9-benzylated-1-substituted-β-carboline derivatives (M47-M113) were synthesised and characterised using four-step reaction and were produced in good yields (>70%). Compounds M23-M113 exhibited the most potent anticancer activity with IC50 values between 0.01-4 μM, except for compounds M88-M90 which produced IC50 values of more than 100 μM. 2018-06 Thesis NonPeerReviewed application/pdf en http://eprints.usm.my/43676/1/MAZLIN%20MOHIDEEN.pdf Mohideen, Mazlin (2018) Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives. PhD thesis, Universiti Sains Malaysia. |
| spellingShingle | RS200-201 Pharmaceutical dosage forms Mohideen, Mazlin Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives |
| title | Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives |
| title_full | Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives |
| title_fullStr | Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives |
| title_full_unstemmed | Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives |
| title_short | Design, Synthesis, Cytotoxic Activity And DNA Intercalation Of New β-Carboline Derivatives |
| title_sort | design synthesis cytotoxic activity and dna intercalation of new β carboline derivatives |
| topic | RS200-201 Pharmaceutical dosage forms |
| url | http://eprints.usm.my/43676/1/MAZLIN%20MOHIDEEN.pdf |
| work_keys_str_mv | AT mohideenmazlin designsynthesiscytotoxicactivityanddnaintercalationofnewbcarbolinederivatives |