Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues
Resveratrol, a natural stilbene found in grapes and wines exhibits a wide range of pharmacological properties. Resveratrol is also known as a good chemopreventive agent for inhibiting carcinogenesis processes that target kinases, cyclooxygenases, ribonucleotide reductase and DNA polymerases. A total...
| Main Authors: | , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI
2013
|
| Subjects: | |
| Online Access: | http://eprints.um.edu.my/10004/1/Design%2C_Synthesis_and_Cytotoxic_Evaluation_of_o-Carboxamido_Stilbene_Analogues.pdf |
| _version_ | 1796946002082529280 |
|---|---|
| author | Azmi, Mohamad Nurul Md Din, Mohd Fadzli Kee, Chin Hui Suhaimi, Munirah Ang, Kheng Ping Ahmad, Kartini Nafiah, Mohd Azlan Thomas, Noel Francis Leong, Kok Hoong Awang, Khalijah |
| author_facet | Azmi, Mohamad Nurul Md Din, Mohd Fadzli Kee, Chin Hui Suhaimi, Munirah Ang, Kheng Ping Ahmad, Kartini Nafiah, Mohd Azlan Thomas, Noel Francis Leong, Kok Hoong Awang, Khalijah |
| author_sort | Azmi, Mohamad Nurul |
| collection | UM |
| description | Resveratrol, a natural stilbene found in grapes and wines exhibits a wide range of pharmacological properties. Resveratrol is also known as a good chemopreventive agent for inhibiting carcinogenesis processes that target kinases, cyclooxygenases, ribonucleotide reductase and DNA polymerases. A total of 19 analogues with an amide moiety were synthesized and the cytotoxic effects of the analogues on a series of human cancer cell lines are reported. Three compounds 6d, 6i and 6n showed potent cytotoxicity against prostate cancer DU-145 (IC50 = 16.68 µM), colon cancer HT-29 (IC50 = 7.51 µM) and breast cancer MCF-7 (IC50 = 21.24 µM), respectively, which are comparable with vinblastine. The resveratrol analogues were synthesized using the Heck method. |
| first_indexed | 2024-03-06T05:25:04Z |
| format | Article |
| id | um.eprints-10004 |
| institution | Universiti Malaya |
| language | English |
| last_indexed | 2024-03-06T05:25:04Z |
| publishDate | 2013 |
| publisher | MDPI |
| record_format | dspace |
| spelling | um.eprints-100042019-02-13T03:03:14Z http://eprints.um.edu.my/10004/ Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues Azmi, Mohamad Nurul Md Din, Mohd Fadzli Kee, Chin Hui Suhaimi, Munirah Ang, Kheng Ping Ahmad, Kartini Nafiah, Mohd Azlan Thomas, Noel Francis Leong, Kok Hoong Awang, Khalijah Q Science (General) QD Chemistry QH301 Biology R Medicine RC0254 Neoplasms. Tumors. Oncology (including Cancer) RM Therapeutics. Pharmacology RS Pharmacy and materia medica Resveratrol, a natural stilbene found in grapes and wines exhibits a wide range of pharmacological properties. Resveratrol is also known as a good chemopreventive agent for inhibiting carcinogenesis processes that target kinases, cyclooxygenases, ribonucleotide reductase and DNA polymerases. A total of 19 analogues with an amide moiety were synthesized and the cytotoxic effects of the analogues on a series of human cancer cell lines are reported. Three compounds 6d, 6i and 6n showed potent cytotoxicity against prostate cancer DU-145 (IC50 = 16.68 µM), colon cancer HT-29 (IC50 = 7.51 µM) and breast cancer MCF-7 (IC50 = 21.24 µM), respectively, which are comparable with vinblastine. The resveratrol analogues were synthesized using the Heck method. MDPI 2013-11-27 Article PeerReviewed application/pdf en http://eprints.um.edu.my/10004/1/Design%2C_Synthesis_and_Cytotoxic_Evaluation_of_o-Carboxamido_Stilbene_Analogues.pdf Azmi, Mohamad Nurul and Md Din, Mohd Fadzli and Kee, Chin Hui and Suhaimi, Munirah and Ang, Kheng Ping and Ahmad, Kartini and Nafiah, Mohd Azlan and Thomas, Noel Francis and Leong, Kok Hoong and Awang, Khalijah (2013) Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues. International Journal of Molecular Sciences, 14 (12). pp. 23369-23389. ISSN 1661-6596, DOI https://doi.org/10.3390/ijms141223369 <https://doi.org/10.3390/ijms141223369>. https://doi.org/10.3390/ijms141223369 doi:10.3390/ijms141223369 |
| spellingShingle | Q Science (General) QD Chemistry QH301 Biology R Medicine RC0254 Neoplasms. Tumors. Oncology (including Cancer) RM Therapeutics. Pharmacology RS Pharmacy and materia medica Azmi, Mohamad Nurul Md Din, Mohd Fadzli Kee, Chin Hui Suhaimi, Munirah Ang, Kheng Ping Ahmad, Kartini Nafiah, Mohd Azlan Thomas, Noel Francis Leong, Kok Hoong Awang, Khalijah Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues |
| title | Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues |
| title_full | Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues |
| title_fullStr | Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues |
| title_full_unstemmed | Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues |
| title_short | Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues |
| title_sort | design synthesis and cytotoxic evaluation of o carboxamido stilbene analogues |
| topic | Q Science (General) QD Chemistry QH301 Biology R Medicine RC0254 Neoplasms. Tumors. Oncology (including Cancer) RM Therapeutics. Pharmacology RS Pharmacy and materia medica |
| url | http://eprints.um.edu.my/10004/1/Design%2C_Synthesis_and_Cytotoxic_Evaluation_of_o-Carboxamido_Stilbene_Analogues.pdf |
| work_keys_str_mv | AT azmimohamadnurul designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT mddinmohdfadzli designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT keechinhui designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT suhaimimunirah designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT angkhengping designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT ahmadkartini designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT nafiahmohdazlan designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT thomasnoelfrancis designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT leongkokhoong designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues AT awangkhalijah designsynthesisandcytotoxicevaluationofocarboxamidostilbeneanalogues |