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Tanatorn Khotavivattana. Design, synthesis, and biological activity evaluation of novel colchicine derivative as anticancer agents. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2024.
Design, synthesis, and biological activity evaluation of novel colchicine derivative as anticancer agents
Name: Gbenga Olorunmodimu
Organization :
Chulalongkorn University. Faculty of Science
Name: Takorn Chow
Organization :
Chulalongkorn University. Faculty of Science
Name: Tanatorn Khotavivattana
Organization :
Chulalongkorn University. Faculty of Science
Email :
tanatorn.k@chula.ac.th
LCSH:
Antineoplastic agents
LCSH:
Colchicine
LCSH:
Drug development
Abstract:
Colchicine has been identified as a potential anticancer agent due to its ability to inhibit the formation
of microtubules by interacting with β-tubulin at the colchicine binding site. However, it exhibits high
systemic toxicity and lacks selectivity, leading to various side effects. Several structural modifications of the
colchicine scaffold, specifically at the C7, and C10 positions have been reported with significant improvement
to its potential in cancer treatment. Notably, replacing the C7-acetamide with long-chain amides significantly
increased the activity due to the interaction of alkyl moieties with the hydrophobic groove of α-tubulin. In this
work, we designed a novel structure of colchicine derivative with a 4-bromophenyl ring linked to the C7 via
an aliphatic linker and the replacement of C10-OMe with NHMe. The synthesis was performed by the
substitution of the C10-OMe of an ester-protected colchicine with methylamine. A newly optimized
hydrolysis of the C7-acetamide gave the amino-colchicine, which was then coupled with our pre-synthesized
linker via amide coupling to give the 4-bromophenyl-linked colchicine derivative in good yield over six steps.
In vitro testing of derivatives against Mia Paca-2 and HCT cell lines demonstrated potent anticancer activity
with IC50 values of 6.77 ± 0.40 nM and 0.71 ± 0.14 nM respectively
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2024
Modified:
2024-12-09
Issued:
2024-12-09
บทความ/Article
application/pdf
BibliograpyCitation :
In Kasetsart University. Faculty of Science. The Pure and Applied Chemistry International Conference 2024 (PACCON 2024) (pp.907-913). Bangkok : Kasetsart University, 2024
eng
©copyrights King Mongkut's University of Technology North Bangkok
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ใช้เวลา
0.022714 วินาที
Gbenga Olorunmodimu
| Title | Contributor | Type |
|---|---|---|
| Design, synthesis, and biological activity evaluation of novel colchicine derivative as anticancer agents
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Gbenga Olorunmodimu ;Takorn Chow;Tanatorn Khotavivattana | บทความ/Article |
Takorn Chow
| Title | Contributor | Type |
|---|---|---|
| Design, synthesis, and biological activity evaluation of novel colchicine derivative as anticancer agents
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Gbenga Olorunmodimu ;Takorn Chow;Tanatorn Khotavivattana | บทความ/Article |
Tanatorn Khotavivattana
| Title | Contributor | Type |
|---|---|---|
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| Design, synthesis, and biological activity evaluation of novel colchicine derivative as anticancer agents
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