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An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine
Authors:
- Julia Krzywik,
- Maral Aminpour,
- Jan Janczak,
- Ewa Maj,
- Mahshad Moshari,
- Witold Mozga,
- Joanna Wietrzyk,
- Jack A. Tuszyński,
- Adam Włodzimierz Huczyński
- Record ID
- UAMb49e2d55608a4279a48c9b1619c2c807
- Author
- Journal series
- European Journal of Medicinal Chemistry, ISSN 0223-5234, e-ISSN 1768-3254
- Issue year
- 2021
- Vol
- 215
- Pages
- 1-24
- Article number
- 113282
- Keywords in original language
- Anticancer agents Carbamate Thiocarbamate Tubulin inhibitors Docking studies QSAR Crystal structure
- ASJC Classification
- ; ; ;
- Abstract in original language
- Colchicine shows very high antimitotic activity, therefore, it is used as a lead compound for generation of new anticancer agents. In the hope of developing novel, useful drugs with more favourable pharmacological profiles, a series of doubly modified colchicine derivatives has been designed, synthesized and characterized. These novel carbamate or thiocarbamate derivatives of 10-demethoxy-10-methylaminocolchicine have been tested for their antiproliferative activity against four human cancer cell lines. Additionally, their mode of action has been evaluated as colchicine binding site inhibitors, using molecular docking studies. Most of the tested compounds showed greater cytotoxicity (IC50 in a low nanomolar range) and were characterized by a higher selectivity index than standard chemotherapeutics such as cisplatin and doxorubicin as well as unmodified colchicine. Their pharmacological use in cancer therapy could possibly be accomplished with lower dosages and result in less acute toxicity problems than in the case of colchicine. In addition, we present a QSAR model for predicting the antiproliferative activity of doubly modified derivatives for two tumour cell lines
- DOI
- DOI:10.1016/j.ejmech.2021.113282 Opening in a new tab
- URL
- https://www.sciencedirect.com/science/article/pii/S0223523421001318?via%3Dihub Opening in a new tab
- Language
- eng (en) English
- License
- Score (nominal)
- 140
- Score source
- journalList
- Score
- = 140.0, 14-03-2022, ArticleFromJournal
- Publication indicators
- = 3; : 2018 = 1.464; : 2019 (2 years) = 5.572 - 2019 (5 years) =5.207
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- Uniform Resource Identifier
- https://researchportal.amu.edu.pl/info/article/UAMb49e2d55608a4279a48c9b1619c2c807/
- URN
urn:amu-prod:UAMb49e2d55608a4279a48c9b1619c2c807
* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or PerishOpening in a new tab system.