Steroid sulfatase inhibitors based on sulfamated derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol as potential anticancer agents - Project - MOST Wiedzy

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Steroid sulfatase inhibitors based on sulfamated derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol as potential anticancer agents

Cancer disease is one of the most common cause of death worldwide. Interestingly, most of the types of cancer demonstrated hormone-dependent nature (e.g., approximately 90% of breast cancer depends on hormones). Therefore, The World Health Organization lists active hormones as major factors responsible for tumor growth induction. The biosynthesis process of active steroids (e.g., estradiol) depends on a few enzymatic pathway, e.g., steroid sulfatase (STS). In the light of the recent studies, STS became a new and interesting molecular target in the treatment of hormone-dependent cancers. This project will realize the next research on novel STS inhibitors based on sulfamated derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol, which were obtained during implementation of PRELUDIUM grant (2015/19/N/NZ7/00938). The basic research indicated that abovementioned compounds are able to inhibit the activity of STS much more effectively than Irosustat – STS inhibitors evaluated in clinical trials. Furthermore, abovementioned compounds occurred to be effective in in vivo studies indicating high anticancer activity and no-toxicity what make them very promising drug candidates in treatment of hormone-dependent cancers. In the course of realization this project we plan to perform conceptual and development work: - providing patent protection for the abovementioned compounds - promotion of obtained results in the world, - performing activities aimed at acquiring a business partner, - performing research on physicochemical properties of sulfamated derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol – determination of logP, pKa parameters, as well as solubility and stability in aqueous solution, - performing research on polymorphic forms and complexing properties to metal ions (mainly calcium).

Details

Project's funding:
TANGO
Agreement:
TANGO-IV-A/0004/2019-00 z dnia 2020-08-28
Realisation period:
2020-10-01 - 2021-12-31
Project manager:
dr inż. Mateusz Daśko
Realised in:
Department of Inorganic Chemistry
Request type:
National Research Programmes
Domestic:
Domestic project
Verified by:
Gdańsk University of Technology

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