Registration Number
0224U031448,
(0123U104256)
, R & D reports
Title
Development of semi-industrial protocols for the synthesis of functionalized carboranes – a promising platform for biomedical applications
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Повний запуск проєкту, адміністрування та логістика, попередні синтетичні дослідження
Head
Rassukana Yuliya V., Доктор хімічних наук
Registration Date
29-04-2024
Organization
Institute of Organic Chemistry NAS of Ukraine
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1. To elaborate convenient cost-efficient protocols for semi-industrial scale synthesis of ortho- meta- and para-disubstituted carboranes.
2. To design a chemical toolbox for the synthesis of functionalized carboranes for needs of medicinal chemistry and material science.
3. To conduct ADME/PK profiling of the carborane-based analogues of the compounds with well-studied biological activity.
4. To prove the concept of the bioisosteric relationships between carborane and benzene cores.
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The project aims to create the reliable and environmentally-friendly laboratory cycle for multigram synthesis of functionalized carboranes starting from commonly used bulk chemicals, which is important for the use of the carborane units for MedChem research and for the needs of material science. In-depth studies will be conducted in order to develop scalable protocols for the synthesis of functionalized carboranes. A series of carboranes with various functional groups will be prepared. Each chemical step will be optimized for semi-industrial scale-up. The practical observations will be supported by DFT studies of carboranes properties and reactivity. A set of building blocks (BB) with carborane core will be synthesized in multigram quantities. Small combinatorial libraries of compounds for MedChem applications will be created based on the previously synthesized carborane BB. The basic physicochemical and biological properties of the MedChem-relevant carborane molecules will be studied.
Product Description
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Konysheva Kateryna M.
Dmytro O. Lega
Mishchenko Artem M.
Mytiuk Andrii P.
Nechaev Maksym A.
Satska Yuliya A.
Smaliy Radomyr V.
Subota Andrii I.
Turchenyuk Volodymyr V.
Shtyl Nataliia A.
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2024-04-29