Carboxyboranylamino ethanol: unprecedented discovery of boron agents for neutron capture therapy in cancer treatment.

Authors :: Zhu Y
Cai J
Hosmane NS
Suzuki M
Uno K
Zhang Y
Takagaki M
Source :: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2021 Oct 05; Vol. 57 (79), pp. 10174-10177. Date of Electronic Publication: 2021 Oct 05.
Publication Year :: 2021
Abstract: Carboxyboranylamino ethanol (Me <subscript>2</subscript> N(BH <subscript>2</subscript> CO <subscript>2</subscript> H)CH <subscript>2</subscript> CH <subscript>2</subscript> OH, 1) was prepared in 75.0% yield by an amine-exchange reaction. Compound 1 shows lower cytotoxicity and higher anti-tumor efficacy in vitro towards the SCCVII cell line in comparison with 4-borono-L-phenylalanine (BPA) and methyl 2-hydroxyl-5-(1'- ortho -carbonylmethyl-1',2',3'-triazol-4'-yl)-benzonate (2). The bio-enhancement is interpreted using molecular docking calculations.

Subjects :: Amino Alcohols chemistry
Animals
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Boron Compounds chemistry
Cell Line, Tumor
Mice
Molecular Docking Simulation
Amino Alcohols pharmacology
Antineoplastic Agents pharmacology
Boron Compounds pharmacology
Boron Neutron Capture Therapy
Carcinoma, Squamous Cell drug therapy
Drug Discovery

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