AgOTf silver triflate Ala alanine aq. aqueous ATP adenosine-5'-triphosphate ATR attenuated total reflection Asn asparagine BF3•OEt2 trifluoroborane diethylether complex Bn benzyl BNCT boron neutron capture therapy In(OTf)3 indium triflate i Pr isopropyl IR infra-red KUR Kyoto University Research Reactor Lg leaving group LLC Lewis lung carcinoma Me methyl MEM minimum essential medium MM molecular mechanics MRI magnetic resonance imaging MS mass spectrometry or molecular sieve MTT

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... 2-thiazolyl)-2,5-diphenyl-2H-tetrazolum bromide 2-NBDG 2-deoxy-2-[7-nitro-2,1,3-benzoxadiazol-4-yl]amino]-Dglucose NBS N-bromosuccinimide NIS N-iodosuccinimide NMR nuclear magnetic resonance p-NO2PhSCl p-nitrophenylsulfenyl chloride [1-2]: General introduction of boron neutron capture therapy Cancer has a major impact on society and is the second leading cause of death in the world. The most common cancers are breast cancer, lung and bronchus cancer, prostate cancer, colon and rectum cancer, melanoma of the skin, bladder cancer, non-Hodgkin lymphoma, kidney and renal pelvis cancer, endometrial cancer, leukemia, pancreatic cancer, thyroid cancer and liver cancer. Although the various new methodology to treat and detect cancer have been developed for several decades, the World Health Organization (WHO) announced that approximately 9.6 million people were estimated to have died from various forms of cancer in 2018. [21] rrent cancer treatments could be classified into the following four categories, as shown in Chart 1-4. The first is surgical therapy, in which target tumor cells are directly removed from patient (Chart 1-4a). The drawbacks of this treatment include the serious surgical damage to patients, requirement of advanced technique. Indeed, surgical operations of the deep-seated tumor such as brain tumors and neck cancers are quite difficult. The second and third methods involves the chemotherapy and biotherapy with drugs such as small or large molecules (e.g. antibodies, vaccines, oligonucleotides and so on), as shown in Charts 1-4b and 1-4c. A major advantage of these therapy is its ability to travel throughout the body and widespread cancers, whereas surgery and radiation are confined to treat one area. However, the disadvantage of these therapies are the toxic side effects due to the death of healthy cells and/or tissues, and the development of resistance to drugs. Forth methodology is radiotherapy, in which target tumor tissues are irradiated by high energy beams such as X-and -ray which work by damaging the DNA of tumor cell leading to cellular death (Chart 1-4d). Although the radiation therapy could kill inoperable and/or deep-seated tumor tissues, side effect would be occurred because radiation therapy can also damage healthy cells and tissues around the treatment area.