54-97-7Relevant articles and documents
CYCLOPROPYLAMINE COMPOUND AS LSD1 INHIBITOR AND USE THEREOF
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Paragraph 0062-0064, (2021/07/24)
Provided is a cyclopropylamine compound as lysine-specific demethylase 1 (LSD1) inhibitor, and a use thereof in preparation of drug for treating diseases associated with LSD1. The cyclopropylamine compound is a compound represented by formula (I), an isomer thereof, and a pharmaceutically acceptable salt thereof.
Synthetic method for arylcyclopropylamine compound
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, (2019/11/29)
The invention relates to a synthetic method for an arylcyclopropylamine compound. The method comprises the following steps: with a cinnamaldehyde compound as a raw material, reacting the cinnamaldehyde compound with bis(pinacolato)diboron to obtain a boroalkylated product; and then subjecting the boroalkylated product and an aminated compound to a ring-closure reaction so as to obtain the arylcyclopropylamine compound. Compared with the prior art, the invention has the following advantages: the synthetic method of the invention is simple to operate and short in reaction time; reagents used inthe invention are cheap and easily available; the target arylcyclopropylamine compound can be prepared from most substrates at a high overall yield and is mainly in the form of transconfiguration; anda route of the method is obviously improved, more economical, safer and easy for industrial production.
Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen
Ota, Yosuke,Itoh, Yukihiro,Kaise, Asako,Ohta, Kiminori,Endo, Yasuyuki,Masuda, Mitsuharu,Sowa, Yoshihiro,Sakai, Toshiyuki,Suzuki, Takayoshi
supporting information, p. 16115 - 16118 (2016/12/26)
Targeting cancer with small molecule prodrugs should help overcome problems associated with conventional cancer-targeting methods. Herein, we focused on lysine-specific demethylase 1 (LSD1) to trigger the controlled release of anticancer drugs in cancer cells, where LSD1 is highly expressed. Conjugates of the LSD1 inhibitor trans-2-phenylcyclopropylamine (PCPA) were used as novel prodrugs to selectively release anticancer drugs by LSD1 inhibition. As PCPA-drug conjugate (PDC) prototypes, we designed PCPA-tamoxifen conjugates 1 a and 1 b, which released 4-hydroxytamoxifen in the presence of LSD1 in vitro. Furthermore, 1 a and 1 b inhibited the growth of breast cancer cells by the simultaneous inhibition of LSD1 and the estrogen receptor without exhibiting cytotoxicity toward normal cells. These results demonstrate that PDCs provide a useful prodrug method that may facilitate the selective release of drugs in cancer cells.