5467-84-5Relevant articles and documents
Oxovanadium(v)-catalyzed amination of carbon dioxide under ambient pressure for the synthesis of ureas
Moriuchi, Toshiyuki,Sakuramoto, Takashi,Matsutani, Takanari,Kawai, Ryota,Donaka, Yosuke,Tobisu, Mamoru,Hirao, Toshikazu
, p. 27121 - 27125 (2021/08/24)
Carbon dioxide is regarded as a reliable C1 building block in organic synthesis because of the nontoxic, abundant, and economical characteristics of carbon dioxide. In this manuscript, a commercially available oxovanadium(v) compound was demonstrated to serve as an efficient catalyst for the catalytic amination of carbon dioxide under ambient pressure in the synthesis of ureas. The catalytic transformation of chiral amines into the corresponding chiral ureas without loss of chirality was also performed. Furthermore, a gram-scale catalytic urea synthesis under ambient pressure was successfully achieved to validate the scalability of this catalytic activation of carbon dioxide. This journal is
Development of a Polo-like Kinase-1 Polo-Box Domain Inhibitor as a Tumor Growth Suppressor in Mice Models
Gunasekaran, Pethaiah,Yim, Min Su,Ahn, Mija,Soung, Nak-Kyun,Park, Jung-Eun,Kim, Jaehi,Bang, Geul,Shin, Sang Chul,Choi, Joonhyeok,Kim, Minkyoung,Kim, Hak Nam,Lee, Young-Ho,Chung, Young-Ho,Lee, Kyeong,Eunkyeong Kim, Eunice,Jeon, Young-Ho,Kim, Min Ju,Lee, Kyeong-Ryoon,Kim, Bo-Yeon,Lee, Kyung S.,Ryu, Eun Kyoung,Bang, Jeong Kyu
, p. 14905 - 14920 (2020/12/02)
Polo-like kinase-1 (Plk1) plays a key role in mitosis and has been identified as an attractive anticancer drug target. Plk1 consists of two drug-targeting sites, namely, N-terminal kinase domain (KD) and C-terminal polo-box domain (PBD). As KD-targeting inhibitors are associated with severe side effects, here we report on the pyrazole-based Plk1 PBD inhibitor, KBJK557, which showed a remarkable in vitro anticancer effect by inducing Plk1 delocalization, mitotic arrest, and apoptosis in HeLa cells. Further, in vivo optical imaging analysis and antitumorigenic activities in mouse xenograft models demonstrate that KBJK557 preferentially accumulates in cancer cells and selectively inhibits cancer cell proliferation. Pharmacokinetic profiles and partition coefficients suggest that KBJK557 was exposed in the blood and circulated through the organs with an intermediate level of clearance (t1/2, 7.73 h). The present investigation offers a strategy for specifically targeting cancer using a newly identified small-molecule inhibitor that targets the Plk1 PBD.
Base-Mediated Intramolecular Decarboxylative Synthesis of Alkylamines from Alkanoyloxycarbamates
Li, Peihe,Ma, Nuannuan,Wang, Zheng,Dai, Qipu,Hu, Changwen
, p. 8233 - 8240 (2018/05/31)
A general and effective method for the synthesis of alkylamine via intramolecular decarboxylation of alkanoyloxycarbamates is described. The alkanoyloxycarbamates are readily prepared with alkyl carboxylic acids and hydroxylamine. The reaction shows a broad range of substrates (primary and secondary alkyl) with functional tolerance, and the corresponding products were obtained in good yields under mild conditions.