5438-70-0Relevant articles and documents
BIODERIVED EPOXIDE TRIAZINE NETWORKS AND METHODS OF MAKING THE SAME
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Paragraph 0048; 0049, (2021/11/26)
The present disclosure relates to a method that includes a first reacting of a first molecule and formaldehyde and/or a paraformaldehyde to form a triazine-containing intermediate and a second reacting of the triazine-containing intermediate with a second
Hapten design and monoclonal antibody to fluoroacetamide, a small and highly toxic chemical
Yang, Ling,Zhang, Xiya,Shen, Dongshuai,Yu, Xuezhi,Li, Yuan,Wen, Kai,Shen, Jianzhong,Wang, Zhanhui
, p. 1 - 12 (2020/07/08)
Fluoroacetamide (FAM) is a small (77 Da) and highly toxic chemical, formerly used as a rodenticide and potentially as a poison by terrorists. Poisoning with FAM has occurred in humans, but few reliably rapid detection methods and antidotes have been reported. Therefore, producing a specific antibody to FAM is not only critical for the development of a fast diagnostic but also a potential treatment. However, achieving this goal is a great challenge, mainly due to the very low molecular weight of FAM. Here, we design two groups of FAM haptens for the first time, maximally exposing the fluorine or amino groups, with the aid of linear aliphatic or phenyl-contained spacer arms. Interestingly, whereas the hapten with fluorine at the far end of the hapten did not induce an antibody response to FAM, the hapten with an amino group at the far end and phenyl-contained spacer arm triggered a significantly specific antibody response. Finally, a monoclonal antibody (mAb) named 5D11 was successfully obtained with an IC50 value of 97 μg mL?1 and negligible cross-reactivities to the other nine functional and structural analogs.
Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors
Jiao, Xiaoyu,Tang, Chunlei,Zhang, Lixun,Zhang, Qing,Zhang, Yongjie,Zhao, Kuantao
supporting information, (2020/10/02)
As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 15b, 16b, 24a, and 24c showed excellent biological activities in a low nanomolar range. In particular, compound 16b demonstrated significant inhibitory potency against FLT3-ITD (IC50 = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC50 = 0.176 nM). It is indicated that compound 16b for the treatment of acute myeloid leukemia could be very promising.
