598-10-7Relevant articles and documents
Hydrolysis of Barbituric Acid Derivatives. Part 6. Hydrolysis of Spirocyclopropane- and Spiro-2'-methylcyclopropane-1',5-barbituric Acids
Mokrosz, Jerzy L.,Paluchowska, Maria H.
, p. 1391 - 1396 (1986)
The title barbiturates are hydrolysed by pyrimidine ring degradation or by cyclopropane ring opening.The cyclopropane ring decreases the hydrolytic reactivity of the pyrimidine moiety in relation to other spirobarbiturates, owing to conjugation between the cyclopropane ring and the C-4 or C-6 carbonyl group.The kinetics and the products of the alcoholysis of these barbiturates have been investigated.The influence of the cyclopropane moiety on the pKa1 values and 13C n.m.r. spectra has also been discussed.
1, 1-cyclopropane dicarboxylic acid amide compound as well as preparation method and application thereof
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Paragraph 0024; 0028; 0031, (2021/01/11)
The invention discloses a 1, 1-cyclopropane dicarboxylic acid amide compound as well as a preparation method and application thereof, and the structural formula of the 1, 1-cyclopropane dicarboxylic acid amide compound is as shown in a formula (I): in the formula (I), the structures of two substituted benzene rings are the same, the number of substituents R on each substituted benzene ring is 1-3,and the substituent R is selected from H, halogen, C1-C4 alkyl, C2-C4 ester group or C1-C3 alkoxy. The 1, 1-cyclopropane dicarboxylic acid amide compound provided by the invention is a novel compoundwith an efficient weeding effect, and provides a basis for research and development of novel herbicides.
Design, synthesis, and biological evaluation of thieno[2,3-d]pyrimidine derivatives as novel dual c-Met and VEGFR-2 kinase inhibitors
Li, Jieming,Gu, Weijie,Bi, Xinzhou,Li, Huilan,Liao, Chen,Liu, Chunxia,Huang, Wenlong,Qian, Hai
supporting information, p. 6674 - 6679 (2017/11/28)
Both c-Met and VEGFR-2 are important targets for cancer therapies. Here we report a series of potent dual c-Met and VEGFR-2 inhibitors bearing thieno[2,3-d]pyrimidine scaffold. The cell proliferation assay in vitro demonstrated that most target compounds had inhibition potency both on c-Met and VEGFR-2 with IC50 values in nanomolar range, especially compound 12j and 12m. Based on the further enzyme assay in vitro, compound 12j was considered as the most potent one, the IC50 values of which were 25 nM and 48 nM for c-Met and VEGFR-2, respectively. Following that, we docked the compound 12j with the proteins c-Met and VEGFR-2, and interpreted the SAR of these analogues. All the results indicate that 12j is a dual inhibitors of c-Met and VEGFR-2 that holds promising potential.
