306937-12-2Relevant academic research and scientific papers
With anti-tumor activity of heterocyclic biphenyl aryl urea compound and its preparation method and application
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Paragraph 0037-0040, (2017/08/19)
The invention provides a heterocyclic biphenyl aryl urea compound with antitumor activity, a preparation method and application thereof. The structural formula of the compound is shown as the specification, wherein R1 is indole, five-membered heterocycle
Discovery of novel VEGFR-2 inhibitors. Part 5: Exploration of diverse hinge-binding fragments via core-refining approach
Shan, Yuanyuan,Gao, Hongping,Shao, Xiaowei,Wang, Jinfeng,Pan, Xiaoyan,Zhang, Jie
, p. 80 - 90 (2015/09/15)
Pathological angiogenesis plays a critical role in numerous diseases including malignancy. VEGFR-2 is the central regulators in angiogenesis and has become a promising target for anticancer drug design. We have identified a novel biphenyl-aryl urea incorporated with salicyladoxime (BPS-7) as potent VEGFR-2 inhibitor. As a continuation to our previous research, various aromatic-heterocyclic were introduced as hinge-binding fragment via a core-refining approach. Interestingly, many compounds exhibited comparable VEGFR-2 inhibition to Sorafenib. In particular, 12e and 12o displayed excellent VEGFR-2 inhibitory activity with IC50 values of 0.50 nM and 0.79 nM, respectively. Several title compounds showed considerable antiproliferative activity against A549 and SMMC-7721 cells. In addition, molecular docking was performed to rationalize the efficiency of the better compounds. These results will be instructive for further inhibitor design and optimization.
Group of amino substituted benzoyl derivatives and their preparation and their use
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Page/Page column 17, (2011/08/04)
A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.
Fine tuning of the cation affinity of artificial receptors based on cyclic peptides by intramolecular conformational control
Kubik, Stefan,Goddard, Richard
, p. 311 - 322 (2007/10/03)
A series of cyclic hexapeptides consisting of alternating 4-substituted 3-aminobenzoic acid units (R = CH3, Cl, CH2OCH3, OCH3, COOCH3) and residues of the natural amino acid proline has been prepared and their ion affinities have been investigated. Whereas the unsubstituted parent compound (R = H) is able to bind cations through cation-π interactions with the aromatic subunits, as well as anions through hydrogen bonding with the peptide NH groups, the introduction of substituents at the 4-positions of the aromatic rings results in complete loss of the anion affinity. The cation complex stabilities depend on the substituents and cover a wide range from Ka = 140 M-1 for R = CH3 to Ka = 10800 M-1 for R = COOCH3 (Ka = 1260 M-1 for R = H) with n-butyltrimethylammonium picrate. The conformations of the peptides in solution have been determined by one-and two-dimensional NMR techniques and FT-IR spectroscopy. It was found that all the substituents prevent the peptides from adopting the necessary conformation for anion binding. For one receptor (R = OCH3), the results have been corroborated by a crystal structure determination. AM1 calculations have been used to estimate the electrostatic potential surfaces of the substituted aromatic subunits. The variation in the cation complex stabilities can be mainly attributed to the effects of the substituents on the solution conformations of the peptides. The influence of the substituents on the electrostatic potentials of the aromatic peptide subunits appears to be less important.
