Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series
摘要:
Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the enzyme activity, but appeared to dramatically affect the cellular efficacy. The discovery of lapatinib emerged from this work. (c) 2006 Elsevier Ltd. All rights reserved.
Synthesis and characterization of novel tetrahedral copper(I) complexes comprising tridentate PNP-aminodiphosphines and tetradentate PN(X)P-substituted aminodiphosphines (X=O, S)
摘要:
Two series of novel tetrahedral copper(I) complexes comprising tridentate PNP-aminodiphosphines and tetradentate PN(X) P-substituted aminodiphosphines (X = O, S) have been prepared and characterized by conventional physico-chemical techniques. The first series includes '3 + 1'-type complexes comprising an aromatic PNP-aminodiphosphine and acetonitrile or triphenylphosphine. In the second series, the central amine function of the PNP-ligand was substituted with functionalized pendant arms containing ether, hydroxyl or thioether groups to enhance the chelation ability of the ligand. Fully coordinated neutral and cationic complexes were isolated. A preliminary study investigating both the labeling of Cu-64 with the prototype PN(S)P ligand and the potential cytotoxic activity of the 'cold' [Cu(PN(S)P)][BF4] complex is reported. (C) 2012 Elsevier B. V. All rights reserved.
Synthesis, characterization, and catalytic behaviours of β-carbonylenamine-derived [O−NS]TiCl3 complexes in ethylene homo- and copolymerization
作者:Xiao-Hong Yang、Zheng Wang、Xiu-Li Sun、Yong Tang
DOI:10.1039/b910868h
日期:——
A series of [OâNS]TiCl3 complexes 5aâl derived from β-carbonylenamine were synthesized and characterized. In the presence of modified methylaluminoxane (MMAO), complexes 1, 5aâi and 5l are highly active for ethylene polymerization and copolymerization of ethylene with 1-hexene, CPE and NBE. Up to 5.12 à 106 g molâ1 hâ1 atmâ1 of activity for the copolymerization of ethylene with 1-hexene is achieved with a 28.9 mol% incorporation ratio.
合成并表征了一系列来自β-羰基胺的[OâNS]TiCl3配合物5aâl。在改性甲基铝氧烯(MMAO)的存在下,配合物1、5aâi和5l对乙烯聚合及乙烯与1-己烯、CPE和NBE的共聚合表现出高活性。在乙烯与1-己烯的共聚合中,活性达到5.12 × 10^6 g molâ1 hâ1 atmâ1,聚合比例达到28.9 mol%。
Synthesis, Characterization, and Highly Selective Ethylene Dimerization to 1-Butene of [O−NX]Ni(II) Complexes
作者:Chongjie Xu、Qi Shen、Xiuli Sun、Yong Tang
DOI:10.1002/cjoc.201100443
日期:2012.5
series of nickel(II) complexes have been synthesized and characterized. Molecular structure analysis exhibits that a square planar geometry around nickel is adopted. Upon activation with MAO, these nickel(II) complexes are efficient in catalyzing the ethylenedimerization, providing 1‐butene with an activity of up to 1.4×107 g/(mol·h·atm). The heteroatoms of the sidearm in the complexes were proved to
已经合成和表征了一系列镍(II)配合物。分子结构分析表明,采用了围绕镍的正方形平面几何形状。通过MAO活化后,这些镍(II)络合物可有效催化乙烯二聚,从而提供1-丁烯,其活性最高可达1.4×10 7 g /(mol·h·atm)。络合物中侧臂的杂原子被证明对1-丁烯的活性和选择性有很大的影响。
Thermoresponsive Sulfone and Sulfoxide‐Containing Polyacrylamides
作者:Jieun Choi、Hyung‐il Lee
DOI:10.1002/bkcs.12341
日期:2021.8
polyacrylamides containing sulfide, sulfone, or sulfoxide was successfully prepared by reversible addition-fragmentation chain transfer (RAFT) polymerization. The thermal properties of polyacrylamides with sulfone or sulfoxide, which have not been studied before, were investigated for the first time. While poly[N-(2-(propylsulfonyl)ethyl)acrylamide] (P2SO2) with sulfone groups was water insoluble, pol