4760-35-4Relevant articles and documents
Half-sandwich Iridium(III) Benzimidazole-Appended Imidazolium-Based N-heterocyclic Carbene Complexes and Antitumor Application
Han, Yali,Liu, Xicheng,Tian, Zhenzhen,Ge, Xingxing,Li, Juanjuan,Gao, Min,Li, Yanru,Liu, Yi,Liu, Zhe
, p. 3697 - 3705 (2018)
A series of half-sandwich iridium(III) benzimidazole-appended imidazolium-based N-heterocyclic carbene (NHC) antitumor complexes [(η5-Cpx)Ir(C^N)Cl]Cl, where Cpx is pentamethylcyclopentadienyl (Cp*) or its biphenyl derivative (Cpxbiph) and C^N is a NHC chelating ligand, were successfully synthesized and characterized. The IrIII complexes showed potential antitumor activity against A549 cells, at most three times more potent than cis-platin under the same conditions. Complexes could bind to BSA by a static quenching mode, catalyzing the change of NADH to NAD+ and inducing the production of reactive oxygen species (maximum turnover number, 9.8), which play an important role in regulating cell apoptosis. Confocal microscopy showed that the complexes could specifically target lysosomes in cells with a Pearson's co-localization coefficient 0.76 and 0.72 after 1 h and 6 h, respectively, followed an energy-dependent cellular uptake mechanism and damaged the integrity of lysosomes. At the same time, complexes caused a marked loss of mitochondrial membrane potential.
Dicopper(II) complexes of chiral C2-symmetric diamino-bis(2-methylpyridyl) and diamino-bis(2-methylbenzimidazolyl) ligands
Pérez, Viridiana,Monsalvo, Iván,Demare, Patricia,Gómez-Vidales, Virginia,Regla, Ignacio,Castillo, Ivan
, p. 389 - 391 (2011)
Reaction of the chiral ligands (1S,4S)-2,5-bis(6-methylpyridyl)- diazabicyclo[2.2.1]heptane (L1), and (1S,4S)-2,5-bis(2- methylbenzimidazolyl)-diazabicyclo[2.2.1]heptane (L2) with copper(II) acetate results in the hydroxo-bridged dic
Synthesis of Carbophosphinocarbene and Their Donating Ability: Expansion of the Carbone Class
Liu, Shu-Kai,Chen, Wen-Ching,Yap, Glenn P. A.,Ong, Tiow-Gan
supporting information, p. 4395 - 4401 (2020/12/23)
In recent years, carbones (CL2) have established themselves to be reliable ligands in organometallic and catalytic reactions. With its superb donating ability as well as a second lone pair for extra coordination, it distinguishes itself from the widely used carbenes and phosphines. However, a lack of modular structural diversity in carbones has limited its use. A carbophosphinocarbene (CPC), a subclass of carbones containing a carbene and phosphine as flanking groups, offers an easy structural modification. In this work, we report a new modular synthetic procedure for CPCs by using readily available starting materials. In addition, the phosphine moiety can be easily exchanged and directly used out of the bottle. The resulting CPCs offer a strong donating ability. Their electronic properties have been determined using Ga and Au complexes.
Antitubercular and Antiparasitic 2-Nitroimidazopyrazinones with Improved Potency and Solubility
Ang, Chee Wei,Tan, Lendl,Sykes, Melissa L.,Abugharbiyeh, Neda,Debnath, Anjan,Reid, Janet C.,West, Nicholas P.,Avery, Vicky M.,Cooper, Matthew A.,Blaskovich, Mark A. T.
, p. 15726 - 15751 (2020/12/02)
Following the approval of delamanid and pretomanid as new drugs to treat drug-resistant tuberculosis, there is now a renewed interest in bicyclic nitroimidazole scaffolds as a source of therapeutics against infectious diseases. We recently described a nitroimidazopyrazinone bicyclic subclass with promising antitubercular and antiparasitic activity, prompting additional efforts to generate analogs with improved solubility and enhanced potency. The key pendant aryl substituent was modified by (i) introducing polar functionality to the methylene linker, (ii) replacing the terminal phenyl group with less lipophilic heterocycles, or (iii) generating extended biaryl side chains. Improved antitubercular and antitrypanosomal activity was observed with the biaryl side chains, with most analogs achieved 2- to 175-fold higher activity than the monoaryl parent compounds, with encouraging improvements in solubility when pyridyl groups were incorporated. This study has contributed to understanding the existing structure-activity relationship (SAR) of the nitroimidazopyrazinone scaffold against a panel of disease-causing organisms to support future lead optimization.
Anti-oligomerization sheet molecules: Design, synthesis and evaluation of inhibitory activities against α-synuclein aggregation
Liu, Hao,Chen, Li,Zhou, Fei,Zhang, Yun-Xiao,Xu, Ji,Xu, Meng,Bai, Su-Ping
supporting information, p. 3089 - 3096 (2019/06/14)
Aggregation of α-synuclein (α-Syn) play a key role in the development of Parkinson Disease (PD). One of the effective approaches is to stabilize the native, monomeric protein with suitable molecule ligands. We have designed and synthesized a series of sheet-like conjugated compounds which possess different skeletons and various heteroatoms in the two blocks located at both ends of linker, which have good π-electron delocalization and high ability of hydrogen-bond formation. They have shown anti-aggregation activities in vitro towards α-Syn with IC50 down to 1.09 μM. The molecule is found binding in parallel to the NACore within NAC domain of α-Syn, interfering aggregation of NAC region within different α-Syn monomer, and further inhibiting or slowing down the formation of α-Syn oligomer nuclei at lag phase. The potential inhibitor obtained by our strategy is considered to be highly efficient to inhibit α-Syn aggregation.
