Abstract Cancer cells usually adapt metabolic phenotypes to chemotherapeutics. A defensive strategy against this flexibility is modulate signaling pathways relevant cancer bioenergetics. triphenylphosphonium‐modified terpyridine platinum(II) complex (TTP) was designed inhibit thioredoxin reductase (TrxR) and multiple metabolisms of cells. TTP exhibited enhanced cytotoxicity cisplatin‐insensitive human ovarian in a caspase‐3‐independent manner showed preferential inhibition mitochondrial...

A cationic copper complex with triphenylphosphine as a targeting group preferentially accumulates in mitochondria of tumor cells and strongly inhibits their proliferation.

A new binucleating “Janus” ligand based on the beta-diketiminato (“NacNac”) donor combined with an NCN pincer framework has been designed and synthesized. By incorporating pyridyl donors imino carbons of NacNac ligand, two binding sites for metals are introduced. The ligand’s capabilities demonstrated by ligating BF2 in pocket NiBr into bay. resulting binuclear boron-nickel complexes chemistry was explored substitution bromide nickel one fluoride ion boron weakly coordinating triflimide...

The medicinal values of many natural bioactive components to treat myocardial ischaemia reperfusion (I/R) injury are limited by their poor permeability. Herein, we demonstrate that an original tanshinone IIA derivative (Tan-TPP) could probably be improved I/R suppressant. It was optimised mitochondria targeting group triphenylphosphine (TPP). Intriguingly, it accumulate in more efficiently inhibit the activity succinate dehydrogenase (SDH), which is closely related with oxidative injury....

Truck automation is emerging as an innovative technology with benefits in traffic safety and the economy to revolutionize freight traffic. Despite these benefits, potential negative or positive effects of different driving levels (from no full automation) on highway geometry remained be determined. In this study, differences related sight distance characteristics among varied were firstly discussed calibrated. Then, seven analysis scenarios typical proposed. Based each level tailored...

Abstract Cancer cells usually adapt metabolic phenotypes to chemotherapeutics. A defensive strategy against this flexibility is modulate signaling pathways relevant cancer bioenergetics. triphenylphosphonium‐modified terpyridine platinum(II) complex (TTP) was designed inhibit thioredoxin reductase (TrxR) and multiple metabolisms of cells. TTP exhibited enhanced cytotoxicity cisplatin‐insensitive human ovarian in a caspase‐3‐independent manner showed preferential inhibition mitochondrial...

Hypoxia is a major obstacle for cancer therapy due to its association with cell proliferation, tumor distant metastasis, and treatment resistance. In this study, hypoxia-activated bifunctional prodrug (CC5) was designed, synthesized encapsulated by photo-responsive ruthenium complex-derived polymer yield light-controlled multi-step drug release system (CC5-RuCa) synergistic against hypoxia. Under NIR irradiation, CC5-RuCa not only generated ROS kill the cells in exterior of but also released...

Abstract ( E )‐3‐(10‐ethylphenothiazine‐3‐yl)acrylic acid (LCOOH) was synthesized. LCOOH reacted with Ph 3 Sn(OH) and n Bu 2 SnO to afford CL 1 ) {[nBu CL] O} ), respectively. The structures of all the compounds were solved by single‐crystal X‐ray diffraction. Compounds present discrete ladder frameworks, one‐photon absorption excited fluorescence, two‐photon fluorescence spectra systematically investigated. results show that two organostannoxanes exhibit much more enhanced properties than...

As present NO donor drugs cannot localize to release at the hypoxic site, along with short half-life and bidirectional regulation of NO, they are unable overcome low bioavailability side effects in treatment myocardial hypoxia injury. In this study, we designed prepared a novel hypoxia-activated (Hano) by hybridization known compound (Nno) group. Hano isosorbide dinitrate were compared terms anti-myocardial Furthermore, Nno on releasing dilating blood vessels, preventing injury studied...

Cardiac inflammation is generally accompanied by hypoxia, while myocardial injury and an abnormal microenvironment caused hypoxia tend to suppress the efficacy of common anti-inflammatory drugs. To improve effect under a hypoxia-activated prodrug HAP1 consisting cyclooxygenase-2 (COX-2) inhibitor Ind carbonic anhydrase (CA) Ace was synthesized. found be activated nitroreductase (NTR) release two pharmacophores achieve combinatory medication intensively at hypoxic site, better than or alone....

Intracellular delivery of biologicals such as peptides, proteins, and nucleic acids presents a great opportunity for innovative therapeutics. However, the endosome entrapment remains major bottleneck in intracellular biomacromolecules, largely limiting their therapeutic potential. Here, we converted cell-penetrating peptide (CPP), low molecular weight protamine (LMWP), to endosomal escape peptides (EEPs) by masking LMWP with pH-responsive counter-ionic peptide. The resulting masked CPPs...

4′-(4-{2-[4-(N,N-diphenylamino)phenyl]ethenyl}phenyl)-2,2′:6′,2′′-terpyridine is a highly conjugated compound, which used to grow polymorphs. The results obtained suggest that polymorphs could appear as the Eu3+/Ag+-induced feature. Only three intermolecular C−H···π interactions stabilize polymorph A in monoclinic space group C2/c with Z = 8, while five assume completely new pattern arrange B P21/c 4. changes patterns of impose on molecular conformation, induced dipole, electronic...

In order to obtain efficient NO donor drugs treat hypoxic cardiac disease, a series of hypoxia-targeted compounds were prepared and screened. Among them, representative compound H3 was found selectively release under hypoxia with higher ratio than isosorbide dinitrate (ISDN). vitro study indicated that had strong capability alleviating vascular dilation reducing myocardial injury due its effective regulation dilatation injury-related proteins in H9c2 cells even at low concentrations. By...

Connected vehicles (CVs) exchange a variety of information instantly with surrounding and traffic facilities, which could smooth flow significantly. The objective this paper is to analyze the effect CVs on running speed. This study compared delay time, travel speed in normal connected states, respectively, through VISSIM (a simulation software developed by PTV company German). optimization model was established simulate decision-makings MATLAB, considering parameters vehicle distance,...