Immune checkpoint inhibitors and monoclonal antibodies reinvigorate cancer immunotherapy. However, these immunotherapies only benefit a subset of patients. We previously reported that ALDH tumor cells were highly enriched for stem (CSCs), CSC lysate-pulsed dendritic cell (CSC-DC) vaccine was shown to induce CSC-specific cytotoxic T lymphocytes. In this study, we investigated the targeting effect CSC-DC combined with dual blockade programmed death-ligand 1 T-lymphocyte-associated protein...

A series of novel anthranilic diamide derivatives (5a–5ab) containing moieties trifluoromethylpyridine and hydrazone was designed synthesized. The synthesized compounds were evaluated in vivo for their activities against tobacco mosaic virus (TMV) cucumber (CMV). Most the displayed good to excellent antiviral activities. 5i, 5k, 5s, 5w, 5x, 5z had curative activity over 65% TMV at concentration 500 μg/mL, which significantly higher than those ningnanmycin (55.0%) ribavirin (37.9%). Notably,...

Abstract Molecular nitrogen (N 2 ), an abundant component of the atmosphere, is appealing for industrial value‐added products. However, its intrinsic inertness limits activation to mainly metallic species. Environmental concerns and harsh reaction conditions have resulted in a demand alternate nonmetallic nontoxic routes activate functionalize N at ambient conditions. Comprehensive density functional theory (DFT) calculations are performed on by boron species, specifically experimentally...

Luminogens characteristic of aggregation-induced emission (AIEgens) have been extensively exploited for the development imaging-guided photodynamic therapeutic (PDT) agents. However, intramolecular rotation donor-acceptor (D-A) type AIEgens favors non-radiative decay photonic energy which results in unsatisfactory fluorescence quantum and singlet oxygen yields. To address this issue, we developed several molecularly engineered with partially "locked" molecular structures enhancing both...

Verticinone, an isosteroidal alkaloid separated from Bulbus Fritillaria (Chinese name "Bei-mu"), was evaluated for its analgesic activities in murine models of inflammatory and neuropathic pain. It shown that oral administarion verticinone could significantly inhibit acetic acid-induced writhing response a dose-dependent way, the inhibition 3 mg/kg 66.2%, which approximately higher than 200 aspirin. In formalin test, high dose (3 mg/kg) nociceptive both phases, but lower (1.5 only second...

Novel trifluoromethyl pyridine derivatives bearing 1,3,4-oxadiazole whereas synthesized, their which showed good insecticidal activity; a 3D-QSAR model with predictability was is proposed.

Several aggregation-induced emission luminogens (AIEgens) with excellent water-solubility and near-infrared were designed synthesized for wash-free "off-on" mitochondrial imaging photodynamic therapy of HeLa cells. The AIEgen TEPP exhibits both bright (φF = 17.8%) high hybrid ROS productivity (including OH˙ 1O2).

The diacylhydrazine derivatives have attracted considerable attention in recently years due to their simple structure, low toxicity, and high insecticidal selectivity. As well as 3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole is an important scaffold many molecules. In effort discover new molecules with good activity, a series of containing was synthesized bio-assayed.Bioassays demonstrated that some the title compounds exhibited favorable activities against Helicoverpa armigera Plutella...

Bridged carbonyls can enhance hyperconjugative aromaticity of group 9 transition metal disubstituted 2<italic>H</italic>-pyrrolium and cyclopentadiene.

Devastating plant virus diseases leading to bad harvests and lower quality of crops have made feeding the beyond seven billion population a huge challenge. Nevertheless, growing resistance cross crop protection agents this challenge harder. Therefore, an efficient agent with novel structure mode action showing higher efficiency eco-friendly is urgently needed.The coat protein (CP) potential target for discovery new antiviral agents. Antiviral molecules can inhibit infection by obstructing...

Abstract A series of trifluoromethyl pyridine derivatives containing an 1,3,4‐oxadiazole moiety was synthesized and characterized by 1 H NMR, 19 F 13 C HR‐MS. The bio‐assay results indicated that some the compounds exhibited good insecticidal activity against Mythimna separate Plutella xylostella . Most compound showed 100% two pests at 500 mg⋅L −1 ; in practically, value median lethal concentration (LC 50 ) for title much lower than commercial chlorpyrifos. Preliminary structure‐activity...

A convenient and efficient β-cyclodextrin-SO3H-assisted strategy for construction of spiro indoline derivatives in aqueous media was disclosed. The present protocol showed various advantages including short reaction time, broad scope substituents, simplicity practice, high yields products, recyclability catalysts, safety, cheapness benign solvents. Preliminary study indicated that some spiroindoline exhibited anti-Tobacco Mosaic Virus (TMV) activity potential use plant protection.

Diamide derivatives are biologically active molecules that have been widely applied in recent years research on pesticides, especially insecticides. Using a simple and environmentally friendly scheme, series of new diamide containing trifluoromethylpyridine skeleton was designed, synthesized, confirmed by 1H, 19F 13C NMR, HR-MS. Their insecticidal activities against Plutella xylostella Helicoverpa armigera were measured the relationship between structure activity investigated. Eight title...

An efficient and chemoselective C(sp2)–N bond cleavage of aromatic imidazo[1,2-a]pyridine molecules is developed. A broad scope amide compounds such as α-ketoamides N-(pyridin-2-yl)arylamides are afforded the final products in up to quantitative yields. Diverse C–N cleavages controlled by oxidative species used this transformation, with various a fashion. preliminary study indicated that some exhibit anti-Tobacco Mosaic Virus activity for potential use plant protection.

Abstract Background Progressive lung cancer is associated with abnormal coagulation. Platelets play a vital part in evading immune surveillance and angiogenesis the case of tumor metastasis. The study aimed to analyze predictive prognostic effects platelet count on non-small cell (NSCLC) patients treated epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs). Methods This retrospectively analyzed platelets 52 NSCLC (EGFR) mutant following EGFR-TKI treatment. Related data,...

The development of aggregation-induced emission luminogens (AIEgens) with high brightness and efficient photodynamic therapy (PDT) is great value for the precise diagnosis treatment cancers. In this contribution, two novel AIEgens, TBBCyP TBTCyP D-A-π-A structure, were designed prepared based on molecular rational design electron-donating receptors. Experimental theoretical results indicated that both own bright AIE feature, satisfy photos ability, generate singlet oxygen (1O2). Notably,...

Density functional theory calculations were used to investigate the reaction mechanisms on [3 + 2] cycloaddition reactions of azides with metal carbyne complexes. Our results reveal that formation a 1,4-metallatriazole regioisomer is kinetically favorable process in comparison 1,5-metallatriazole. Aromaticity plays an important role stabilizing products these reactions. Further analyses show electron-donating ligand centers or electron-withdrawing group azide could accelerate reaction. All...