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In our continuing search for novel small‐molecule anticancer agents, we designedand synthesized a series of novel (E)‐N'‐(3‐allyl‐2‐hydroxy)benzylidene‐2‐(4‐oxoquinazolin‐3(4H)‐yl)acetohydrazides (5), focusing on the modification of sub-stitution in the quinazolin‐4(3H)‐one moiety. The biological evaluation showed thatall 13 designed and synthesized compounds displayed significant cytotoxicity againstthree human cancer cell lines (SW620, colon cancer; PC‐3, prostate cancer; NCI‐H23, lung cancer). The most potent compound5ldisplayed cytotoxicity up to 213‐fold more potent than 5‐fluorouracil and 87‐fold more potent than PAC‐1, the firstprocaspase‐activating compound. Structure–activity relationship analysis revealedthat substitution of either electron‐withdrawing or electron‐releas... |
Compound and simple droplets have been studied and appeared in many life applications, e.g., drug processing and microfluidic systems. Many studies have been conducted on the thermocapillary effects on simple droplets, but similar studies on compound droplets are quite rare. Filling this missing gap, this paper presents the front-tracking-based simulation results of the thermocapillary effects on compound droplets in a certain limited domain. The compound droplet consists of a single inner core that is initially concentric with the outer one. Various dimensionless parameters including Reynolds number from 1 to 50, Marangoni number from 1 to 100, droplet radius ratio from 0.3 to 0.8, and viscosity ratios from 0.1 to 6.4 are varied to reveal their influences on the migration of a comp... |
Although most Asian states are signatories to UNCLOS, which offers options for dispute resolution by either voluntary or compulsory processes, in reality fewer than a dozen Asian states have taken advantage of such an approach. The decision to adopt third-party mechanisms comes under great scrutiny and deliberation, not least because of the entailing legal procedures and the politically sensitive nature of disputes. Vietnam claims the second-largest maritime area in the South China Sea dispute after China. A comparison of two recent cases—the arbitration between the Philippines and China and the conciliation between Timor-Leste and Australia—highlights the importance of selecting between binding and nonbinding decisions and framing a complaint. In particular, any legal action under ... |
Affective computing, also known as emotional artificial intelligence (AI), is an emerging and cutting-edge field of AI research. It draws on computer science, engineering, psychology, physiology, and neuroscience to computationally model, track, and classify human emotions and affective states. While the US once dominated the field in terms of research and citation from 1995–2015, China is now emerging as a global contender in research output, claiming second place for the most cited country from 2016–2020. This article maps the rhizomatic growth and development of scientific publications devoted to emotion-sensing AI technologies. It employs a bibliometric analysis that identifies major national contributors and international alliances in the field over the past 25 years. |
To date, a very limited number of peptides reported as quorum sensing inhibitors. Herein, we report the synthesis and evaluation of a series of β-turn mimetic-based peptides as potent quorum sensing inhibitors and antibiofilm formation. In this series, peptides P1, P4, and P5 showed very promising anti-quorum sensing activity on lasB-gfp reporter strain of Pseudomonas aeruginosa without affecting bacterial growth. Under our condition, these compounds also showed good anti-violacein production of Chromobacterium violaceum. In terms of antibiofilm formation, except P5, two β-turn mimetic-based peptides P1 and P4 showed maximum inhibition of 80% total biomass of Pseudomonas aeruginosa. This report provides the first β-turn mimetic-based scaffold for future drug development. |
In this paper, the authors investigate the stability and stick-slip motion of a friction-induced vibrating system placed on a belt moving at constant velocity using two-state model with consideration of dwell-time effect. The two-state model can be considered as an extension of the LuGre model because it can capture both Stribeck and dwell-time effects in the case of near-zero relative motion velocity between two surfaces. The previously known Stribeck effect is that the friction force decreases as the relative velocity increases in the near-zero range, while the dwell-time effect exhibits that the friction force increases as two surfaces are kept in contact for a certain time. With new effect of dwell-time, properties of stick-slip motion are explored in detail, including the equil... |
We theoretically investigate high-pressure effects on the atomic dynamics of metallic glasses. The theory predicts compression-induced rejuvenation and the resulting strain hardening that have been recently observed in metallic glasses. Structural relaxation under pressure is mainly governed by local cage dynamics. The external pressure restricts the dynamical constraints and slows down the atomic mobility. In addition, the compression induces a rejuvenated metastable state (local minimum) at a higher energy in the free-energy landscape. Thus, compressed metallic glasses can rejuvenate and the corresponding relaxation is reversible. This behavior leads to strain hardening in mechanical deformation experiments. Theoretical predictions agree well with experiments. |
We investigate the impact dynamics of a single wet agglomerate composed of primary spherical particles impacting a flat plane by using three-dimensional discrete element method simulations. The primary particle is assumed to be rigid and interacted with its near-neighboring particles by introducing approximate analytical expressions of capillary cohesion forces and lubrication forces induced from the liquid in addition to their elastic and frictional interactions. The paper analyzes the mechanical strength, the deformation, and the connectivity of wet particle agglomerate during the impact as well as in its early-stage impact and the final-stage deposition. We show that the mechanical strength, deformation, and connectivity of granule strongly depend on the key parameters (the liqui... |
2014 marked a rising public commitment to universal health coverage in Vietnam to eliminate the financial burden for patients, but there are lots of hindrances. It is evident that patients met difficulties to validate their insurances, so health insurance does not significantly address out-of-pocket payments issues. Furthermore, the unequal geographical distribution of hospitals in Vietnam has created an inequality between non-residing patients and residing patients; the former usually pay more. This calls into question how the validity of healthcare insurance and patient’s residence could be related to patient’s financial status and their satisfaction with health insurance |
The trial was feasible. The promising results of the study suggest that further testing of self-acupressure is warranted to inform its effectiveness on the targeted symptom cluster in patients with cancer. A placebo effect was evident alongside therapeutic effects. |
