Synthesis, Antimicrobial - Cytotoxic Evaluation, and Molecular Docking Studies of Quinolin-2-one Hydrazones Containing Nitrophenyl or Isonicotinoyl/Nicotinoyl Moiety.

By applying the hybrid molecular strategy, in this study, we reported the synthesis of fifteen quinolin-2-one hydrazones containing nitrophenyl or nicotinonyl/isonicotinoyl moiety, followed by in vitro and in silico evaluations of their potential antimicrobial and anticancer activities. In vitro antimicrobial evaluation of the target compounds on seven pathogenic strains, applying the broth microdilution method, revealed that compound 4a demonstrated the most potential antifungal activity against C. albicans (MIC 512 μg mL) and C.

Phytochemistry and Cytotoxic Activity of Pericarp on MDA-MB-468 Cell Lines.

The extracts of pericarp were investigated on the MDA-MB-468, a breast cancer cell line, at desired concentration (1-50 μg/mL). The results showed that the dichloromethane (DCM) extract exhibited the strongest toxicity and was carried out subsequently. A total of nine compounds were isolated from the DCM extract using column chromatography and recrystallization, of which their structures were determined.

Design, synthesis, in vitro and in silico evaluation of anti-colorectal cancer activity of curcumin analogues containing 1,3-diphenyl-1H-pyrazole targeting EGFR tyrosine kinase.

Recent studies have shown that monocarbonyl analogues of curcumin (MACs) and 1H-pyrazole heterocycle both demonstrated promising anticancer activities, in which several compounds containing these scaffolds could target EGFR. In this research, 24 curcumin analogues containing 1H-pyrazole (a1-f4) were synthesized and characterized by using modern spectroscopic techniques. Firstly, synthetic MACs were screened for cytotoxicity against human cancer cell lines such as SW480, MDA-MB-231 and A549, from which the 10 most potential cytotoxic compounds were identified and selected.

Synthesis, Biological Evaluation, and Molecular Modeling Studies of 1-Aryl-1-pyrazole-Fused Curcumin Analogues as Anticancer Agents.

Addressing the growing burden of cancer and the shortcomings of chemotherapy in cancer treatment are the current research goals. Research to overcome the limitations of curcumin and to improve its anticancer activity via its heterocycle-fused monocarbonyl analogues (MACs) has immense potential. In this study, 32 asymmetric MACs fused with 1-aryl-1-pyrazole () were synthesized and characterized to develop new curcumin analogues.

Transgenerational exposure to marine heatwaves ameliorates the lethal effect on tropical copepods regardless of predation stress.

Marine heatwaves (MHWs) are emerging as a severe stressor in marine ecosystems. Extreme warm sea surface temperatures during MHWs often exceed the optimal thermal range for more than one generation of tropical coastal zooplankton. However, it is relatively unknown whether transgenerational plasticity (TGP) to MHWs may shape the offspring's fitness, particularly in an ecologically relevant context with biotic interactions such as predation stress.

Parental exposures increase the vulnerability of copepod offspring to copper and a simulated marine heatwave.

Extreme temperatures from marine heatwaves (MHWs) and pollution are dominant stressors in tropical marine ecosystems. However, we know little about the role of transgenerational effects of metals and MHWs in shaping the offspring's vulnerability to these stressors. We addressed this fundamental knowledge gap by exposing the planktonic copepod Pseudodiaptomus incisus to copper (Cu: control, 15 and 60 μg L) under 2 temperatures (30 and a simulated marine heatwave at 34 °C) in the first generation (F1) and 16 treatments in F2: offspring from each of 4 F1 conditions (control or 15 μg Cu L × 30 or 34 °C) was reared in 4 F2 conditions (control or 15 μg Cu L × 30 or 34 °C).

Interactive effects of extreme temperature and a widespread coastal metal contaminant reduce the fitness of a common tropical copepod across generations.

Tropical coastal areas are increasingly exposed to temperature extremes from marine heatwaves and contaminants from anthropogenic activities. The interactive effects of these environmental changes on marine life are understudied. We investigated the direct and cross-generational effects of copper (Cu) on F0 and F1 generations of the common tropical copepod Pseudodiaptomus annandalei under extreme temperatures (30 and 34 °C).

Molecular Docking Studies of Glycyrrhetinic Acid Derivatives as Anti- Colorectal Cancer Agents.

Background: In this study, the anti-colorectal cancer (CRC) activities of 40 glycyrrhetinic acid derivatives were proposed and evaluated by the molecular docking method, which allowed the flexibility of both ligand-receptor, with twelve CRC-related targets.

Methods: The proposed derivatives, which clearly distinguish isomers at position 18 as well as the different tautomers, were divided into five groups, including (1) glycyrrhetinic acid and its oxidation derivatives, (2) glycoside derivatives, (3) 3β-amine derivatives, (4) five-membered heterocyclic ring-combined derivatives, and (5) six-membered heterocyclic ring-combined derivatives.

Results: Finally, four out of twelve proposed targets related to CRC with good binding affinities to the proposed glycyrrhetinic acid derivatives were selected, including Epidermal Growth Factor Receptor (EGFR), Focal Adhesion Kinase (FAK), Lactate Dehydrogenase A (LDHA), and Thymidylate Synthase (TS).

Author Correction: Extreme temperature impairs growth and productivity in a common tropical marine copepod.

An amendment to this paper has been published and can be accessed via a link at the top of the paper.

Extreme temperature impairs growth and productivity in a common tropical marine copepod.

Shallow, tropical marine ecosystems provide essential ecosystem goods and services, but it is unknown how these ecosystems will respond to the increased exposure to the temperature extremes that are likely to become more common as climate change progresses. To address this issue, we tracked the fitness and productivity of a key zooplankton species, the copepod Pseudodiaptomus annandalei, acclimated at two temperatures (30 and 34 °C) over three generations. 30 °C is the mean temperature in the shallow water of the coastal regions in Southeast Asia, while 34 °C simulated a temperature extreme that occurs frequently during the summer period.

Attitudes of Canadian psychiatry residents if mentally ill: awareness, barriers to disclosure, and help-seeking preferences.

Background: The medical culture is defined by mental illness stigma, non-disclosure, and avoidance of professional treatment. Little research has explored attitudes and help-seeking behaviors of psychiatry trainees if they were to become mentally ill.

Method: Psychiatry residents ( = 106) from training centres across Ontario, Canada completed a postal survey on their attitudes, barriers to disclosure, and help-seeking preferences in the context of hypothetically becoming mentally ill.