6-Bromoquinazoline Derivatives as Potent Anticancer Agents: Synthesis,Cytotoxic Evaluation,and Computational Studies

A series of 6-bromoquinazoline derivatives ( 5a – j ) were synthesized. Cytotoxic effectiveness of compounds was done against two cancerous cell lines (MCF-7 and SW480) by standard MTT method. Fortunately, all of the compounds showed desirable activity in reducing the viability of the studied cancerous cell lines with IC₅₀ value in the range of 0.53–46.6 μM. Compound 5b with a fluoro substitution at meta position of the phenyl moiety showed stronger activity than cisplatin with IC₅₀=0.53–1.95 μM. Studies on the hit compound ( 5b ) through apoptosis assay illustrated that it could induce apoptosis in MCF-7 cell lines in dose dependent manner. Molecular docking study was done to investigate the detailed binding modes and interactions with EGFR as a plausible mechanism. The drug- likeness was predicted. To survey the reactivity of compounds, DFT calculation was performed. Taken together, 6-bromoquinazoline derivatives, especially 5b can be considered as hit compounds to rational drug designing as antiproliferative agents.     

Do bright-light shock exposures during breaks reduce subjective sleepiness in night workers?

Sleep and Biological Rhythms - Night work has many harmful effects on the health, efficiency and safety of workers. This study evaluates the effects of bright-light exposure (BL) on subjective...     

Computational electrode potential of a coumestan derivative: theoretical and experimental studies

Electrode potential of a coumestan derivative, an important biological molecule, in aqueous solution is computed theoretically using Self-Consistent Field (SCF) theory at the level of Hartree--Fock and employing 6-31G(d) basis set and also obtained experimentally by employing electrochemical technique of cyclic voltammetry (CV). Frequency calculations have been carried out and thermal corrections and entropies have been taken into account. Polarizable continuum model is used to describe the solvent. The theoretical and experimental values for the standard electrode potential of the studied coumestan are in excellent agreement with each other and there is only 0.001 V discrepancy between experiment and theory. The agreement mutually verifies the accuracy of experimental method and the validity of mathematical model.     

Bex,the Bacillus subtilis homolog of the essential Escherichia coli GTPase Era,is required for normal cell division and spore formation

The Bacillus subtilis bex gene complemented the defect in an Escherichia coli era mutant. The Bex protein showed 39 percent identity and 67 percent similarity to the E. coli Era GTPase. In contrast to era, bex was not essential in all strains. bex mutant cells were elongated and filled with diffuse nucleoid material. They grew slowly and exhibited severely impaired spore formation.     

Effect of prostaglandins on the in vitro steroidogenesis in human ovarian tissues

Although prostaglandins are luteolytic in some species, in $\text{in vitro}$ conditions they stimulate progesterone production in the corpus luteum (1). Apart from this effect prostaglandins may also stimulate other steps in the steroidogenic sequence e.g. corticosteroidogenesis in superfused rat adrenal glands (2) and aromatization of testosterone by perfused human placenta (3). With this possibility in view and also because of paucity of data on the effect of prostaglandins on steroidogenesis in human ovarian tissues we have been studying under $\text{in vitro}$ conditions the effect of prostaglandins on progesterone formation in human corpora lutea and on the utilization of C₂₁ steroids by the luteal and follicular compartments of the ovary. These studies are still in progress. However, the data obtained so far indicates that in addition to stimulating progesterone synthesis in the corpus luteum prostaglandins may also affect other steps in steroidogenesis in human ovarian tissues. We wish to report here in brief these preliminary results.     

Environmental Response and Genomic Regions Correlated with Rice Root Growth and Yield under Drought in the OryzaSNP Panel across Multiple Study Systems

The rapid progress in rice genotyping must be matched by advances in phenotyping. A better understanding of genetic variation in rice for drought response, root traits, and practical methods for studying them are needed. In this study, the OryzaSNP set (20 diverse genotypes that have been genotyped for SNP markers) was phenotyped in a range of field and container studies to study the diversity of rice root growth and response to drought. Of the root traits measured across more than 20 root experiments, root dry weight showed the most stable genotypic performance across studies. The environment (E) component had the strongest effect on yield and root traits. We identified genomic regions correlated with root dry weight, percent deep roots, maximum root depth, and grain yield based on a correlation analysis with the phenotypes and aus, indica, or japonica introgression regions using the SNP data. Two genomic regions were identified as hot spots in which root traits and grain yield were co-located; on chromosome 1 (39.7–40.7 Mb) and on chromosome 8 (20.3–21.9 Mb). Across experiments, the soil type/ growth medium showed more correlations with plant growth than the container dimensions. Although the correlations among studies and genetic co-location of root traits from a range of study systems points to their potential utility to represent responses in field studies, the best correlations were observed when the two setups had some similar properties. Due to the co-location of the identified genomic regions (from introgression block analysis) with QTL for a number of previously reported root and drought traits, these regions are good candidates for detailed characterization to contribute to understanding rice improvement for response to drought. This study also highlights the utility of characterizing a small set of 20 genotypes for root growth, drought response, and related genomic regions.     

The regulation of CD47-SIRPα signaling axis by microRNAs in combination with conventional cytotoxic drugs together with the help of nano-delivery: a choice for therapy?

Molecular Biology Reports - CD47, a member of the immunoglobulin superfamily, is an important “Don’t Eat-Me” signal in phagocytosis process [clearance of apoptotic cells] as well...     

Human adipose derived stem cell exosomes enhance the neural differentiation of PC12 cells

Molecular Biology Reports - Human adipose stem cells (hADSCs) are proper cell sources for tissue regeneration. They mainly mediate their therapeutic effects through paracrine factors as exosomes....