A range of tamoxifen derivatives substituted in the 4-position of the 1-phenyl ring are described. The key steps in the synthesis of 4-iodo-, 4-bromo-, and 4-(methylthio)tamoxifen were reactions of 1,2-diarylbutanones with the (4-halogenophenyl)lithium or [4-(methylthio)phenyl]magnesium bromide. Oxidized precursors of 4-(methylthio)tamoxifen were used to prepare the methylsulfinyl and methylsulfonyl derivatives. Further derivatives (formyl, hydroxymethyl, oxirane, mercapto) were prepared from 4-bromotamoxifen via the 4-lithio derivative. Several of the derivatives (Br, I, SMe, SOMe, SO2Me, oxirane, CHO, CH2OH) displayed a higher affinity for estrogen receptors (ER) of calf uterine cytosol than did tamoxifen, but there was no relationship between affinity to ER and the ability to inhibit the growth of the MCF-7 breast cancer cell line in vitro.

The coronavirus disease 2019 (COVID-19) pandemic has caused a surge in mental health problems across the United States, and some reports suggest a more severe impact for racial and ethnic minorities. The present study was conducted to gain a preliminary understanding of the mental health consequences of the COVID-19 pandemic specifically for dreamers, i.e., undocumented immigrants who entered the U.S. as minors. A population of about 150 dreamers currently enrolled at a public university in Delaware were invited to participate in an online survey. The survey contained questions about demographics, mental health, academics, immigration, COVID-19 infection, and unemployment, in addition to mental health screens for anxiety (GAD-7), depression (PHQ-9), and stress (PSS-10). In total, 109 dreamers completed the survey. We observed remarkably high clinical levels of anxiety and depression: 47% of the dreamers met the clinical cutoff for anxiety, 63% met the cutoff for depression, and 67% (2 in 3) met the cutoff for anxiety and/or depression. Rates of anxiety and depression in our sample were significantly higher than those recently reported for college students overall, suggesting that dreamers may be experiencing a more severe mental health impact of the COVID-19 pandemic. We also found that pandemic-induced concerns about finances, COVID-19 infection, immigration, and unemployment (among other factors) were associated with greater anxiety, stress, and depression among the dreamers in our sample. The present findings are consistent with recent predictions by social scientists that the COVID-19 pandemic would have a disproportionately negative impact on the mental health of undocumented immigrants.

The effect of 60 h without sleep upon maximal oxygen intake was examined in 12 young women, using a cycle ergometer protocol. The arousal of the subjects was maintained by requiring the performance of a sequence of cognitive tasks throughout the experimental period. Well-defined oxygen intake plateaus were obtained both before and after sleep deprivation, and no change of maximal oxygen intake was observed immediately following sleep deprivation. The endurance time for exhausting exercise also remained unchanged, as did such markers of aerobic performance as peak exercise ventilation, peak heart rate, peak respiratory gas exchange ratio, and peak blood lactate. However, as in an earlier study of sleep deprivation with male subjects (in which a decrease of treadmill maximal oxygen intake was observed), the formula of Dill and Costill (4) indicated the development of a substantial (11.6%) increase of estimated plasma volume percentage with corresponding decreases in hematocrit and red cell count. Possible factors sustaining maximal oxygen intake under the conditions of the present experiment include (1) maintained arousal of the subjects with no decrease in peak exercise ventilation or the related respiratory work and (2) use of a cycle ergometer rather than a treadmill test with possible concurrent differences in the impact of hematocrit levels and plasma volume expansion upon peak cardiac output and thus oxygen delivery to the working muscles.

Resting and submaximal isometric exercise 31P magnetic resonance spectroscopy (MRS) was carried out on 7 endurance-trained males (26.0 +/- 3 yrs) and 7 sedentary males (27.0 +/- 4 yrs). Spectral analysis provided peak areas of phosphocreatine (PCr), inorganic phosphate (Pi), adenosine triphosphate (ATP), and the chemical shift of Pi relative to PCr. The ratio of PCr/Pi was moderately lower during rest (preexercise p = .13, postexercise p = .18), and significantly higher during exercise (p < .05) in the trained subjects. Intracellular pH patterns were the same for both groups; a transient alkalosis was observed at the onset of exercise with a return to resting levels after 2 min. Differences suggest improved ATP resynthesis rate in the trained subjects during exercise. Intracellular pH changes can be attributed to the utilization of hydrogen ions that accompany PCr hydrolysis during work. The findings are congruent with previous reports indicating a superior oxidative capacity in trained skeletal muscle.

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