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1.
Biosci Biotechnol Biochem ; 85(1): 160-167, 2021 Jan 07.
Artigo em Inglês | MEDLINE | ID: mdl-33577660

RESUMO

UTKO1 is a synthetic analog of a natural tumor cell migration inhibitor, moverastin, isolated from microbial extracts of Aspergillus sp. 7720. UTKO1 was initially developed as a mixture of the stereoisomers. In this study, a concise and unified synthesis of the 4 optically active stereoisomers of UTKO1 was achieved from a known optically pure dihydro-α-ionone through a 5-step sequence. The key transformation in the synthesis was a Nozaki-Hiyama-Kishi (NHK) reaction between an optically active enoltriflate and a known aldehyde to install the chiral allylic hydroxy group at C2'. Simple chromatographic separation of the 2 diastereomers with regard to the allylic hydroxy group was possible by the derivatization into the corresponding acetals with Nemoto's optical resolution reagent, (S)- or (R)-5-allyl-2-oxabicyclo[3.3.0]octene (ALBO). All 4 synthetic stereoisomers of UTKO1 exhibited comparable tumor cell migration inhibitory activity.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Benzaldeídos/química , Benzaldeídos/síntese química , Benzaldeídos/farmacologia , Movimento Celular/efeitos dos fármacos , Cicloexanonas/química , Desenho de Fármacos , Antineoplásicos/química , Linhagem Celular Tumoral , Técnicas de Química Sintética , Humanos
2.
Asian Spine J ; 11(6): 975-980, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29279754

RESUMO

STUDY DESIGN: Cross-sectional study. PURPOSE: The purpose of this study was to evaluate the correlation between pelvic tilt (PT) and the sacro-femoral-pubic (SFP) angle, which is easier to identify than PT, in middle-aged and elderly Asian subjects from the general population. OVERVIEW OF LITERATURE: Measuring PT is important in the diagnosis and treatment of adult spinal deformity. However, identifying femoral heads, which are necessary to determine PT, using sagittal radiographs is often difficult. METHODS: Standing coronal and sagittal pelvic radiographs of individuals aged more than 50 years were taken during a local medical examination. The subjects were divided into female, male, and total groups at the time of evaluation. Linear regression analysis was performed to investigate the relationship between PT and the SFP angle, which were obtained from the X-rays. RESULTS: The present study included 291 subjects. There were no statistically significant differences between the left and right SFP angles, and there was gender difference regarding the SFP angle. However, a gender difference was observed regarding PT. The correlation between PT and the SFP angle was substantiated in each group. Pearson's correlation coefficients between PT and the SFP angle in the total, female, and male groups were 0.696, 0.853, and 0.619, respectively. In the linear regression analysis, PT was calculated as follows: PT=60.1-0.77×(SFP angle) in the total group, PT=62.8-0.80×(SFP angle) in the female group, and PT=51.5-0.64×(SFP angle) in the male group. CONCLUSIONS: A significant correlation between PT and the SFP angle was observed in middle-aged and elderly Asian subjects from the general population.

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