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1.
J Org Chem ; 88(21): 15142-15150, 2023 Nov 03.
Article in English | MEDLINE | ID: mdl-37824414

ABSTRACT

The first total synthesis of 19-nordigitoxigenin, an aglycon of antiroside Y, has been achieved. The key steps of our synthesis are (i) construction of the 19-norsteroid ring system via a Mizoroki-Heck reaction between a bromoanisole corresponding to the A-ring and cyclic alkene incorporating the CD-rings, followed by a Friedel-Crafts-type cyclodehydration, and (ii) incorporation of the butenolide moiety at C17 via a silyl-tethered radical cyclization and subsequent ozone oxidation.

2.
Elife ; 92020 11 10.
Article in English | MEDLINE | ID: mdl-33168136

ABSTRACT

Here, we have developed DIAMonDS (Drosophila Individual Activity Monitoring and Detection System) comprising time-lapse imaging by a charge-coupled device (CCD) flatbed scanner and Sapphire, a novel algorithm and web application. DIAMonDS automatically and sequentially identified the transition time points of multiple life cycle events such as pupariation, eclosion, and death in individual flies at high temporal resolution and on a large scale. DIAMonDS performed simultaneous multiple scans to measure individual deaths (≤1152 flies per scanner) and pupariation and eclosion timings (≤288 flies per scanner) under various chemical exposures, environmental conditions, and genetic backgrounds. DIAMonDS correctly identified 74-85% of the pupariation and eclosion events and ~ 92% of the death events within ± 10 scanning frames. This system is a powerful tool for studying the influences of genetic and environmental factors on fruit flies and efficient, high-throughput genetic and chemical screening in drug discovery.


Subject(s)
Drosophila melanogaster/physiology , Animals , Drosophila melanogaster/growth & development , Female , Life Cycle Stages , Male , Monitoring, Physiologic/methods , Movement , Time-Lapse Imaging
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