2022
DOI: 10.1021/acs.jmedchem.1c01800
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Probing Embryonic Development Enables the Discovery of Unique Small-Molecule Bone Morphogenetic Protein Potentiators

Abstract: We report on the feasibility to harness embryonic development in vitro for the identification of small-molecule cytokine mimetics and signaling activators. Here, a phenotypic, target-agnostic, high-throughput assay is presented that probes bone morphogenetic protein (BMP) signaling during mesodermal patterning of embryonic stem cells. The temporal discrimination of BMP- and transforming growth factor-β (TGFβ)-driven stages of cardiomyogenesis underpins a selective, authentic orchestration of BMP cues that can … Show more

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Cited by 8 publications
(46 citation statements)
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“…9-Chloro-2-furan-2-yl-6H-5,6-dihydro [1,2,4]triazolo [1,5-c]quinazoline-5-one (4a). 24,25 The general procedure was performed with 2.76 g of 3a (12.29 mmol, 1.0 equiv) and 1.55 g of furan-2carbohydrazide (12.29 mmol, 1.0 equiv) in 20 mL of NMP for 18 h to yield 4a as a light-brown solid (3.40 g, 97%).…”
Section: Journal Ofmentioning
confidence: 99%
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“…9-Chloro-2-furan-2-yl-6H-5,6-dihydro [1,2,4]triazolo [1,5-c]quinazoline-5-one (4a). 24,25 The general procedure was performed with 2.76 g of 3a (12.29 mmol, 1.0 equiv) and 1.55 g of furan-2carbohydrazide (12.29 mmol, 1.0 equiv) in 20 mL of NMP for 18 h to yield 4a as a light-brown solid (3.40 g, 97%).…”
Section: Journal Ofmentioning
confidence: 99%
“…Note: The 1 H NMR spectral data differed slightly from the literature reported values. 25 9-Bromo-2-furan-2-yl-6H-5,6-dihydro [1,2,4]triazolo [1,5-c]quinazoline-5-one (4b). The general procedure was performed with 1.88 g of 3b (6.99 mmol, 1.0 equiv) and 0.88 g of furan-2carbohydrazide (6.98 mmol, 1.0 equiv) in 15 mL of NMP for 18 h to yield 4b as a brown solid (2.31 g, 100%).…”
Section: Journal Ofmentioning
confidence: 99%
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