Milne, Kirsty published the artcileA fragment-like approach to PYCR1 inhibition, Related Products of bromides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(18), 2626-2631, database is CAplus and MEDLINE.
Pyrroline-5-carboxylate reductase 1 (PYCR1) is the final enzyme involved in the biosynthesis of proline and has been found to be upregulated in various forms of cancer. Due to the role of proline in maintaining the redox balance of cells and preventing apoptosis, PYCR1 is emerging as an attractive oncol. target. Previous PYCR1 knockout studies led to a reduction in tumor growth. Accordingly, a small mol. inhibitor of PYCR1 could lead to new treatments for cancer, and a focused screening effort identified pargyline as a fragment-like hit. Herein the design and synthesis of the first tool compounds as PYCR1 inhibitors, derived from pargyline, which were assayed to assess their ability to attenuate the production of proline, are reported. Structural activity studies have revealed the key determinants of activity, with the most potent compound, 4-bromobenzyl(propargyl)methylamine, showing improved activity in vitro in enzyme (IC50 = 8.8μM) and pathway relevant effects in cell-based assays.
Bioorganic & Medicinal Chemistry Letters published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Related Products of bromides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary