Shultz, Michael D. published the artcileStructure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases, Application of 3-(2,6-Dichlorophenyl)propanoic acid, the publication is Journal of Medicinal Chemistry (2013), 56(17), 7049-7059, database is CAplus and MEDLINE.
Tankyrases 1 and 2 are members of the poly(ADP-ribose) polymerase (PARP) family of enzymes that modulate Wnt pathway signaling. While amide- and lactam-based nicotinamide mimetics that inhibit tankyrase activity, such as XAV939, are well-known, the discovery and evaluation of a novel nicotinamide isostere that demonstrates selectivity over other PARP family members is reprted. The utilization of lipophilic efficiency-based structure-efficiency relationships (SER) to rapidly drive the evaluation of this series is demonstrated. These efforts led to a series of selective, cell-active compounds with solubility, physicochem., and in vitro properties suitable for further optimization.
Journal of Medicinal Chemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C15H19BO2, Application of 3-(2,6-Dichlorophenyl)propanoic acid.
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