Yoshida, Masahito published the artcileStructure-activity relationship study on Col-003, a protein-protein interaction inhibitor between collagen and Hsp47, Recommanded Product: 5-Bromo-3-chloro-2-hydroxybenzaldehyde, the publication is Chemical & Pharmaceutical Bulletin (2020), 68(3), 220-226, database is CAplus and MEDLINE.
This study demonstrates the structure-activity relationship of Col-003, a potent collagen-heat-shock protein 47 (Hsp47) interaction inhibitor. Col-003 analogs were successfully synthesized by Pd(0)-catalyzed cross-coupling reactions of 5-bromosalicylaldehyde derivatives with alkyl-metal species, and the inhibitory activities of the synthetic analogs were evaluated using surface plasmon resonance anal. (BIAcore). We succeeded in discovering two potent inhibitors that showed 85 and 81% inhibition at a concentration of 1.9μM against the collagen-Hsp47 interaction. This indicates that elongation of an alkyl linker between two aromatic rings could considerably improve inhibitory activity due to the adjustment of a pendant Ph moiety to an appropriate position, in addition to the hydrophobic interaction with an alkyl linker moiety.
Chemical & Pharmaceutical Bulletin published new progress about 19652-33-6. 19652-33-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Phenol,Aldehyde, name is 5-Bromo-3-chloro-2-hydroxybenzaldehyde, and the molecular formula is C4H10O2, Recommanded Product: 5-Bromo-3-chloro-2-hydroxybenzaldehyde.
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