Title : Novel Disulfiram Derivatives as ALDH1a1-Selective Inhibitors.

Pub. Date : 2022 Jan 12

PMID : 35056791






7 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Novel Disulfiram Derivatives as ALDH1a1-Selective Inhibitors. Disulfiram aldehyde dehydrogenase 1 family member A1 Homo sapiens
2 Drugs that can inhibit ALDH1a1 include disulfiram, an FDA-approved drug to treat chronic alcoholism. Disulfiram aldehyde dehydrogenase 1 family member A1 Homo sapiens
3 Disulfiram, by carbamylation of the catalytic cysteines, irreversibly inhibits ALDH1a1 and ALDH2. Disulfiram aldehyde dehydrogenase 1 family member A1 Homo sapiens
4 Given the fact that ALDH1a1 has a larger substrate tunnel than that in ALDH2, replacing disulfiram ethyl groups with larger motifs will yield selective ALDH1a1 inhibitors. Disulfiram aldehyde dehydrogenase 1 family member A1 Homo sapiens
5 Given the fact that ALDH1a1 has a larger substrate tunnel than that in ALDH2, replacing disulfiram ethyl groups with larger motifs will yield selective ALDH1a1 inhibitors. Disulfiram aldehyde dehydrogenase 1 family member A1 Homo sapiens
6 We report herein the synthesis of new inhibitors of ALDH1a1 where (hetero)aromatic rings were introduced into the structure of disulfiram. Disulfiram aldehyde dehydrogenase 1 family member A1 Homo sapiens
7 Most of the developed compounds retained the anti-ALDH1a1 activity of disulfiram; however, they were completely devoid of inhibitory activity against ALDH2. Disulfiram aldehyde dehydrogenase 1 family member A1 Homo sapiens