Synthesis and Experimental Validation of New PDI Inhibitors with Antiproliferative Activity
Joint Authors
Badolato, Mariateresa
Carullo, Gabriele
Aiello, Francesca
Garofalo, Antonio
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-9, 9 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-06-15
Country of Publication
Egypt
No. of Pages
9
Main Subjects
Abstract EN
Protein disulfide isomerase (PDI) is a member of the thioredoxin superfamily of redox enzymes.
PDI is a multifunctional protein that catalyzes disulfide bond formation, cleavage, and rearrangement in unfolded or misfolded proteins and functions as a chaperone in the endoplasmic reticulum.
Besides acting as a protein folding catalyst, several evidences have suggested that PDI can bind small molecules containing, for example, a phenolic structure, which includes the estrogenic one.
Increasing studies indicate that PDI is involved in both physiology and pathophysiology of cells and tissues and is involved in the survival and proliferation of different cancers.
Propionic acid carbamoyl methyl amides (PACMAs) showed anticancer activity in human ovarian cancer, both in vitro and in vivo, by inhibiting PDI.
The inhibition of PDI’s activity may have a therapeutic role, in various diseases, including cancer.
In the present study, we designed and synthesized a diversified small library of compounds with the aim of identifying a new class of PDI inhibitors.
Most of synthesized compounds showed a good inhibitory potency against PDI and particularly 4-methyl substituted 2,6-di-tert-butylphenol derivatives (8–10) presented an antiproliferative activity in a wide panel of human cancer cell lines, including ovarian ones.
American Psychological Association (APA)
Badolato, Mariateresa& Carullo, Gabriele& Aiello, Francesca& Garofalo, Antonio. 2017. Synthesis and Experimental Validation of New PDI Inhibitors with Antiproliferative Activity. Journal of Chemistry،Vol. 2017, no. 2017, pp.1-9.
https://search.emarefa.net/detail/BIM-1171529
Modern Language Association (MLA)
Badolato, Mariateresa…[et al.]. Synthesis and Experimental Validation of New PDI Inhibitors with Antiproliferative Activity. Journal of Chemistry No. 2017 (2017), pp.1-9.
https://search.emarefa.net/detail/BIM-1171529
American Medical Association (AMA)
Badolato, Mariateresa& Carullo, Gabriele& Aiello, Francesca& Garofalo, Antonio. Synthesis and Experimental Validation of New PDI Inhibitors with Antiproliferative Activity. Journal of Chemistry. 2017. Vol. 2017, no. 2017, pp.1-9.
https://search.emarefa.net/detail/BIM-1171529
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1171529