60759-02-6Relevant academic research and scientific papers
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor
Jung, Hui Jin,Nam, Eun Hye,Park, Jin Young,Ghosh, Prithwish,Kim, In Su
supporting information, (2021/02/26)
Fibroblast activation protein (FAP) belongs to the family of prolyl-specific serine proteases and displays both exopeptidase and endopeptidase activities. FAP expression is undetectable in most normal adult tissues, but is greatly upregulated in sites of tissue remodeling, which include fibrosis, inflammation and cancer. Due to its restricted expression pattern and dual enzymatic activities, FAP inhibition is investigated as a therapeutic option for several diseases. In the present study, we described the structure–activity relationship of several synthesized compounds against DPPIV and prolyl oligopeptidase (PREP). In particular, BR102910 (compound 24) showed nanomolar potency and high selectivity. Moreover, the in vivo FAP inhibition study of BR102910 (compound 24) using C57BL/6J mice demonstrated exceptional profiles and satisfactory FAP inhibition efficacy. Based on excellent in vitro and in vivo profiles, the potential of BR102910 (compound 24) as a lead candidate for the treatment of type 2 diabetes is considered.
Cytotoxic 1,3-thiazole and 1,2,4-thiadiazole alkaloids from Penicillium oxalicum: Structural elucidation and total synthesis
Yang, Zheng,Huang, Nianyu,Xu, Bang,Huang, Wenfeng,Xie, Tianpeng,Cheng, Fan,Zou, Kun
, (2016/04/20)
Two new thiazole and thiadiazole alkaloids, penicilliumthiamine A and B (2 and 3), were isolated from the culture broth of Penicillium oxalicum, a fungus found in Acrida cinerea. Their structures were elucidated mainly by spectroscopic analysis, total synthesis and X-ray crystallographic analysis. Biological evaluations indicated that compound 1, 3a and 3 exhibit potent cytotoxicity against different cancer cell lines through inhibiting the phosphorylation of AKT/PKB (Ser 473), one of important cancer drugs target.
A mild and versatile synthesis of thioamides
Mahammed,Jayashankara,Premsai Rai,Mohana Raju,Arunachalam
experimental part, p. 2338 - 2340 (2009/12/08)
Aliphatic and aromatic nitriles react with thioacetic acid in the presence of calcium hydride to give the corresponding thioamides in good to excellent yields. The examples studied include haloaryl nitriles in which the halogen is facile towards SNAr reactions under other conditions. Georg Thieme Verlag Stuttgart.
Phosphorus pentasulfide: A mild and versatile reagent for the preparation of thioamides from nitriles
Kaboudin, Babak,Elhamifar, Dawood
, p. 224 - 226 (2007/10/03)
A simple, efficient, and new method has been developed for the synthesis of thioamides from nitriles. The reaction of a variety of aromatic and aliphatic nitriles in the presence of phosphorus pentasulfide afforded the corresponding thioamides in high yields. This method is easy, rapid, and high-yielding for the synthesis of thioamides from nitriles. Georg Thieme Verlag Stuttgart.
