106787-27-3

Upstream product

• 110814-36-3 Diphenyl α-(diethoxythiophosphinylamino)-benzylphosphonate 
• 101-02-0 triphenyl phosphite 
• 100-52-7 benzaldehyde 
• 4712-55-4 diphenyl hydrogen phosphite 

Downstream Products

• 84044-04-2 diphenyl [1-(1-amino)benzyl]phosphonate 
• 1403781-79-2 diphenyl (isothiocyanato(phenyl)methyl)phosphonate 
• 901773-70-4 (formylamino-phenyl-methyl)-phosphonic acid diphenyl ester 
• 254982-95-1 (isocyanato-phenyl-methyl)-phosphonic acid diphenyl ester 

Relevant academic research and scientific papers

A Suite of Activity-Based Probes to Dissect the KLK Activome in Drug-Resistant Prostate Cancer

Kallikrein-related peptidases (KLKs) are a family of secreted serine proteases, which form a network (the KLK activome) with an important role in proteolysis and signaling. In prostate cancer (PCa), increased KLK activity promotes tumor growth and metastasis through multiple biochemical pathways, and specific quantification and tracking of changes in the KLK activome could contribute to validation of KLKs as potential drug targets. Herein we report a technology platform based on novel activity-based probes (ABPs) and inhibitors enabling simultaneous orthogonal analysis of KLK2, KLK3, and KLK14 activity in hormone-responsive PCa cell lines and tumor homogenates. Importantly, we identifed a significant decoupling of KLK activity and abundance and suggest that KLK proteolysis should be considered as an additional parameter, along with the PSA blood test, for accurate PCa diagnosis and monitoring. Using selective inhibitors and multiplexed fluorescent activity-based protein profiling (ABPP), we dissect the KLK activome in PCa cells and show that increased KLK14 activity leads to a migratory phenotype. Furthermore, using biotinylated ABPs, we show that active KLK molecules are secreted into the bone microenvironment by PCa cells following stimulation by osteoblasts suggesting KLK-mediated signaling mechanisms could contribute to PCa metastasis to bone. Together our findings show that ABPP is a powerful approach to dissect dysregulation of the KLK activome as a promising and previously underappreciated therapeutic target in advanced PCa.

Convenient syntheses of novel 1-isothiocyano-alkylphosphonate diphenyl ester derivatives with potential biological activity

Herein, we describe a convenient method for the syntheses of novel 1-isothiocyano-alkylphosphonate diaryl ester derivatives and their antiproliferative activity. The syntheses are based on dithiocarbamates obtained in situ with the use of carbon disulfide

Synthesis of isocyanide derivatives of α-aminoalkylphosphonate diphenyl esters

This letter describes the first example of the synthesis of isocyanide derivatives of α-aminoalkylphosphonate diphenyl esters. This method produces the title compounds in high purity and in very good yields. It also permits the generation of an α-aminopho

Synthesis and bioactivities of 1,3,2-benzodiazaphosphorin-2-carboxamide 2-oxides containing α-aminophosphonate groups

In order to search for novel antitumor and antiviral agents with high activity and low toxicity, a series of 1-ethoxycarbonylmethyl-3-ethyl-1,2,3,4-tetrahydro-4-oxo-1, 3,2-benzodiazaphosphorin-2-carboxamide 2-oxides containing α-aminophosphonate groups have been designed and synthesized by a convenient one-pot procedure in good yields. The structures of products were confirmed by 1H NMR, 31P NMR, IR spectra, and elemental analyses. The bioassay results showed that some of them possess excellent anti-tobacco mosaic virus activities and exhibit higher inhibitory effects compared with that of the contrast drug 2,4-dioxyhexahydro-1,3,5-triazine.

Studies on Organophosphorus Compounds; Part XX. A Facile Synthesis of α-Amino-Substituted Benzylphosphonic and -phosphinic Acids by Use of Thiophosphoramide

A facile method for the preparation of α-amino-substituted benzylphosphonic and -phosphinic acids is reported.It consists of the reaction of O,O-diethyl or O-ethyl O-phenyl phosphoroamidothioate (1) with a substituted benzaldehyde (2) and a phosphorous or