951892-07-2Relevant academic research and scientific papers
Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L
Parker, Erica N.,Odutola, Samuel O.,Wang, Yifan,Strecker, Tracy E.,Mukherjee, Rajeswari,Shi, Zhe,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
, p. 1304 - 1310 (2017)
The magnitude of expression of cathepsin L, often upregulated in the tumor microenvironment, correlates with the invasive and metastatic nature of certain tumors. Inhibition of cathepsin L represents an emerging strategy for the treatment of metastatic ca
COMPOSITIONS AND METHODS FOR INHIBITION OF CATHEPSINS
-
, (2017/03/14)
This present disclosure is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin L, cathepsin K, and/or cathepsin B, will be therapeutically useful.
Exploring the substituent effects on a novel series of C1′-dimethyl-aryl Δ8-tetrahydrocannabinol analogs
Krishnamurthy, Mathangi,Gurley, Steven,Moore II, Bob M.
, p. 6489 - 6500 (2008/12/21)
The synthesis and characterization of novel C1′-phenyl-substituted Δ8-THC analogs were previously reported by our laboratory. Within this small series of compounds, the C1′-dimethyl phenyl group was found to impart 13.5-fold selectivity for the CB2 receptor with a Ki 0.91 nM. The current study expands on the previous report by evaluating the effects of aromatic ring substitution on CB1 and CB2 receptor subtype binding and selectivity. The ring substituents synthesized in this study include aliphatic, halogen, nitrile, and acetamido functional groups. In addition, the isosteric replacement of the phenyl group by thiophene was evaluated. The anti-glioma activities of selected compounds were evaluated in vitro and compared to the lead compound 2.
