Identification, synthesis and structure assignment of two impurities of Erlotinib, a drug used for the treatment of some types of cancer.

Morales-Vilchis, María Guadalupe; Flores-Sánchez, Patricia; Escalante, Jaime

doi:10.29356/jmcs.v63i1.714

Cited by 1 publication

(1 citation statement)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A summary of selected spectroscopic properties of TKI’s is collected in Table 1 [ 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 ].…”

Section: Fluorescence Tyrosine-kinase Inhibitors and Beyondmentioning

confidence: 99%

Intrinsically Fluorescent Anti-Cancer Drugs

Kabir

Wang

Clayton

2022

Biology

View full text Add to dashboard Cite

At present, about one-third of the total protein targets in the pharmaceutical research sector are kinase-based. While kinases have been attractive targets to combat many diseases, including cancer, selective kinase inhibition has been challenging, because of the high degree of structural homology in the active site where many kinase inhibitors bind. Despite efficacy as cancer drugs, kinase inhibitors can exhibit limited target specificity and rationalizing their target profiles in the context of precise molecular mechanisms or rearrangements is a major challenge for the field. Spectroscopic approaches such as infrared, Raman, NMR and fluorescence have the potential to provide significant insights into drug-target and drug-non-target interactions because of sensitivity to molecular environment. This review places a spotlight on the significance of fluorescence for extracting information related to structural properties, discovery of hidden conformers in solution and in target-bound state, binding properties (e.g., location of binding sites, hydrogen-bonding, hydrophobicity), kinetics as well as dynamics of kinase inhibitors. It is concluded that the information gleaned from an understanding of the intrinsic fluorescence from these classes of drugs may aid in the development of future drugs with improved side-effects and less disease resistance.

show abstract

“…A summary of selected spectroscopic properties of TKI’s is collected in Table 1 [ 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 ].…”

Section: Fluorescence Tyrosine-kinase Inhibitors and Beyondmentioning

confidence: 99%