Abstract
Aurora-A kinase, a key mitosis regulator, is expressed in a cell cycle-dependent manner and has an essential role in maintaining chromosomal stability and the normal progression of the cell through mitosis. Aurora-A kinase is overexpressed in many malignant solid tumors, such as breast, ovarian, colon, and pancreatic cancers. Thus, inhibiting Aurora-A kinase activity is a promising approach for cancer treatment. Here, new triazole derivatives were designed as bioisosteric analogues of the known inhibitor JNJ-7706621. The new compounds showed interesting inhibitory activity against Aurora-A kinase, as attested by IC50s in the low to submicromolar range.
Highlights
Most types of cancers are characterized by genomic instability, which can range fromMost types of cancers are characterized by genomic chromosome instability, which can range from subtle DNA sequence changes to gene amplification, translocations, and subtleDNA sequence changes to gene amplification, chromosome translocations, and alalterations in chromosome numbers [1,2]
NJ-7706621 promoted reversal of resistance radioimmunoradioimmunotherapy in DLBCthe lymphoma cell lines [8].toInCD37-targeted the present study, we report the synthesis of JNJ-7706621 analogues
We report the synthesis of isosteric approach where amide bond of were
Summary
Most types of cancers are characterized by genomic instability, which can range from. Most types of cancers are characterized by genomic chromosome instability, which can range from subtle DNA sequence changes to gene amplification, translocations, and subtle. Aurora-A kinasechromosomal is expressed in a cell cycle-dependent and has an essential role in maintaining stability and the normalmanner progression of the cell through in maintaining chromosomal and the normal progression the cell through mitosis [3]. NJ-7706621 promoted reversal of resistance radioimmunoradioimmunotherapy in DLBCthe lymphoma cell lines [8].toInCD37-targeted the present study, we report the synthesis of JNJ-7706621 analogues. These derivatives were designed using an therapy in DLBC lymphoma cell lines [8].(1).
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
