Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy was written by Goff, Dane;Zhang, Jing;Heckrodt, Thilo;Yu, Jiaxin;Ding, Pingyu;Singh, Raj;Holland, Sacha;Li, Weiqun;Irving, Mark. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Reference of 35265-83-9 This article mentions the following:
Axl tyrosine kinase has been shown to be involved in multiple pathways contributing to tumor development, angiogenesis, and metastasis. High Axl expression has been observed in many human tumors where it appears to confer aggressive tumor behavior. Here we present several series of dual Axl-VEGF-R2 kinase inhibitors based on extensive optimization of an acyl diaminotriazole. It was hypothesized that dual inhibition of these two receptor tyrosine kinases may have a synergistic affect in inhibiting tumor angiogenesis and metastasis. One of these mols., R916562 showed comparable activity to Sunitinib in two mouse tumor xenograft models and a mouse corneal micropocket model. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9Reference of 35265-83-9).
2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Reference of 35265-83-9
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia