Synthesis and Biological Evaluation of Novel Thiazol-2yl-amine Derivatives as Potential Anticancer Agents

Somu, Chaithanya; Hegde, Mahesh; Kumar, Kothanahally S. Sharath; Ananda, Hanumappa; Srivastava, Mrinal; Harsha, Kachigere B.; Mohan, Chakrabhavi Dhananjaya; Ananthaswamy, Kavya; Basappa, Basappa; Raghavan, Sathees C.; Rangappa, Kanchugarakoppal S.

doi:10.2174/1570178614666170907122026

Cited by 9 publications

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The phosphatidylserine translocation to the outer leaflet of the biological membrane is the critical event observed in the cells undergoing apoptosis which can be detected using annexin V staining [47,48]. We treated UD SCC2, JMAR, YD-10B cells with 5 nM of BT for 24 h and analyzed for presence of annexin-V-positive cells and observed an augmentation of annexin-V-positive cells from 3.5% to 13.3%, 3.1% to 14.2%, and 2.4% to 12.4% compared with non-treated (NT), respectively (Figure 4B).…”

Section: Resultsmentioning

confidence: 99%

Brusatol, a Nrf2 Inhibitor Targets STAT3 Signaling Cascade in Head and Neck Squamous Cell Carcinoma

et al. 2019

Self Cite

View full text Add to dashboard Cite

STAT3 is a latent transcription factor that plays a vital role in the transmission of extracellular signal from receptors to the nucleus. It has been regarded as a master transcription factor due to its role in the regulation of a broad spectrum of genes, which can contribute to oncogenesis. Persistent activation of STAT3 and deregulation of its signaling has been observed in various human cancers including head and neck squamous cell carcinoma (HNSCC). In the present work, we identified brusatol (BT) as a potential blocker of STAT3 signaling pathway in diverse HNSCC cells. The data from the cell-based experiments suggested that BT-induced cytotoxicity and abrogated the activation of STAT3 and that of upstream kinases such as JAK1, JAK2, and Src. It reduced the levels of nuclear STAT3 and its DNA binding ability. BT treatment increased annexin-V-positive cells, promoted procaspase-3 and PARP cleavage, and downregulated the mRNA and protein expression of diverse proteins (Bcl-2, Bcl-xl, survivin) in HNSCC cells. Taken together, brusatol can function as a promising inhibitor targeting STAT3 signaling pathway in HNSCC.

show abstract

Section: Resultsmentioning

confidence: 99%