1612891-75-4

Upstream product

• 76554-28-4 C₂₀H₂₀O₅ 
• 1167577-15-2 C₂₀H₁₈O₅ 
• 40663-68-1 4-(2-propenyloxy)benzaldehyde 
• 3445-11-2 1-(2-hydroxyethyl)-2-pyrrolidinone 
• 16290-50-9 3-(4-hydroxyphenyl)-5,7-dimethoxy-4H-chromen-4-one 
• 90-24-4 2-hydroxy-4,6-dimethoxyacetophenone 

Relevant academic research and scientific papers

APIGENIN ANALOGS, COMPOSITIONS, AND METHODS RELATED THERETO

Certain embodiments are directed to apigenin analogues or derivatives. In certain aspects, the derivatives are developed as cystathionine-beta-synthase (CBS) inhibitors. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents. Certain embodiments are directed methods of treating or compositions used to treat fibrosis and cancers. In certain aspects one or more compounds described herein can be administered to a subject to treat pancreatic fibrosis, liver fibrosis, pancreatic cancer, colon cancer, breast cancer, brain tumors, head/neck cancer, prostate and lung cancers as well as other inflammation.

Design, synthesis, and characterization of novel apigenin analogues that suppress pancreatic stellate cell proliferation in vitro and associated pancreatic fibrosis in vivo

Accumulating evidence suggests that activated pancreatic stellate cells (PSC) play an important role in chronic pancreatitis (CP), and inhibition of the activated PSC is considered as a potential strategy for the treatment and prevention of CP. Herein, we disclose our findings that apigenin and its novel analogues suppress the proliferation and induce apoptosis in PSC, which reduce the PSC-mediated fibrosis in CP. Chemical modifications of apigenin have been directed to build a focused library of O-alkylamino-tethered apigenin derivatives at 4′-O position of the ring C with the attempt to enhance the potency and drug-like properties including aqueous solubility. A number of compounds such as 14, 16, and 24 exhibited potent antiproliferative effects as well as improved aqueous solubility. Intriguingly, apigenin, new analogues 23 and 24 displayed significant efficacy to reduce pancreatic fibrosis even at a low dose of 0.5 mg/kg in our proof-of-concept study using a preclinical in vivo mouse model of CP.