55395-01-2

Upstream product

• 55929-05-0 3,4'-di-O-methyl-8-(3-methyl-2-butenyl)kaempferol 
• 38226-86-7 3,5-dihydroxy-2-(4-methoxyphenyl)-8,8-dimethyl-9,10-dihydro-8H-pyrano[2,3-f]chromen-4-one 
• 77-78-1 dimethyl sulfate 
• 118525-40-9 icaritin 

Downstream Products

• 55395-02-3 3,5,4'-trimethoxy-6'',6''-dimethyldihydropyrano<2'',3'':7,8>flavone 

Relevant academic research and scientific papers

Selective alkylation of β-anhydroicaritine and their biological evaluation on anticancer

A convenient and selective alkylation of icaritin has been developed. The methodology involved initial formation of β-anhydroicaritine (3) under acidic conditions followed by selective methylation at the C-3 position and then alkylation at C-5 position. Several alkylated β-anhydroicaritine derivatives were synthesised using this methodology. These newly synthesised derivatives, especially the compounds 5b, 5c and 5j, significantly suppressed cell proliferation when tested against cancer cell lines in?vitro. Compound 5j (R = Bn) exhibited a competitive inhibition against MCF7 in?vivo compared to tamoxifen.

5-substituted icaritin derivative and anti-tumor application thereof

The invention provides a 5-substituted icaritin derivative as shown in a structural formula 4, and a preparation method and anti-tumor application thereof. Activity tests prove that the 5-substitutedicaritin derivative as shown in 4 is designed and synthesized in the invention, is a suitable anti-tumor candidate drug, and especially can be used as an anti-liver cancer candidate drug, an anti-colon cancer candidate drug, an anti-lung cancer candidate drug and an anti-colon cancer candidate drug. Besides, the preparation method of the 5-substituted icaritin derivative is high in synthetic routeyield and easy to operate and implement.