852333-36-9

Upstream product

• 110-91-8 morpholine 
• 50-00-0 formaldehyd 
• 491-67-8 5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4-one 
• 21967-41-9 baicalin 

Relevant academic research and scientific papers

Synthesis and structure confirmation of 7-ester-8-aminomethylene-substituted baicalein derivatives

Twelve baicalein derivatives, derivatized with 7-ester and 8-aminomethylene groups, were synthesized as cyclin-dependent kinase 1 (CDK1) inhibitors, by the addition of one of four secondary amines to C-8, using the Mannich reaction, followed by mono-esterification with one of three carboxylic acids. Analysis by 1H-, 13C-NMR, and HMBC spectra, as well as a chemical test, confirmed that the esterification occurred at the 7-phenolic hydroxyl position of baicalein but not at the 5- or 6-positions.

Design, synthesis, and primary activity assays of baicalein derivatives as cyclin-dependent kinase 1 inhibitors

Malignant tumor is a disease with high mortality. Traditional treatment methods have many disadvantages, such as side-effects, drug resistance. Because cyclin-dependent kinase 1 (CDK1) plays an indispensable role in cell cycle regulation, it became an att

Baicalein or derivative thereof, preparation method and application of baicalein or derivative of baicalein

The invention discloses baicalein or a derivative thereof. The structure is shown in the specification, wherein R1 is hydrogen, alkyl, substituted or unsubstituted aryl; R2 is hydrogen, halogen, alkyl, alkoxy, substituted or unsubstituted amino, and subst

Baicalein derivative as well as preparation method and application thereof (by machine translation)

The invention discloses a baicalein derivative, structure as shown in the specification : In-flight, R1 A hydrogen, alkyl, is substituted or unsubstituted aryl ;R. 2 The hydrogen, halogen, alkyl, alkoxy, may be substituted or unsubst

Flavonoid derivative as well as preparation method and identification method thereof

The invention discloses a flavonoid derivative, which has structure formulas shown as a general formula (I) and a general formula (II) as in the description, wherein R1 is alkyl or cyclo alkane; R2 isalkyl or cyclo alkane; R1, R2 and nitrogen atoms form cycloaliphatic ring or heterocycle; R3 is alkyl or aryl or aralkyl; the value of n is 1 to 10. The invention also discloses a preparation methodand an identification method of the flavonoid derivative.

Nitrogen-containing flavonoid analogues as CDK1/cyclin B inhibitors: Synthesis, SAR analysis, and biological activity

A series of nitrogen-containing flavonoid analogues were designed and synthesized by Mannich reaction, and screened for the inhibitory activities of cyclin-dependent kinases using a FRET-based biochemical assay method. The results showed that C-8 nitrogen-containing baicalein analogues 3a-3f exhibited potent CDK1/Cyclin B inhibitory activities. 5,6,7-Trihydroxy-8-(dimethylaminomethyl)-2-phenyl-4H-chromen-4-one 3a, 5,6,7-trihydroxy-8-(pyrrolid inylmethyl)-2-phenyl-4H-chromen-4-one 3b, and 5,6,7-trihydroxy-8-(piperidinylmethyl)-2-phenyl-4H-chromen-4-one 3c (IC50 1.05-1.28 μM) were about sixfold more potent than baicalein 2 (IC50 6.53 μM). 5,6,7-Trihydroxy-8-(morpholinomethyl)-2-phenyl-4H-chromen-4-one 3d, 5,6,7-trihydroxy-8-(thiomorpholinomethy)-2-phenyl-4H-chrom en-4-one 3e, and 5,6,7-trihydroxy-8-(4-methylpiperazinylmethyl)-2-phenyl-4H-chromen-4-one 3f (IC50 0.27-0.38 μM) were about 20-fold more potent than baicalein, and were at the same level as flavopiridol (IC50 0.33 μM).