Steroid chalcone and ester derivatives thereof and preparation method and application thereof

The invention discloses steroid chalcone and ester derivatives thereof, the structural formula of the derivatives is as shown in the formula (I), R1 is hydrogen or halogen group, R2 is hydrogen or a C1-3 alkoxy group, and R3 is hydrogen, a halogen group, a benzyloxy group, a mercaptomethyl group, a...

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Bibliographic Details
Main Authors ZHAO SHULIN, XIN DAISHAN, CAI XIAORUI
Format Patent
LanguageChinese
English
Published 28.07.2020
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
STEROIDS
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Summary:The invention discloses steroid chalcone and ester derivatives thereof, the structural formula of the derivatives is as shown in the formula (I), R1 is hydrogen or halogen group, R2 is hydrogen or a C1-3 alkoxy group, and R3 is hydrogen, a halogen group, a benzyloxy group, a mercaptomethyl group, a C1-3 alkyl group or a C1-3 alkoxy group. The steroid chalcone and the ester derivative thereof provided by the invention are simple to prepare, raw materials are easy to obtain, meanwhile, good anti-inflammatory activity is realized, the selectivity is higher, the cytotoxicity is lower, the steroidchalcone and the ester derivative thereof disclosed by the invention have a very strong inhibition effect on nitric oxide (NO) generated by lipopolysaccharide (LPS)-induced mouse peritoneal macrophageRAW 264.7 cells, particularly, the IC50 value of the compound 7 is close to that of dexamethasone, the dexamethasone derivative has an obvious inhibition effect on inflammatory factors TNF-alpha, IL-6 and PGE-2 released by RA
Bibliography:Application Number: CN202010365570