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Anti-breast cancer application of indeno isoquinoline estrogen receptor alpha regulator

An estrogen receptor and compound technology, applied in the field of estrogen receptor alpha modulators, can solve the problems of increasing the incidence of breast cancer, the occurrence of endometrial cancer, the induction of breast cancer and endometrial cancer, etc.

Inactive Publication Date: 2013-04-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Because estrogen replacement therapy can significantly reduce the incidence of postmenopausal osteoporotic fractures and coronary heart disease in the treatment of menopausal syndrome, osteoporosis, Alzheimer's disease and cardiovascular system diseases, but it may induce breast cancer and endometrium cancer; in order to overcome the adverse reactions of estrogen-induced carcinogenesis, the combination of estrogen and progestin may still increase the incidence of breast cancer and lead to the occurrence of endometrial cancer. These adverse reactions have prompted people to look for a Drugs that exhibit antiestrogenic effects on the uterus and mammary gland and estrogen-like effects on the iliac and cardiovascular systems

Method used

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  • Anti-breast cancer application of indeno isoquinoline estrogen receptor alpha regulator
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  • Anti-breast cancer application of indeno isoquinoline estrogen receptor alpha regulator

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Experimental program
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specific Embodiment approach

[0019] 1. Test of the binding activity of the compound to be tested to antagonize estradiol and ERα

[0020] 1) Experimental materials

[0021] Estrogen Receptor-alpha (ERα) Human Recombinant (Invitrogen, USA), FluormoneTMES2 (Invitrogen, USA), ES2Screening Buffer (Invitrogen, USA), Estradiol is the standard product preserved in our laboratory, domestic analytical grade, Tamoxifen is the medicinal chemistry of China Pharmaceutical University Standards, 384-well black microplates (Corning, USA), pipette tips (Axygen, USA) provided by the laboratory.

[0022] 2) Experimental steps

[0023] ●Weigh each compound to be tested accurately, add DMSO solvent to form a mother solution, and then use ES2Screening Buffer to prepare the compound solution to be tested to the required concentration, the initial screening concentration is about 1×10 -3 mol / L.

[0024] ●Solution preparation 2X Fluormone TM ES2 / ERαComplex: Prepare 2X Fluormone with ES2Screening Buffer TM The mixed solutio...

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Abstract

The present invention relates to an estrogen receptor regulator of a formula (I) or a pharmaceutically acceptable salt thereof. The compounds can combine with the estrogen receptor alpha to produce the anti-breast cancer function and produce regulation function in uterus and other parts at the same time. The compounds have strong function of combining with the estrogen receptor alpha in vitro, and can effectively antagonize the combination of estrogen and the estrogen receptor alpha, thus treating breast cancer caused by excessive estrogen, while playing the role of regulating in the uterus and other parts.

Description

technical field [0001] The invention relates to a class of indenoisoquinoline estrogen receptor α modulator and its anti-breast cancer effect, and simultaneously produces a regulating effect on the uterus and other parts. Background technique [0002] In recent years, breast cancer has become the first common malignant tumor in women, and the research on anti-breast cancer drugs has important academic and practical significance. [0003] Studies have found that the occurrence and development of breast cancer is related to estrogen receptor (ER). ER is a nuclear receptor, including two subtypes of ERα and ERβ. The homology of the amino acid sequences of ERα and ERβ in DNA binding domain (DNA binding domain, DBD) and ligand binding domain (ligand binding domain, LBD) is 96% and 53%, respectively. There is a large amount of ERα distribution in the classic target tissues of estradiol, such as uterus and breast, while the non-classic target tissues of estradiol, such as prostat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/18A61K31/473A61P35/00
Inventor 严明向华张陆勇苗靖姗唐智超
Owner CHINA PHARM UNIV
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