Isoquinolinone derivatives, and preparation method and medical purpose thereof
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A pharmaceutical and compound technology, applied in the treatment of ER-type breast cancer, in the field of isoquinolinone derivatives, which can solve problems such as cancer cell stimulation
Inactive Publication Date: 2013-01-16
CHINA PHARM UNIV
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But tamoxifen also has a big disadvantage, it exhibits estrogen agonist properties in the uterus and has a stimulating effect on cancer cells in the uterus
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[0105] Specific embodiments (the embodiments are only used to illustrate the present invention, not to limit the present invention)
Embodiment 1
[0109] Preparation of 7-methoxy-3-(4-methoxyphenyl)-1H-isochrome-1-one (IVa)
[0110] M-Methoxy perphthalic acid (0.18g, 0.86mmol), p-methoxybenzoyl chloride (0.09g, 3.44mmol), stir at 200°C for 6 hours, add 50ml of dichloromethane, wash with saturated sodium carbonate, and spin the organic phase Dry, column chromatography gave a white solid (0.092g, 35%). m.p.144-146℃
Embodiment 2
[0112] Preparation of 7-methoxy-3-(4-methoxyphenyl)-2-(4-hydroxyphenyl)isoquinolin-1(2H)-one (Va)
[0113] 7-Methoxy-3-(4-methoxyphenyl)-1H-isochromen-1-one (1g, 3.54mmol), p-hydroxyaniline (1.93g, 17.7mmol), acetic acid 2ml, reflux and stir After 4 hours, spin-dry, dissolve in dichloromethane, wash with 1N HCl, spin-dry the organic phase, and column chromatography to obtain 0.67 g of white solid powder with a yield of 51.1%. m.p.236-240°C. 1 H-NMR(CDCl 3 ) δ: 3.76 (s, 3H, OCH3), 3.94 (s, 2H, OCH3), 6.67-775 (m, 12H, Ar-H & C4-H), 9.58 (s, 1H, OH). EI-MS m / z: 374[M] + .
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Abstract
The invention relates to the fields of pharmaceutical chemistry and organic chemistry, in particular to isoquinolinone derivatives. The compounds can be used for treating various medical indications associated with postmenopausal symptoms, uterine fiber lesions and arterial smooth muscle cell proliferation, particularly ER-(+) breast cancer by inhibiting alpha-estrogen receptor subtype (ER alpha) and through vascular endothelial growth factor receptor (VEGFR-2) bi-target. Meanwhile, the compounds have an obvious inhibiting effect on tumor metastasis, and have a general formula I.
Description
Technical field [0001] The invention relates to the fields of medicinal chemistry and organic chemistry, in particular to a class of isoquinolinone derivatives. These compounds can treat a variety of medical indications related to postmenopausal syndrome and uterine fibrosis by inhibiting the dual targets of estrogen receptor alpha subtype (ERα) and vascular endothelial cell growth factor receptor (VEGFR-2) And arterial smooth muscle cell proliferation, especially suitable for the treatment of ER-(+) breast cancer. At the same time, these compounds also have a significant inhibitory effect on tumor metastasis. Background technique [0002] "Postmenopausal syndrome" refers to a variety of pathological conditions caused by a decrease in estrogen secretion when a woman is in or has completed a physiological metamorphosis, that is, menopause. It is mainly manifested in: osteoporosis, estrogen-dependent cancers (breast cancer, endometrial cancer and ovarian cancer), cardiovascular d...
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