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Hydroxamic acid derivative and application thereof
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A technology of derivatives and hydroxamic acid, which is applied in the field of hydroxamic acid derivatives and its application, can solve the problem of no PARP-1 bifunctional inhibitor
Inactive Publication Date: 2014-04-30
CENT SOUTH UNIV
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However, according to literature survey results, there are no bifunctional inhibitors of PARP-1 and HDAC
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[0108] Add hydroxylaminehydrochloride (2.085g, 0.03mmol), triethylamine (6.2mL) and dichloromethane (15mL) successively into a 50mL round bottom flask, stir at room temperature for 5 minutes, and place in an ice bath. After cooling to 0°C, add compound a (0.66g, 0.003mol), continue the reaction for 1 hour, add 20mL of water to stop the reaction, extract, collect the dichloromethane layer, add anhydroussodiumsulfate to dry, concentrate under vacuum and reduce pressure, HPLC Separated and lyophilized to obtain 225mg of yellow solid. 1 H NMR (400MHz, DMSO-d 6 ): δ8.41(d, J=2.0Hz, 1H), 8.05(dd, J=8.4Hz, J=2.0Hz, 1H), 7.90(d, J=8.4Hz, 1H). MS(m / z):214.98[M+H] + .
[0111] The synthetic route is the same as in Example 1. 1 H NMR (400MHz, DMSO-d 6 ): δ8.55(d, J=2.0Hz, 1H), 8.35(dd, J=8.0Hz, J=2.0Hz, 1H), 8.01(d, J=8.0Hz, 1H). MS(m / z):251.17[M+H] + .
[0116] In a 1000ml dry three-neck flask, dissolve 30g of compound a in 400ml of methanol, add 45ml of concentrated sulfuric acid dropwise with a constant pressuredropping funnel, slowly raise the temperature to 80°C, stir for 24 hours, then pour the reaction solution into an appropriate amount of ice-water mixture while it is still hot , with saturated Na 2 CO 3 Adjust the pH of the aqueous solution to about 8, filter with suction, dry the obtained solid, and recrystallize with absolute ethanol to obtain 22.6 g of compound b. Yield: 70.1%; Purity by HPLC: 98.7%; 1 H-NMR (400MHz, DMSO-d 6 ):δ8.35(s,2H),8.34(dd,J=1.6Hz,8.3Hz,1H),8.22(dd,J=1.6Hz,7.8Hz,1H),6.75(t,J=7.8Hz, 8.3Hz,1H),3.87(s,3H); 13 C-NMR (100MHz, DMSO-d 6 ): δ167.30, 146.77, 139.77, 133.18, 132.55, 114.62, 114.35, 52.84.
[0117]
[0118] In a 500ml reaction flask, 22.5g of compound...
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Abstract
The invention relates to a hydroxamic acid derivative with a structural formula (I), wherein R1, R2, R3 and L are defined in the specification of the invention. The invention further relates to application of the hydroxamic acid derivative with the structural formula (I) as a histone deacetylase (HDAC) inhibitor or / and a PARP-1 (Poly-ADP-RibosePolymerase-1) inhibitor.
Description
technical field [0001] The invention relates to the field of medicine, in particular to hydroxamic acid derivatives and applications thereof. Background technique [0002] Cancer remains one of the diseases with high morbidity and mortality. There are 2 million new cancer patients and 1.5 million cancer deaths in my country every year. Among various cancers, breast cancer has become the most threatening disease to women's health. The China Population Association released the "China Breast Disease Survey Report" in Beijing on February 1, 2010. The report shows that: with the development of society and economy in our country, the change of people's lifestyle and living environment has caused the incidence of breast cancer to increase year by year: my country The growth rate of breast cancer morbidity and mortality is 1-2 percentage points higher than that of high-incidence countries, and it shows a clear younger trend. my country now has more than 200,000 new breast cancer p...
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