RU2000101307A - CHALKONS WITH ANTI-PROLIFERATIVE ACTIVITY - Google Patents

CHALKONS WITH ANTI-PROLIFERATIVE ACTIVITY

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Publication number
RU2000101307A
RU2000101307A RU2000101307/04A RU2000101307A RU2000101307A RU 2000101307 A RU2000101307 A RU 2000101307A RU 2000101307/04 A RU2000101307/04 A RU 2000101307/04A RU 2000101307 A RU2000101307 A RU 2000101307A RU 2000101307 A RU2000101307 A RU 2000101307A
Authority
RU
Russia
Prior art keywords
phenyl
hydroxy
propen
methylallyloxy
enyloxy
Prior art date
Application number
RU2000101307/04A
Other languages
Russian (ru)
Other versions
RU2203883C2 (en
Inventor
Эцио БОМБАРДЕЛЛИ
Пьеро ВАЛЕНТИ
Original Assignee
Индена С.П.А.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9712966.2A external-priority patent/GB9712966D0/en
Application filed by Индена С.П.А. filed Critical Индена С.П.А.
Publication of RU2000101307A publication Critical patent/RU2000101307A/en
Application granted granted Critical
Publication of RU2203883C2 publication Critical patent/RU2203883C2/en

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Claims (6)

1. Соединение, имеющее общую формулу (А)
Figure 00000001

где Ar - фенил, который может быть незамещенным либо замещенным одним, двумя либо тремя заместителями, независимо выбираемыми из числа Cl, Br, F, -ОМе, NO2, CF3, C1-4 низшего алкила, -NMe2, -NEt2, -SCH3, -NHCOCH3; 2-тиенил, 2-фурил; 3-пиридил; 4-пиридил либо 3-индолил;
R - -OCH2R1, где R1 выбирают из числа -СН=СМе2, -СМе=СН2, -С
Figure 00000002
СН; при условии, что в случае, когда Ar представляет собой фенил, R может быть любым, за исключением 3-метил-2-бутенила.
1. The compound having the General formula (A)
Figure 00000001

where Ar is phenyl, which may be unsubstituted or substituted by one, two or three substituents independently selected from the group of Cl, Br, F, —OMe, NO 2 , CF 3 , C 1-4 lower alkyl, —NMe 2 , —NEt 2 , -SCH 3 , -NHCOCH 3 ; 2-thienyl, 2-furyl; 3-pyridyl; 4-pyridyl or 3-indolyl;
R is —OCH 2 R 1 , where R 1 is selected from —CH = CME 2 , —CMe = CH 2 , —C
Figure 00000002
CH; with the proviso that when Ar is phenyl, R may be anything but 3-methyl-2-butenyl.
2. Соединение по п. 1, где Ar выбирают из числа незамещенного фенила, 4-диметиламинофенила, 4-ацетамидофенила, 3-пиридила, 4-пиридила и 3-индолила. 2. The compound of claim 1, wherein Ar is selected from unsubstituted phenyl, 4-dimethylaminophenyl, 4-acetamidophenyl, 3-pyridyl, 4-pyridyl and 3-indolyl. 3. Соединение, которое выбирают из:
1-[2-гидрокси-4-(3-метилбут-2-енилокси)-фенил] -3(пиридин-4-ил)-пропен-1-она,
1-[2-гидрокси-4-(3-метилбут-2-енилокси)-фенил] -3(пиридин-3-ил)-пропен-1-она,
1-[2-гидрокси-4-(3-метилбут-2-енилокси)-фенил] -3-(4-ацетамид)-фенил-пропен-1-она,
1-[2-гидрокси-4-(2-метилаллилокси)-фенил-3-(4-диметиламин)-фенил] -пропен-1-она,
1-[2-гидрокси-4-(3-метилбут-2-енилокси)-фенил-3-(индол-3-ил)-пропен-1-она,
1-[2-гидрокси-4-(2-метилаллилокси)-фенил]-3-(индол-3-ил)-пропен-1-она,
1-[2-гидрокси-4-(проп-2-инилокси)-фенил-3-(индол-3-ил)пропен-1-она,
1-[2-гидрокси-4-(2-метилаллилокси)-фенил]-3-(пиридин-3-ил)-пропен-1-она,
1-[2-гидрокси-4-(2-метилаллилокси)-фенил-3-(3-метоксифенил)-пропен-1-она,
1-[2-гидрокси-4-(проп-2-инилокси)-фенил-3-(пиридин-3-ил)пропен-1-она.
3. A compound that is selected from:
1- [2-hydroxy-4- (3-methylbut-2-enyloxy) phenyl] -3 (pyridin-4-yl) propen-1-one,
1- [2-hydroxy-4- (3-methylbut-2-enyloxy) phenyl] -3 (pyridin-3-yl) propen-1-one,
1- [2-hydroxy-4- (3-methylbut-2-enyloxy) phenyl] -3- (4-acetamide) phenylpropen-1-one,
1- [2-hydroxy-4- (2-methylallyloxy) phenyl-3- (4-dimethylamine) phenyl] propen-1-one,
1- [2-hydroxy-4- (3-methylbut-2-enyloxy) -phenyl-3- (indol-3-yl) -propen-1-one,
1- [2-hydroxy-4- (2-methylallyloxy) phenyl] -3- (indol-3-yl) propen-1-one,
1- [2-hydroxy-4- (prop-2-ynyloxy) phenyl-3- (indol-3-yl) propen-1-one,
1- [2-hydroxy-4- (2-methylallyloxy) phenyl] -3- (pyridin-3-yl) propen-1-one,
1- [2-hydroxy-4- (2-methylallyloxy) phenyl-3- (3-methoxyphenyl) propen-1-one,
1- [2-hydroxy-4- (prop-2-ynyloxy) phenyl-3- (pyridin-3-yl) propen-1-one.
4. Фармацевтическая композиция, включающая соединение, соответствующее любому из предшествующих пунктов, и фармацевтически приемлемый наполнитель. 4. A pharmaceutical composition comprising a compound according to any one of the preceding paragraphs, and a pharmaceutically acceptable excipient. 5. Соединение по любому из пп.1-3 для использования в качестве фармацевтического препарата. 5. The compound according to any one of claims 1 to 3 for use as a pharmaceutical preparation. 6. Использование соединения по любому из пп.1-4 при изготовлении фармацевтической композиции для лечения либо предупреждения опухолей, лечения либо предупреждения климактерических расстройств, для лечения либо предупреждения остеопороза. 6. The use of a compound according to any one of claims 1 to 4 in the manufacture of a pharmaceutical composition for the treatment or prevention of tumors, the treatment or prevention of menopausal disorders, for the treatment or prevention of osteoporosis.
RU2000101307/04A 1997-06-19 1998-06-12 Chalcones eliciting antiproliferative activity RU2203883C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9712966.2A GB9712966D0 (en) 1997-06-19 1997-06-19 Novel chalcones
GB9712966.2 1997-06-19

Publications (2)

Publication Number Publication Date
RU2000101307A true RU2000101307A (en) 2001-11-10
RU2203883C2 RU2203883C2 (en) 2003-05-10

Family

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RU2000101307/04A RU2203883C2 (en) 1997-06-19 1998-06-12 Chalcones eliciting antiproliferative activity

Country Status (22)

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US (1) US6147082A (en)
EP (1) EP0989973B1 (en)
JP (1) JP4064471B2 (en)
KR (1) KR20010013603A (en)
CN (1) CN1198802C (en)
AT (1) ATE303362T1 (en)
AU (1) AU742784C (en)
CA (1) CA2294278C (en)
CZ (1) CZ294976B6 (en)
DE (1) DE69831409T2 (en)
DK (1) DK0989973T3 (en)
ES (1) ES2244075T3 (en)
GB (1) GB9712966D0 (en)
HK (1) HK1023770A1 (en)
HU (1) HU227628B1 (en)
NO (1) NO314802B1 (en)
PL (1) PL190495B1 (en)
PT (1) PT989973E (en)
RU (1) RU2203883C2 (en)
SI (1) SI0989973T1 (en)
SK (1) SK283077B6 (en)
WO (1) WO1998058913A1 (en)

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WO2001054682A1 (en) * 2000-01-27 2001-08-02 Takara Bio Inc. Remedies
KR100377514B1 (en) * 2000-05-23 2003-03-26 신국현 Chalcone derivatives, method for preparation thereof and pharmaceutical composition containing the said derivatives
DE10060677A1 (en) * 2000-12-05 2002-06-20 Aventis Pharma Gmbh Klainetins and their derivatives, processes for their preparation and their use
US7514579B2 (en) * 2002-06-13 2009-04-07 Johns Hopkins University Boronic chalcone derivatives and uses thereof
EP1563841A4 (en) * 2002-10-01 2009-08-12 Takara Bio Inc Remedies
NZ552298A (en) * 2004-05-23 2011-04-29 Gerard M Housey Method for identifying inhibitors or activators of a theramutein by comparing the phenoresponse of cells exposed to a test compound
CN100336797C (en) * 2005-08-19 2007-09-12 浙江大学 Tetra substituted chalcone derivative and preparing method and use
CN102060792B (en) * 2010-12-24 2016-08-03 西南大学 2 '-amido chalcone azole compounds and pyrazoline thereof and cyclopropyl azole derivative, preparation method and purposes
ES2540457B2 (en) * 2013-06-19 2015-12-28 Universidad De Sevilla Procedure for obtaining leaf extracts from Corema album and its therapeutic application
CN103360338B (en) * 2013-07-30 2015-04-01 中国科学院新疆理化技术研究所 Preparation method of chalconebenzothiazoleamide derivatives, and use of derivatives
CN103910691A (en) * 2014-04-18 2014-07-09 山东药品食品职业学院 Halogenated phenyl chalcone derivative as well as preparation method and application thereof
CN103896932A (en) * 2014-04-18 2014-07-02 山东药品食品职业学院 Isoxazolyl aryl chalcone derivative as well as preparation method and application thereof
CZ307046B6 (en) * 2015-09-02 2017-12-13 Univerzita Palackého v Olomouci Copper complexes with derivatives of (E)-1-(2'-hydroxyphenyl)-3-phenyl-prop-2-en-1-one and their use as pharmaceuticals in antitumour therapy
WO2017103637A1 (en) 2015-12-18 2017-06-22 Blirt S.A. Diphenylpropane compounds and their cytotoxic activity
CN106279082B (en) * 2016-08-02 2019-02-01 浙江大学 Substituted furans chalcone derivative and preparation method thereof
CN111138264B (en) * 2019-11-29 2023-08-04 温州医科大学 Syringaldehyde derivative and application thereof in preparing anti-gynecological tumor drugs
KR102496887B1 (en) * 2020-10-15 2023-02-06 경상국립대학교산학협력단 Composition for preventing, improving or treating of breast cancer comprising butein derivatives or pharmaceutically acceptable salts

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EP0528975A4 (en) * 1990-05-17 1993-09-15 Baylor College Of Medicine Growth inhibitors and methods of treating cancer and cell proliferative diseases
IT1271301B (en) * 1994-12-20 1997-05-27 Indena Spa NATURAL AND SYNTHETIC CALCONES AND THEIR ESTERS WITH ANTI-PROLIFERATIVE ACTIVITY IN CANCER OF THE UTERUS, OVARIAN AND BREAST AND FORMULATIONS CONTAINING THEM

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