摘要:
The invention provides a cancer cell useful in screening BCRP-inhibitors, and a BCRP-inhibitor.The BCRP-inhibitor contains, as the active ingredient, a flavonoid represented by any of the following formulae (1), (2), (3), (4), and (5): and glycosides, esters, or salts thereof; and an anticancer agent containing the BCRP-inhibitor together with an anticancer agent available as the substrate of BCRP.
摘要:
The invention provides a cancer cell useful in screening BCRP-inhibitors, and a BCRP-inhibitor. The BCRP-inhibitor contains, as the active ingredient, a flavonoid represented by any of the following formulae (1), (2), (3), (4), and (5): and glycosides, esters, or salts thereof; and an anticancer agent containing the BCRP-inhibitor together with an anticancer agent available as the substrate of BCRP.
摘要:
The invention provides a drug which inhibits BCRP.A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1−7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., —OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
摘要:
A breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative or a salt thereof.
摘要:
The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor.The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom;Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
摘要翻译:本发明涉及一种乳腺癌抗性蛋白(BCRP / ABCG2)抑制剂。 BCRP抑制剂含有式(1)表示的丙烯腈衍生物作为活性成分:其中R1和R2之一表示氰基,另一个表示氢原子; Ar 1表示由式(2)〜(4)表示的基团中的基团,Ar 2表示具有可被卤素原子取代的稠环的芳香族烃基或选自由 下述式(5)〜(15)表示:或其盐。
摘要:
The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1−7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., —OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
摘要:
A diarylheptanoide derivative of the following formula (1), ##STR1## and a drug composition comprising this compound, such as a 5-lipoxygenase inhibitor, an antiinflammatory agent, and the like. The diarylheptanoide derivative (1) is effective for treating and preventing various inflammatory diseases due to its strong 5-lipoxygenase inhibiting effect.
摘要:
A composition for retarding skin aging which contains an edible herb medicine or medicines round in Taiwan, in particular a plant extract or extracts having melanin formation-unhibiting, elastase-inhibiting, hyaluronidase-inhibiting, active oxygen-eliminating and/or radical-capturing type antioxidant activities, and a medicinally acceptable base and/or additives for external dermal application. The composition is useful in promoting skin whitening effects, maintaining the tension and elasticity of the skin, facilitating skin moistening and providing the skin with anti-inflammatory and/or anti-allergic properties.
摘要:
A camptothecin-containing pharmaceutical composition which contains: (a) camptothecin or a derivative thereof, and (b) one or more compounds selected from among ascorbic acid or a salt thereof, sodium hydrogen sulfite, sodium sulfite, potassium pyrosulfite, sodium erythorbate, sodium thioglycolate, sodium pyrosulfite, and α-thioglycerin. The pharmaceutical composition is useful in that, after storage for a long period of time or under light-irradiation conditions, camptothecin or a derivative thereof contained therein undergoes minimum degradation.
摘要:
A camptothecin-containing pharmaceutical composition which contains: (a) camptothecin or a derivative thereof, and (b) one or more compounds selected from among ascorbic acid or a salt thereof, sodium hydrogen sulfite, sodium sulfite, potassium pyrosulfite, sodium erythorbate, sodium thioglycolate, sodium pyrosulfite, and α-thioglycerin. The pharmaceutical composition is useful in that, after storage for a long period of time or under light-irradiation conditions, camptothecin or a derivative thereof contained therein undergoes minimum degradation.