Patent
Substituted phenylethenyl compounds having retinoid-like biological activity
TLDR
In this article, the authors defined the formula (STR1) where n is 0-5, lower branched chain alkyl having 3 to 6 carbons, cyclo-alkyl having 3-to-6 carbons and 1 or 2 double bonds, alkynyl having 2-6-carbons and 2-or 2 triple bonds, and Z-Y substituent is in a 1,2 or 1,3 position on the phenyl ring relative to the ethene moiety.Abstract:
Compounds of the formula ##STR1## wherein R1, R2, R3 and R4 independently are hydrogen, lower alkyl of 1 to 6 carbons, halogen or lower alkoxy of 1 to 6 carbons; R5 and R5 ' independently are hydrogen or lower alkyl of 1 to 6 carbons; Y is oxygen or sulfur; Z is n-alkyl having 2 to 10 carbons, cyclo or branch-chained alkyl of 3 to 10 carbons, and straight chain alkenyl having 2 to 10 carbons, or cyclo or branched chained alkenyl of 3 to 10 carbons, and the Z-Y substituent is in a 1,2 (ortho) or 1,3 (meta) position on the phenyl ring relative to the ethene moiety; A is (CH2)n where n is 0-5, lower branched chain alkyl having 3 to 6 carbons, cycloalkyl having 3 to 6 carbons, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9 R10, --CH2 OH, CH2 OR11, CH2 OCOR11, CHO, CH(OR12)2, CHOR13 O, --COR7, CR7 (OR12)2, or CR7 OR13 O, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R11 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.read more
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Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid-like activity
TL;DR: In this paper, the retinoid-like activity is exhibited by compounds of formula (I) where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is H, -COOH or a pharmaceutically acceptable salt, ester or amide thereof, -CH2OH or an ether or ester derivative, or -CHO or an acetal derivative; m is 0-4; n is 0.
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Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
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References
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Journal ArticleDOI
A Convenient Synthesis of Ethynylarenes and Diethynylarenes
Journal ArticleDOI
Conversion of methyl ketones into terminal acetylenes and (E)-trisubstituted olefins of terpenoid origin
Patent
Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid-like activity
TL;DR: In this paper, the retinoid-like activity is exhibited by compounds of formula (I) where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is H, -COOH or a pharmaceutically acceptable salt, ester or amide thereof, -CH2OH or an ether or ester derivative, or -CHO or an acetal derivative; m is 0-4; n is 0.
Journal ArticleDOI
A general synthesis of terminal and internal arylalkynes by the palladium-catalyzed reaction of alkynylzinc reagents with aryl halides
Patent
Acetylenes disubstituted with a phenyl group and a heterobicyclic group having retinoid-like activity
TL;DR: In this paper, the same authors describe the retinoid-like activity of compounds of the formula "STR1" where X is S, O or NR 1 where R 1 is hydrogen or lower alkyl; n is 0-5; R is H or lower a lower akyl and A is a pharmaceutically acceptable salt.