46745-36-2Relevant academic research and scientific papers
USE OF DISUBSTITUTED BENZENES TO CONTROL INSECTICIDE-RESISTANT PESTS
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Page/Page column 35; 36, (2018/11/26)
The invention is in the technical field of insect control and relates to the use of a disubstituted benzenes for controlling insecticide-resistant pests such as mosquitoes and cockroaches.
SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Page/Page column 79, (2012/06/30)
The invention provides compounds of Formula (I) : wherein R1 is hydrogen, OH, halo, -CN, -NO2, -N=0, -NHOQ2, -OQ2, -SOQ2, -SO2Q2, -SON(Q2)2, - SO2N(Q2)2, -N(Q2)2, -C(O)OQ2, -C(O)Q2, -C(O)N(Q2)2, -C(=NQ2)NQ2, -NQ2C(=NQ2)NQ2, - C(O)N(Q2)(OQ2), -N(Q2)C(O)-Q2, -N(Q2)C(O)N(Q2)2, -N(Q2)C(O)O-Q2, -N(Q2)SO2Q2, -N(Q2)SOQ2, aliphatic, alkoxy, cycloaliphatic, aryl, arylalkyl, heterocyclic, or heteroaryl ring, each aliphatic, alkoxy, cycloaliphatic, aryl, arylalkyl, heterocyclic, and heteroaryl ring optionally including 1-3 substituents independently selected Q3; R2 and R3 are each independently hydrogen, OH, oxo, aliphatic, cycloaliphatic, heterocycloaliphatic, aryl, or heteroaryl, optionally substituted with 1-3 of Q1 or Q2; X is a branched or straight C1-12 aliphatic chain wherein up to two carbon units are optionally and independently replaced by -C(Q1)2-, -C(Q2)2-, CHQ1, CHQ2-, -CO-, -CS-, -CONQ2, -CO2-, -OCO-, -NQ2-, -NQ2CO2-, - O-, -NQ2CONQ2-, -OCONQ2-, -NQ2CO-, -S-, -SO-, -SO2-, -SO2NQ2-, -NQ2SO2-, or -NQ2SO2NQ2-; G and G1 are each independently a branched or straight C1-2 aliphatic chain, or heterocycloalkyl, wherein up to two carbon units are optionally and independently replaced by -C(Q1)2-, -C(Q2)2-, CHQ1, CHQ2-, -CO-, - CS-, -CONQ2, -CO2-, -OCO-, -NQ2-, -NQ2CO2-, -O-, -NQ2CONQ2-, -OCONQ2-, -NQ2CO-, -S-, -SO-, - SO2-, -SO2NQ2-, -NQ2SO2-, or -NQ2SO2NQ2-, and pharmaceutically acceptable salts, solvates or prodaigs thereof, as well as methods of treating estrogen receptor mediated diseases and disorders using the compounds of Formula (I).
Design, synthesis and bioevaluation of novel candidate selective estrogen receptor modulators
Yadav, Yogesh,MacLean, Erin D.,Bhattacharyya, Annyt,Parmar, Virinder S.,Balzarini, Jan,Barden, Christopher J.,Too, Catherine K.L.,Jha, Amitabh
, p. 3858 - 3866 (2011/11/12)
In an systematic attempt to develop novel Selective Estrogen Receptor Modulators (SERMs), chiral 1-((4-(2-(dialkylamino)ethoxy)phenyl)(2- hydroxynaphthalen-1-yl)methyl)piperidin-4-ols were designed based on an accepted pharmacophore model. Simpler prototypes, viz. racemic 1-((2-hydroxynaphthalen- 1-yl)arylmethyl)piperidin-4-ols, were first synthesized to develop kinetic resolution to pure enantiomers. Simultaneously, a series of racemic 1-((4-(2-(dialkylamino)ethoxy)phenyl)(2-hydroxynaphthalen-1-yl)methyl) piperidin-4-ols were evaluated against estrogen-responsive human MCF-7 breast cancer cells, but the compounds were found to be moderately active. The lack of potency could be due to the molecular bulk resulting in inadequate fit at the receptor. Subsequently, the molecular motif was modified to achiral 1-(4-(2-(dialkylamino)ethoxy)benzyl)naphthalen-2-ols by removing the piperidinol moiety. Bioevaluation of this new series of compounds displayed significantly enhanced cytotoxicity against MCF-7 cells. A representative compound for this series showed estrogen receptor alpha binding activity and the action is that of an antagonist.
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators
Ji, Qinggang,Gao, Jie,Wang, Junbo,Yang, Chunhao,Hui, Xin,Yan, Xueming,Wu, Xihan,Xie, Yuyuan,Wang, Ming-Wei
, p. 2891 - 2893 (2007/10/03)
A series of estrogen receptor ligands based on benzothieno[3,2-b]indole were synthesized and their binding affinity for estrogen receptor subtypes (ERα and ERβ) and effects on mouse uterus and bone were evaluated. Some of these compounds showed strong bin
