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Article ; Online: Modeling, Synthesis, and Biological Evaluation of Potential Retinoid-X-Receptor (RXR) Selective Agonists: Analogs of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahyro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and 6-(Ethyl(4-isobutoxy-3-isopropylphenyl)amino)nicotinic Acid (NEt-4IB).

Jurutka, Peter W / di Martino, Orsola / Reshi, Sabeeha / Mallick, Sanchita / Sabir, Zhela L / Staniszewski, Lech J P / Warda, Ankedo / Maiorella, Emma L / Minasian, Ani / Davidson, Jesse / Ibrahim, Samir J / Raban, San / Haddad, Dena / Khamisi, Madleen / Suban, Stephanie L / Dawson, Bradley J / Candia, Riley / Ziller, Joseph W / Lee, Ming-Yue /
Liu, Chang / Liu, Wei / Marshall, Pamela A / Welch, John S / Wagner, Carl E

International journal of molecular sciences

2021  Volume 22, Issue 22

Abstract: Five novel analogs of 6-(ethyl)(4-isobutoxy-3-isopropylphenyl)amino)nicotinic acid-or NEt-4IB-in addition to seven novel analogs of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) were prepared and evaluated ... ...

Abstract Five novel analogs of 6-(ethyl)(4-isobutoxy-3-isopropylphenyl)amino)nicotinic acid-or NEt-4IB-in addition to seven novel analogs of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) were prepared and evaluated for selective retinoid-X-receptor (RXR) agonism alongside bexarotene (
MeSH term(s) Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/pharmacology ; Apolipoproteins E/genetics ; Apolipoproteins E/metabolism ; Bexarotene/analogs & derivatives ; Bexarotene/chemical synthesis ; Bexarotene/pharmacology ; Cell Line, Tumor ; Dose-Response Relationship, Drug ; Gene Expression ; Humans ; Leukocytes/drug effects ; Leukocytes/metabolism ; Leukocytes/pathology ; Nicotinic Acids/chemical synthesis ; Nicotinic Acids/pharmacology ; Retinoid X Receptor alpha/agonists ; Retinoid X Receptor alpha/genetics ; Retinoid X Receptor alpha/metabolism ; Structure-Activity Relationship
Chemical Substances Antineoplastic Agents ; ApoE protein, human ; Apolipoproteins E ; Nicotinic Acids ; RXRA protein, human ; Retinoid X Receptor alpha ; Bexarotene (A61RXM4375)
Language English
Publishing date 2021-11-16
Publishing country Switzerland
Document type Journal Article
ZDB-ID 2019364-6
ISSN 1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online) 1422-0067
ISSN 1422-0067 ; 1661-6596
DOI 10.3390/ijms222212371
Database MEDical Literature Analysis and Retrieval System OnLINE

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