Analogues of orphan nuclear receptor small heterodimer partner ligand and apoptosis inducer (E)-4-[3-(1-adamantyl)-4-hydroxyphenyl]-3-chlorocinnamic acid. 2. …

…, L Farhana, DJ Castro, J Yu, RG Oshima…

Index: Xia, Zebin; Correa, Ricardo G.; Das, Jayanta K.; Farhana, Lulu; Castro, David J.; Yu, Jinghua; Oshima, Robert G.; Fontana, Joseph A.; Reed, John C.; Dawson, Marcia I. Journal of Medicinal Chemistry, 2012 , vol. 55, # 1 p. 233 - 249

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Citation Number: 5

Abstract

The parent phenol of adapalene and its (E)-cinnamic acid analogue were found to induce cancer cell apoptosis but cause adverse systemic effects when administered to mice. In contrast, their respective 5-Cl-and 3-Cl-substituted analogues had their adverse effects mitigated without a comparable loss of cancer cell inhibitory activity. As a result, pharmacologic space in this region of the cinnamic phenyl ring scaffold was explored. ...