Cyclic Ketoximes as Estrogen Receptor β Selective Agonists. Carlotta Granchi, Margherita Lapillo, Concetta Russo Spena, Flavio Rizzolio, Tiziano Tuccinardi, Teresa A.Design, Synthesis, and Evaluation of GLUT Inhibitors. Carlotta Granchi, Tiziano Tuccinardi, Filippo Minutolo.Organic & Biomolecular Chemistry 2020, 18 Transition metal-free synthesis of sterically hindered allylarenes from 5-hexene-2-one. Ranjay Shaw, Ismail Althagafi, Amr Elagamy, Reeta Rai, Chandan Shah, Vishal Nemaysh, Harpreet Singh, Ramendra Pratap.Structural Evolutions of Salicylaldoximes as Selective Agonists for Estrogen Receptor β. Filippo Minutolo, Simone Bertini, Carlotta Granchi, Teresa Marchitiello, Giovanni Prota, Simona Rapposelli, Tiziano Tuccinardi, Adriano Martinelli, Jillian R.Triaryl-Substituted Schiff Bases Are High-Affinity Subtype-Selective Ligands for the Estrogen Receptor. Zong-Quan Liao, Chune Dong, Kathryn E.The Journal of Organic Chemistry 2015, 80 Chromatography-Free Entry to Substituted Salicylonitriles: Mitsunobu-Triggered Domino Reactions of Salicylaldoximes.

Highly Selective Salicylketoxime-Based Estrogen Receptor β Agonists Display Antiproliferative Activities in a Glioma Model. Ilaria Paterni, Simone Bertini, Carlotta Granchi, Tiziano Tuccinardi, Marco Macchia, Adriano Martinelli, Isabella Caligiuri, Giuseppe Toffoli, Flavio Rizzolio, Kathryn E.Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer. Pham, Huiping Zhao, Kathryn Carlson, Teresa Martin, John A. Gutgesell, Jiong Zhao, Loruhama Delgado-Rivera, Thao N. Oxime-Bridged Mn6 Clusters Inserted in One-Dimensional Coordination Polymer. Mirela-Fernanda Zaltariov, Maria Cazacu, Liviu Sacarescu, Angelica Vlad, Ghenadie Novitchi, Cyrille Train, Sergiu Shova, and Vladimir B.Rh(III)-Catalyzed Enaminone-Directed Alkenyl C–H Activation for the Synthesis of Salicylaldehydes. Bing Qi, Shan Guo, Wenjing Zhang, Xiaolong Yu, Chao Song, Jin Zhu.This article is cited by 21 publications. The chloro-substituted derivative showed the highest β affinity and selectivity, and it also proved to be an ERβ partial agonist with an EC 50 of 11 nM. The binding affinities of the compounds herein reported were in good agreement with the results of computational docking analysis. The measured ERβ affinity proved to be very sensitive to the effect of central core substituents. An efficient sequential halogen-selective double cross-coupling reaction was developed for the synthesis of the methyl-substituted ER ligand. In this series, small substituents (CH 3, CN, Cl) were introduced into the central phenyl scaffold. Monoaryl-substituted salicylaldoximes were obtained by replacing the phenol moiety (ring A) of the ERβ pharmacophore with the pseudocycle A′ ring, which has previously been shown to behave as a bioequivalent of phenols in nonselective ER ligands. Salicylaldoximes possess a hydrogen-bonded pseudocyclic A′ ring in place of the typical phenolic A ring that is characteristic of most estrogen receptor (ER) ligands.

Giovanni prota