Pharmacology and clinical use of sex steroid hormone receptor modulators

A Cleve, KH Fritzemeier, B Haendler… - Sex and Gender …, 2012 - Springer
Sex steroid receptors are ligand-triggered transcription factors. Oestrogen, progesterone
and androgen receptors form, together with the glucocorticoid and mineralocorticoid …

Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators

SJ Lusher, HCA Raaijmakers, D Vu-Pham… - Journal of Biological …, 2011 - ASBMB
The progesterone receptor is able to bind to a large number and variety of ligands that elicit
a broad range of transcriptional responses ranging from full agonism to full antagonism and …

Calcium (II)-catalyzed enantioselective conjugate additions of amines

BE Uno, RD Dicken, LR Redfern, CM Stern… - Chemical …, 2018 - pubs.rsc.org
The direct enantioselective chiral calcium (II)· phosphate complex (Ca [CPA] 2)-catalyzed
conjugate addition of unprotected alkyl amines to maleimides was developed. This mild …

Nitrogen containing privileged structures and their solid phase combinatorial synthesis

A Verma, M Ram Yadav, R Giridhar… - … Chemistry & High …, 2013 - benthamdirect.com
The existence of preferred molecular scaffolds that possess inherent biological activity,
called privileged structures, is now well recognized. Such privileged structures not only …

Solid-phase synthesis of N-substituted pyrrolidinone-tethered N-substituted piperidines via Ugi reaction

Z Liu, A Nefzi - Journal of combinatorial chemistry, 2010 - ACS Publications
Solid-Phase Synthesis of N-Substituted Pyrrolidinone-Tethered N-Substituted Piperidines via
Ugi Reaction | ACS Combinatorial Science ACS ACS Publications C&EN CAS Find my …

Improving the developability profile of pyrrolidine progesterone receptor partial agonists

LS Kallander, DG Washburn, TH Hoang… - Bioorganic & medicinal …, 2010 - Elsevier
The previously reported pyrrolidine class of progesterone receptor partial agonists
demonstrated excellent potency but suffered from serious liabilities including hERG …

Expeditious synthesis of nitrogenated spongianes: 4-methyldecarboxyspongolactams

P Basabe, A Blanco, O Bodero, M Martín, IS Marcos… - Tetrahedron, 2010 - Elsevier
Herein, the synthesis of 4-methyldecarboxyhaumanamide (9) and 4-
methyldecarboxyspongolactams A (11) and C (13) is presented.(−)-Sclareol is the starting …

Catalysts and methods for enantioselective conjugate additions of amines to unsaturated electrophiles

KA Scheidt, B Uno - US Patent 10,781,172, 2020 - Google Patents
Chiral amines are a ubiquitous motif in pharmaceuticals and natural products (FIG. 1). The
conjugate addition of 50 amine nucleophiles to various a, ß-unsaturated systems is a well …

Diastereoselective synthesis of novel N-substituted pyrrolidine-2-one containing piperazine derivatives

M Ghandi, M Khodadadi, A Abbasi - Journal of the Iranian Chemical …, 2016 - Springer
Synthesis of novel hybrid derivatives of two known scaffolds, pyrrolidine-2-one and
piperazine, is described. Initially, the Ugi reaction of phenylglyoxal, aromatic amines …

Drug design approaches to manipulate the agonist-antagonist equilibrium in steroid receptors

SJ Lusher, P Conti, W Dokter, PH Hermkens… - Steroids-Basic …, 2012 - books.google.com
The steroid hormone receptors, the Androgen Receptor (AR), Estrogen Receptors (ERα and
ERβ), Glucocorticoid Receptor (GR), Mineralocorticoid Receptor and Progesterone …