Multi-target drug discovery in anti-cancer therapy: fragment-based approach toward the design of potent and versatile anti-prostate cancer agents
A Speck-Planche, VV Kleandrova, F Luan… - Bioorganic & medicinal …, 2011 - Elsevier
Prostate cancer (PCa) is the second-leading cause of cancer deaths among men in the
around the world. Understanding the biology of PCa is essential to the development of novel …
around the world. Understanding the biology of PCa is essential to the development of novel …
Titanium‐Mediated Amination of Grignard Reagents Using Primary and Secondary Amines
Make it, then break it: N‐chlorosuccinimide (NCS) was employed as the oxidant in the
synthesis of aniline derivatives using the title transformation (see scheme). Functionalization …
synthesis of aniline derivatives using the title transformation (see scheme). Functionalization …
Labda‐8(17),12,14‐trien‐19‐oic Acid Contained in Fruits of Cupressus sempervirens Suppresses Benign Prostatic Hyperplasia in Rat and In Vitro Human Models …
Fruit extract of Cupressus sempervirens (CS), which is used traditionally to treat Benign
Prostatic Hyperplasia (BPH)‐like urinary symptoms in patients, was scientifically validated …
Prostatic Hyperplasia (BPH)‐like urinary symptoms in patients, was scientifically validated …
Design, synthesis and biological profiling of aryl piperazine based scaffolds for the management of androgen sensitive prostatic disorders
In the quest for novel scaffolds for the management of androgen sensitive prostatic disorders
like prostate cancer and benign prostatic hyperplasia, a series of twenty-six aryl/heteroaryl …
like prostate cancer and benign prostatic hyperplasia, a series of twenty-six aryl/heteroaryl …
Novel aryl piperazines for alleviation of 'andropause'associated prostatic disorders and depression
S Gupta, D Pandey, D Mandalapu, V Sharma… - European Journal of …, 2017 - Elsevier
A series of seventeen piperazine derivatives have been synthesized and biologically
evaluated for the management of andropause-associated prostatic disorders and …
evaluated for the management of andropause-associated prostatic disorders and …
Synthesis of new aryl (hetaryl)-substituted tandospirone analogues with potential anxiolytic activity via reductive Heck type hydroarylations
Tandospirone (I), developed as an anxiolytic drug, is an aryl-piperazine compound that
binds to both 5-HT1A and dopamine D4 receptors. Palladium-catalysed hydroarylation …
binds to both 5-HT1A and dopamine D4 receptors. Palladium-catalysed hydroarylation …
Design, synthesis, crystal structure, biological evaluation and molecular docking studies of carbazole-arylpiperazine derivatives
W Xu, J Huang, B Shao, X Xu, R Jiang… - Bioorganic & Medicinal …, 2016 - Elsevier
Abstract Subtype-selective α 1-adrenoceptor (AR) antagonists display optimum therapeutic
efficacies for the treatment of benign prostatic hyperplasia (BPH). In this study, we designed …
efficacies for the treatment of benign prostatic hyperplasia (BPH). In this study, we designed …
X-ray Crystallography, DFT Calculations and Molecular Docking of Indole-Arylpiperazine Derivatives as α1A-Adrenoceptor Antagonists
W Xu, JJ Huang, BH Shao, XJ Xu, RW Jiang, M Yuan - Molecules, 2015 - mdpi.com
Indole-arylpiperazine derivatives have exhibited good selectivity for the α1A-adrenoceptor,
but the structure-activity-binding mechanism relationship remains unclear. In the current …
but the structure-activity-binding mechanism relationship remains unclear. In the current …
[HTML][HTML] Crystal structures, absolute configurations and molecular docking studies of naftopidil enantiomers as α1D-adrenoceptor antagonists
W Xu, J Huang, R Jiang, M Yuan - Acta pharmaceutica sinica B, 2017 - Elsevier
Chiral drug naftopidil (NAF), a specific α 1D-adrenoceptor (AR) antagonist for the treatment
of benign prostatic hyperplasia, was used in racemic form for several decades. Our recent …
of benign prostatic hyperplasia, was used in racemic form for several decades. Our recent …
Synthesis of new tandospirone analogues carrying 1-(3-(trifluoromethyl) phenyl) piperazine
OT Gunkara, BO Sucu, M Guleli… - Synthetic Communications, 2014 - Taylor & Francis
New tandospirone analogues containing a 1-[3-(trifluoromethyl) phenyl] piperazine (TFMPP)
moiety have been synthesized by hydroarylation reactions with Pd (OAc) 2. The …
moiety have been synthesized by hydroarylation reactions with Pd (OAc) 2. The …