Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups

Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs

(2020) Benjamin Jeffries et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tricyclic indazoles – a novel class of selective estrogen receptor degrader antagonists.

(2019) James S. Scott et al.   JOURNAL OF MEDICINAL CHEMISTRY

A New Straightforward Method for Lipophilicity (logP) Measurement using 19F NMR Spectroscopy

(2019) Zhong Wang et al.   Jove-Journal of Visualized Experiments

CF2H, a Functional Group-Dependent Hydrogen-Bond Donor: Is It a More or Less Lipophilic Bioisostere of OH, SH, and CH3?

(2019) Yossi Zafrani et al.   JOURNAL OF MEDICINAL CHEMISTRY

Predicting Octanol–Water Partition Coefficients: Are Quantum Mechanical Implicit Solvent Models Better than Empirical Fragment-Based Methods?

(2019) Varun Kundi et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Optimization of LpxC Inhibitor Lead Compounds Focusing on Efficacy and Formulation for High Dose Intravenous Administration

(2019) Philippe Panchaud et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fluorinated cyclopropanes: synthesis and chemistry of the aryl α,β,β-trifluorocyclopropane motif

(2018) Connor J. Thomson et al.   CHEMICAL COMMUNICATIONS

Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization

(2018) Kenji Nakahara et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and structure—activity relationships of cyclopropane-containing analogs of pharmacologically active compounds

(2018) I. A. Novakov et al.   RUSSIAN CHEMICAL BULLETIN

Exploring physicochemical space via a bioisostere of the trifluoromethyl and ethyl groups (BITE): attenuating lipophilicity in fluorinated analogues of Gilenya® for multiple sclerosis

(2018) Nathalie Erdeljac et al.   CHEMICAL COMMUNICATIONS

Advances in the Development of Shape Similarity Methods and Their Application in Drug Discovery

(2018) Ashutosh Kumar et al.   Frontiers in Chemistry

Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry

(2017) Tanaji T. Talele   JOURNAL OF MEDICINAL CHEMISTRY

Oxetanes: Recent Advances in Synthesis, Reactivity, and Medicinal Chemistry

(2016) James A. Bull et al.   CHEMICAL REVIEWS

The “Cyclopropyl Fragment” is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules

(2016) Tanaji T. Talele   JOURNAL OF MEDICINAL CHEMISTRY

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

(2016) Kevin W. Kuntz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Investigating the Influence of (Deoxy)fluorination on the Lipophilicity of Non-UV-Active Fluorinated Alkanols and Carbohydrates by a New log P Determination Method

(2015) Bruno Linclau et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Molecular Recognition in Chemical and Biological Systems

(2015) Elke Persch et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fluorination Patterning: A Study of Structural Motifs That Impact Physicochemical Properties of Relevance to Drug Discovery

(2015) Quentin A. Huchet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Benzamide-Based Histamine H3 Receptor Antagonists: The Identification of Two Candidates for Clinical Development

(2015) Michael A. Letavic et al.   ACS Medicinal Chemistry Letters

Profound Methyl Effects in Drug Discovery and a Call for New CH Methylation Reactions

(2013) Heike Schönherr et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

On the polarity of partially fluorinated methyl groups

(2013) Quentin A. Huchet et al.   JOURNAL OF FLUORINE CHEMISTRY

The Methylation Effect in Medicinal Chemistry

(2011) Eliezer J. Barreiro et al.   CHEMICAL REVIEWS

Oxetanes in Drug Discovery: Structural and Synthetic Insights

(2010) Georg Wuitschik et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Medicinal Chemist’s Guide to Molecular Interactions

(2010) Caterina Bissantz et al.   JOURNAL OF MEDICINAL CHEMISTRY