Hitting a Moving Target: How Does anN-Methyl Group Impact Biological Activity?

Predicting the unpredictable: Recent structure–activity studies on peptide-based macrocycles

(2015) Hendra Wahyudi et al.   BIOORGANIC CHEMISTRY

N-terminal and C-terminal modulation of Hsp90 produce dissimilar phenotypes

(2015) Y. Wang et al.   CHEMICAL COMMUNICATIONS

Heat-shock protein 90 inhibitors: will they ever succeed as chemotherapeutics?

(2015) Yao Wang et al.   Future Medicinal Chemistry

Going Out on a Limb: Delineating The Effects of β-Branching, N-Methylation, and Side Chain Size on the Passive Permeability, Solubility, and Flexibility of Sanguinamide A Analogues

(2015) Andrew T. Bockus et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cell-Permeable Cyclic Peptides from Synthetic Libraries Inspired by Natural Products

(2015) William M. Hewitt et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Combining an Hsp70 inhibitor with either an N- or C-terminal Hsp90 inhibitor produces mechanistically distinct phenotypes

(2015) Y. Wang et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Regulating the cytoprotective response in cancer cells using simultaneous inhibition of Hsp90 and Hsp70

(2015) Y. Wang et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

C-terminal heat shock protein 90 modulators produce desirable oncogenic properties

(2015) Y. Wang et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Blocking the heat shock response and depleting HSF-1 levels through heat shock protein 90 (hsp90) inhibition: a significant advance on current hsp90 chemotherapies

(2015) Yen Chin Koay et al.   RSC Advances

Sanguinamide B analogs: identification of active macrocyclic structures

(2014) Hendra Wahyudi et al.   TETRAHEDRON LETTERS

Synthesis of macrocycles that inhibit protein synthesis: stereochemistry and structural based studies on sanguinamide B derivatives

(2014) Adrian L. Pietkiewicz et al.   TETRAHEDRON LETTERS

Chemically Accessible Hsp90 Inhibitor That Does Not Induce a Heat Shock Response

(2014) Yen Chin Koay et al.   ACS Medicinal Chemistry Letters

A heat shock protein 90 inhibitor that modulates the immunophilins and regulates hormone receptors without inducing the heat shock response

(2013) Jeanette R. McConnell et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Macrocyclic Drugs and Clinical Candidates: What Can Medicinal Chemists Learn from Their Properties?

(2013) Fabrizio Giordanetto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Macrocycles in new drug discovery

(2012) Jamie Mallinson et al.   Future Medicinal Chemistry

Synthesis, Structure–Activity Analysis, and Biological Evaluation of Sanguinamide B Analogues

(2012) Hendra Wahyudi et al.   JOURNAL OF ORGANIC CHEMISTRY

Intestinal Permeability of Cyclic Peptides: Common Key Backbone Motifs Identified

(2012) Johannes G. Beck et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Finding the sweet spot: the role of nature and nurture in medicinal chemistry

(2012) Michael M. Hann et al.   NATURE REVIEWS DRUG DISCOVERY

Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance

(2012) Arthur C. Rand et al.   MedChemComm

Macrocycles That Inhibit the Binding between Heat Shock Protein 90 and TPR-Containing Proteins

(2011) Veronica C. Ardi et al.   ACS Chemical Biology

Cilengitide: The First Anti-Angiogenic Small Molecule Drug Candidate. Design, Synthesis and Clinical Evaluation

(2011) Carlos Mas-Moruno et al.   Anti-Cancer Agents in Medicinal Chemistry

Macrocycles Are Great Cycles: Applications, Opportunities, and Challenges of Synthetic Macrocycles in Drug Discovery

(2011) Eric Marsault et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of sansalvamide A peptidomimetics: triazole, oxazole, thiazole, and pseudoproline containing compounds

(2011) Melinda R. Davis et al.   TETRAHEDRON

Design and synthesis of Hsp90 inhibitors: Exploring the SAR of Sansalvamide A derivatives

(2010) Robert P. Sellers et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Mechanistic Studies of Sansalvamide A-Amide: An Allosteric Modulator of Hsp90

(2010) Robert C. Vasko et al.   ACS Medicinal Chemistry Letters

Thermodynamic and Structural Effects of Macrocyclic Constraints in Protein−Ligand Interactions

(2010) John E. DeLorbe et al.   ACS Medicinal Chemistry Letters

A comprehensive study of Sansalvamide A derivatives: The structure–activity relationships of 78 derivatives in two pancreatic cancer cell lines

(2009) Po-Shen Pan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

N-Methylation of Peptides: A New Perspective in Medicinal Chemistry

(2008) Jayanta Chatterjee et al.   ACCOUNTS OF CHEMICAL RESEARCH

Comprehensive Study of Sansalvamide A Derivatives and their Structure–Activity Relationships against Drug-Resistant Colon Cancer Cell Lines

(2008) Katerina Otrubova et al.   JOURNAL OF MEDICINAL CHEMISTRY

The exploration of macrocycles for drug discovery — an underexploited structural class

(2008) Edward M. Driggers et al.   NATURE REVIEWS DRUG DISCOVERY