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

2017-09-19T10:49:26+00:00 August 28th, 2013|on Macrocycles, Publications|

by Fabrizio Giordanetto and Jan Kihlberg

Macrocycles are ideal in efforts to tackle “difficult” targets, but our understanding of what makes them cell permeable and orally bioavailable is limited. Analysis of approximately 100 macrocyclic drugs and clinical candidates revealed that macrocycles are predominantly used for infectious disease and in oncology and that most belong to the macrolide or cyclic peptide class. A significant number (N = 34) of these macrocycles are administered […]

Macrocycles and Constrained Peptides

2017-09-19T10:50:05+00:00 April 11th, 2013|on Macrocycles, Publications|

Macrocycles and constrained peptides, generally defined as cyclic small molecules or peptides of 500–2,000 Da, have undergone a rebirth over the last five years in drug discovery, due mainly to the introduction of new approaches for their synthesis and screening. This scientific progress has fueled a burst of business activity, with at least 12 biotech companies in the space, of which almost half were founded in the last 5 years.

This special collection from SciBX: Science-Business eXchange p […]

Macrocycles in New Drug Discovery

2017-09-19T10:50:41+00:00 August 2nd, 2012|on Macrocycles, Publications|

by Jamie Mallinson and Ian Collins

The use of drug-like macrocycles is emerging as an exciting area of medicinal chemistry, with several recent examples highlighting the favorable changes in biological and physicochemical properties that macrocyclization can afford. Natural product macrocycles and their synthetic derivatives have long been clinically useful and attention is now being focused on the wider use of macrocyclic scaffolds in medicinal chemistry in the search for new drugs […]