The DOI matches its Crossref record; 82 of the 82 references it cites were found in a registry or an index.
Macrocycles In New Drug Discovery
Abstract
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 for increasingly challenging targets. With the increasing awareness of concepts of drug-likeness and the dangers of 'molecular obesity', functionalized macrocyclic scaffolds could provide a way to generate ligand-efficient molecules with enhanced properties. In this review we will separately discuss the effects of macrocyclization upon potency, selectivity and physicochemical properties, concentrating on recent case histories in oncology drug discovery. Additionally, we will highlight selected advances in the synthesis of macrocycles and provide an outlook on the future use of macrocyclic scaffolds in medicinal chemistry.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00129-0 · Cited by 18,139
Molecular properties that influence the oral bioavailability of drug candidates
Veber, D. F., Johnson, S. R., Cheng, H.-Y., Smith, B. R., Ward, K. W., & Kopple, K. D. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm020017n · Cited by 8,420
Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success
Lovering, F., Bikker, J., & Humblet, C. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm901241e · Cited by 4,495
Advanced Organic Chemistry: Reactions, Mechanisms, and Structure
March, J. (1977) · Andalas University Repository (Andalas University) · Cited by 4,022
Ligand efficiency: a useful metric for lead selection
Hopkins, A. L., Groom, C. R., & Alex, A. (2004) · Drug Discovery Today · doi:10.1016/s1359-6446(04)03069-7 · Cited by 1,846
Natural products in drug discovery
Harvey, A. L. (2008) · Drug Discovery Today · doi:10.1016/j.drudis.2008.07.004 · Cited by 1,832
A Medicinal Chemist’s Guide to Molecular Interactions
Bissantz, C., Kuhn, B., & Stahl, M. (2010) · Journal of Medicinal Chemistry · doi:10.1021/jm100112j · Cited by 1,731
The exploration of macrocycles for drug discovery — an underexploited structural class
Driggers, E. M., Hale, S. P., Lee, J., & Terrett, N. K. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2590 · Cited by 1,370
Contemporary strategies for peptide macrocyclization
White, C. J., & Yudin, A. K. (2011) · Nature Chemistry · doi:10.1038/nchem.1062 · Cited by 1,088
Current development of mTOR inhibitors as anticancer agents
Faivre, S., Kroemer, G., & Raymond, E. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd2062 · Cited by 1,000
Cited by
A review on recent developments of indole-containing antiviral agents
Zhang, M.-Z., Chen, Q., & Yang, G.-F. (2015) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.10.065 · Cited by 887
Oral Druggable Space beyond the Rule of 5: Insights from Drugs and Clinical Candidates
Doak, B. C., Over, B., Giordanetto, F., & Kihlberg, J. (2014) · Chemistry & Biology · doi:10.1016/j.chembiol.2014.08.013 · Cited by 835
Villar, E. A., Beglov, D., Chennamadhavuni, S., Porco, J. A., Kozakov, D., Vajda, S., & Whitty, A. (2014) · Nature Chemical Biology · doi:10.1038/nchembio.1584 · Cited by 400
New Modalities for Challenging Targets in Drug Discovery
Valeur, E., Guéret, S. M., Adihou, H., Gopalakrishnan, R., Lemurell, M., Waldmann, H., Grossmann, T. N., & Plowright, A. T. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201611914 · Cited by 382
Electrochemical Late-Stage Functionalization
Wang, Y., Dana, S., Long, H., Xu, Y., Li, Y., Kaplaneris, N., & Ackermann, L. (2023) · Chemical Reviews · doi:10.1021/acs.chemrev.3c00158 · Cited by 361
Metadata
- Authors
- Mallinson, J., & Collins, I.
- Venue
- Future Medicinal Chemistry
- Publisher
- Informa UK Limited
- Published
- 2012-07
- Volume
- 4
- Issue
- 11
- Pages
- 1409-1438
- ISSN
- 1756-8919 (ISSN-L)
- 1756-8927
- OpenAlex
- W2097888801
- Cited by
- 468
- References
- 82
- FWCI
- 7.90
- Type
- journal article
- Language
- en
- Open access
- closed
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: Macrocycles In New Drug Discovery. https://app.cochat.ai/papers/10.4155/fmc.12.93
- The paper
- Mallinson, J., & Collins, I. (2012). Macrocycles In New Drug Discovery. Future Medicinal Chemistry. https://doi.org/10.4155/fmc.12.93
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
