Macrocycles: MCR synthesis and applications in drug discovery

Eman M.M. Abdelraheem; Shabnam Shaabani; Alexander Dömling

doi:10.1016/j.ddtec.2018.06.008

Macrocycles: MCR synthesis and applications in drug discovery

Eman M.M. Abdelraheem
, Shabnam Shaabani
, Alexander Dömling

Research output: Contribution to Journal › Review article › Academic › peer-review

Abstract

Macrocycles are an emerging and largely underexploited part of chemical space where potential drugs for difficult genomic targets can be discovered. Macrocycles can have advantages over their natural twins such as better control over synthesis, physicochemical properties and target binding. Fast and convergent synthesis pathways are underdeveloped. Multicomponent reaction (MCR) chemistry is very well suited for the synthesis of a diverse range of macrocycles and is also able to generate great levels of molecular diversity and complexity at low synthetic costs.

Original language	English
Pages (from-to)	11-17
Journal	Drug Discovery Today: Technologies
Volume	29
DOIs	https://doi.org/10.1016/j.ddtec.2018.06.008
Publication status	Published - 1 Nov 2018
Externally published	Yes

Funding

The work in the PIs laboratory was financially supported from the NIH (NIH 2R01GM097082-05 ) and by the Innovative Medicines Initiative Joint Undertaking under grant agreement No. 115489 , resources of which are composed of financial contribution from the European Union’s Seventh Framework Programme ( FP7/2007-2013 ) and EFPIA companies’ in-kind. Moreover, funding has also been received from the European Union’s Horizon 2020 research and innovation programme under MSC ITN “Accelerated Early stage drug dIScovery” (AEGIS), grant agreement No. 675555 . SS is grateful for a postdoctoral fellowship from KWF (Grant Agreement No. 10504 ). The work in the PIs laboratory was financially supported from the NIH (NIH 2R01GM097082-05) and by the Innovative Medicines Initiative Joint Undertaking under grant agreement No. 115489, resources of which are composed of financial contribution from the European Union's Seventh Framework Programme (FP7/2007-2013) and EFPIA companies? in-kind. Moreover, funding has also been received from the European Union's Horizon 2020 research and innovation programme under MSC ITN ?Accelerated Early stage drug dIScovery? (AEGIS), grant agreement No. 675555. SS is grateful for a postdoctoral fellowship from KWF (Grant Agreement No. 10504). The work in the PIs laboratory was financially supported from the NIH (NIH 2R01GM097082-05) and by the Innovative Medicines Initiative Joint Undertaking under grant agreement No. 115489, resources of which are composed of financial contribution from the European Union's Seventh Framework Programme (FP7/2007-2013) and EFPIA companies’ in-kind. Moreover, funding has also been received from the European Union's Horizon 2020 research and innovation programme under MSC ITN “Accelerated Early stage drug dIScovery” (AEGIS), grant agreement No. 675555. SS is grateful for a postdoctoral fellowship from KWF (Grant Agreement No. 10504).

Funders	Funder number
National Institutes of Health	2R01GM097082-05
European Federation of Pharmaceutical Industries and Associations
European Commission
KWF Kankerbestrijding	10504
Seventh Framework Programme
Horizon 2020	675555
Kommission zur Förderung der wissenschaftlichen Forschung )
Innovative Medicines Initiative	115489

Access to Document

10.1016/j.ddtec.2018.06.008

Persistent URL (handle)

Persistent link

Cite this

@article{a20ac4b3f809459299b883889cd587ed,

title = "Macrocycles: MCR synthesis and applications in drug discovery",

abstract = "Macrocycles are an emerging and largely underexploited part of chemical space where potential drugs for difficult genomic targets can be discovered. Macrocycles can have advantages over their natural twins such as better control over synthesis, physicochemical properties and target binding. Fast and convergent synthesis pathways are underdeveloped. Multicomponent reaction (MCR) chemistry is very well suited for the synthesis of a diverse range of macrocycles and is also able to generate great levels of molecular diversity and complexity at low synthetic costs.",

author = "Abdelraheem, \{Eman M.M.\} and Shabnam Shaabani and Alexander D{\"o}mling",

year = "2018",

month = nov,

day = "1",

doi = "10.1016/j.ddtec.2018.06.008",

language = "English",

volume = "29",

pages = "11--17",

journal = "Drug Discovery Today: Technologies",

issn = "1740-6749",

publisher = "Elsevier Ltd",

}

TY - JOUR

T1 - Macrocycles

T2 - MCR synthesis and applications in drug discovery

AU - Abdelraheem, Eman M.M.

AU - Shaabani, Shabnam

AU - Dömling, Alexander

PY - 2018/11/1

Y1 - 2018/11/1

N2 - Macrocycles are an emerging and largely underexploited part of chemical space where potential drugs for difficult genomic targets can be discovered. Macrocycles can have advantages over their natural twins such as better control over synthesis, physicochemical properties and target binding. Fast and convergent synthesis pathways are underdeveloped. Multicomponent reaction (MCR) chemistry is very well suited for the synthesis of a diverse range of macrocycles and is also able to generate great levels of molecular diversity and complexity at low synthetic costs.

AB - Macrocycles are an emerging and largely underexploited part of chemical space where potential drugs for difficult genomic targets can be discovered. Macrocycles can have advantages over their natural twins such as better control over synthesis, physicochemical properties and target binding. Fast and convergent synthesis pathways are underdeveloped. Multicomponent reaction (MCR) chemistry is very well suited for the synthesis of a diverse range of macrocycles and is also able to generate great levels of molecular diversity and complexity at low synthetic costs.

UR - http://www.scopus.com/inward/record.url?scp=85049726643&partnerID=8YFLogxK

U2 - 10.1016/j.ddtec.2018.06.008

DO - 10.1016/j.ddtec.2018.06.008

M3 - Review article

SN - 1740-6749

VL - 29

SP - 11

EP - 17

JO - Drug Discovery Today: Technologies

JF - Drug Discovery Today: Technologies

ER -

Macrocycles: MCR synthesis and applications in drug discovery

Abstract

Funding

Access to Document

Persistent URL (handle)

Other files and links

Fingerprint

Cite this