An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review
The profound pharmacological properties of macrocyclic compounds have led to their development as drugs. In conformationally pre-organized ring structures, the multiple functions and stereochemical complexity provided by the macrocycle result in high affinity and selectivity of protein targets while...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/9/2837 |
| _version_ | 1827671999192760320 |
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| author | Yan Liang Ru Fang Qiu Rao |
| author_facet | Yan Liang Ru Fang Qiu Rao |
| author_sort | Yan Liang |
| collection | DOAJ |
| description | The profound pharmacological properties of macrocyclic compounds have led to their development as drugs. In conformationally pre-organized ring structures, the multiple functions and stereochemical complexity provided by the macrocycle result in high affinity and selectivity of protein targets while maintaining sufficient bioavailability to reach intracellular locations. Therefore, the construction of macrocycles is an ideal choice to solve the problem of “undruggable” targets. Inspection of 68 macrocyclic drugs on the market showed that 10 of them were used to treat cancer, but this structural class still has been poorly explored within drug discovery. This perspective considers the macrocyclic compounds used for anti-tumor with different targets, their advantages and disadvantages, and the various synthetic methods of them. |
| first_indexed | 2024-03-10T03:53:34Z |
| format | Article |
| id | doaj.art-572dc8640a804ee8b3d4aa8f2ca78ba5 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T03:53:34Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-572dc8640a804ee8b3d4aa8f2ca78ba52023-11-23T08:50:31ZengMDPI AGMolecules1420-30492022-04-01279283710.3390/molecules27092837An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic ReviewYan Liang0Ru Fang1Qiu Rao2Department of Pathology, Jinling Hospital, Nanjing University School of Medicine, Nanjing 210000, ChinaDepartment of Pathology, Jinling Hospital, Nanjing University School of Medicine, Nanjing 210000, ChinaDepartment of Pathology, Jinling Hospital, Nanjing University School of Medicine, Nanjing 210000, ChinaThe profound pharmacological properties of macrocyclic compounds have led to their development as drugs. In conformationally pre-organized ring structures, the multiple functions and stereochemical complexity provided by the macrocycle result in high affinity and selectivity of protein targets while maintaining sufficient bioavailability to reach intracellular locations. Therefore, the construction of macrocycles is an ideal choice to solve the problem of “undruggable” targets. Inspection of 68 macrocyclic drugs on the market showed that 10 of them were used to treat cancer, but this structural class still has been poorly explored within drug discovery. This perspective considers the macrocyclic compounds used for anti-tumor with different targets, their advantages and disadvantages, and the various synthetic methods of them.https://www.mdpi.com/1420-3049/27/9/2837macrocyclic compoundantitumorsynthetic methods |
| spellingShingle | Yan Liang Ru Fang Qiu Rao An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review Molecules macrocyclic compound antitumor synthetic methods |
| title | An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review |
| title_full | An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review |
| title_fullStr | An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review |
| title_full_unstemmed | An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review |
| title_short | An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review |
| title_sort | insight into the medicinal chemistry perspective of macrocyclic derivatives with antitumor activity a systematic review |
| topic | macrocyclic compound antitumor synthetic methods |
| url | https://www.mdpi.com/1420-3049/27/9/2837 |
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