Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents
Lung cancer is the leading cause of death in men and women worldwide, affecting millions of people. Between the two types of lung cancers, non-small cell lung cancer (NSCLC) is more common than small cell lung cancer (SCLC). Besides surgery and radiotherapy, chemotherapy is the most important method...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/25/7/1615 |
| _version_ | 1797571722567745536 |
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| author | Jyothi Dhuguru Rachid Skouta |
| author_facet | Jyothi Dhuguru Rachid Skouta |
| author_sort | Jyothi Dhuguru |
| collection | DOAJ |
| description | Lung cancer is the leading cause of death in men and women worldwide, affecting millions of people. Between the two types of lung cancers, non-small cell lung cancer (NSCLC) is more common than small cell lung cancer (SCLC). Besides surgery and radiotherapy, chemotherapy is the most important method of treatment for lung cancer. Indole scaffold is considered one of the most privileged scaffolds in heterocyclic chemistry. Indole may serve as an effective probe for the development of new drug candidates against challenging diseases, including lung cancer. In this review, we will focus on discussing the existing indole based pharmacophores in the clinical and pre-clinical stages of development against lung cancer, along with the synthesis of some of the selected anti-lung cancer drugs. Moreover, the basic mechanism of action underlying indole based anti-lung cancer treatment, such as protein kinase inhibition, histone deacetylase inhibition, DNA topoisomerase inhibition, and tubulin inhibition will also be discussed. |
| first_indexed | 2024-03-10T20:44:33Z |
| format | Article |
| id | doaj.art-0db0350b18ec424d9827bb5aba191108 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T20:44:33Z |
| publishDate | 2020-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-0db0350b18ec424d9827bb5aba1911082023-11-19T20:23:40ZengMDPI AGMolecules1420-30492020-04-01257161510.3390/molecules25071615Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer AgentsJyothi Dhuguru0Rachid Skouta1Department of Biology, University of Massachusetts, Amherst, MA 01003, USADepartment of Biology, University of Massachusetts, Amherst, MA 01003, USALung cancer is the leading cause of death in men and women worldwide, affecting millions of people. Between the two types of lung cancers, non-small cell lung cancer (NSCLC) is more common than small cell lung cancer (SCLC). Besides surgery and radiotherapy, chemotherapy is the most important method of treatment for lung cancer. Indole scaffold is considered one of the most privileged scaffolds in heterocyclic chemistry. Indole may serve as an effective probe for the development of new drug candidates against challenging diseases, including lung cancer. In this review, we will focus on discussing the existing indole based pharmacophores in the clinical and pre-clinical stages of development against lung cancer, along with the synthesis of some of the selected anti-lung cancer drugs. Moreover, the basic mechanism of action underlying indole based anti-lung cancer treatment, such as protein kinase inhibition, histone deacetylase inhibition, DNA topoisomerase inhibition, and tubulin inhibition will also be discussed.https://www.mdpi.com/1420-3049/25/7/1615lung cancerindolenon-small cell lung cancerkinase inhibitionapoptosisDNA topoisomerase, histone deacetylase inhibition |
| spellingShingle | Jyothi Dhuguru Rachid Skouta Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents Molecules lung cancer indole non-small cell lung cancer kinase inhibition apoptosis DNA topoisomerase, histone deacetylase inhibition |
| title | Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents |
| title_full | Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents |
| title_fullStr | Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents |
| title_full_unstemmed | Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents |
| title_short | Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents |
| title_sort | role of indole scaffolds as pharmacophores in the development of anti lung cancer agents |
| topic | lung cancer indole non-small cell lung cancer kinase inhibition apoptosis DNA topoisomerase, histone deacetylase inhibition |
| url | https://www.mdpi.com/1420-3049/25/7/1615 |
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