Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell lines
The current study describes, a novel combinatorial library of substituted fused pyrimido[3,2–e]pyrrolo[1,2-a]piperazine and pyrido[3,2-b]pyrrolo[1,2-d][1,4]diazepin heterocycles procured via utilization of suzuki coupling and acid amine coupling protocols. The synthesized compounds were screened for...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2023-01-01
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| Series: | Results in Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S221171562200426X |
| _version_ | 1797799084241715200 |
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| author | Jignesh B. Timaniya Paranjay H. Parikh Mrugesh J. Patel Gayatri Dave Kaushal P. Patel |
| author_facet | Jignesh B. Timaniya Paranjay H. Parikh Mrugesh J. Patel Gayatri Dave Kaushal P. Patel |
| author_sort | Jignesh B. Timaniya |
| collection | DOAJ |
| description | The current study describes, a novel combinatorial library of substituted fused pyrimido[3,2–e]pyrrolo[1,2-a]piperazine and pyrido[3,2-b]pyrrolo[1,2-d][1,4]diazepin heterocycles procured via utilization of suzuki coupling and acid amine coupling protocols. The synthesized compounds were screened for their in vitro cytotoxic activity over nine different cancer cell lines such as U-251, Panc-1, MCF-7, HepG2, DU-145, A549, 786-O, OVCAR3 and HCT-116 as well as on non-cancerous cell lines like normal human lung cell line WI38 and Mouse embryonic normal cell line NIH3T3 to evaluate safety profile of synthesized compounds. The bioassay results indicates that compound Cpd-J2 to be most potent among all the synthesized compounds towards ovary cancer cell lines (OVCAR-3) with promising activity value (EC50: 6.3 μM) relative to standard doxorubicin (EC50: 0.2 μM). |
| first_indexed | 2024-03-13T04:13:36Z |
| format | Article |
| id | doaj.art-7c94e99778104d2e95d0dc87820c7293 |
| institution | Directory Open Access Journal |
| issn | 2211-7156 |
| language | English |
| last_indexed | 2024-03-13T04:13:36Z |
| publishDate | 2023-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Results in Chemistry |
| spelling | doaj.art-7c94e99778104d2e95d0dc87820c72932023-06-21T06:51:41ZengElsevierResults in Chemistry2211-71562023-01-015100707Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell linesJignesh B. Timaniya0Paranjay H. Parikh1Mrugesh J. Patel2Gayatri Dave3Kaushal P. Patel4Department of Advanced Organic Chemistry, P. D. Patel Institute of Applied Sciences, Charotar University of Science and Technology, Gujarat 388421, IndiaDepartment of Advanced Organic Chemistry, P. D. Patel Institute of Applied Sciences, Charotar University of Science and Technology, Gujarat 388421, IndiaDepartment of Advanced Organic Chemistry, P. D. Patel Institute of Applied Sciences, Charotar University of Science and Technology, Gujarat 388421, IndiaDepartment of Biological Sciences, P. D. Patel Institute of Applied Sciences, Charotar University of Science and Technology, Gujarat 388421, IndiaDepartment of Advanced Organic Chemistry, P. D. Patel Institute of Applied Sciences, Charotar University of Science and Technology, Gujarat 388421, India; Corresponding author.The current study describes, a novel combinatorial library of substituted fused pyrimido[3,2–e]pyrrolo[1,2-a]piperazine and pyrido[3,2-b]pyrrolo[1,2-d][1,4]diazepin heterocycles procured via utilization of suzuki coupling and acid amine coupling protocols. The synthesized compounds were screened for their in vitro cytotoxic activity over nine different cancer cell lines such as U-251, Panc-1, MCF-7, HepG2, DU-145, A549, 786-O, OVCAR3 and HCT-116 as well as on non-cancerous cell lines like normal human lung cell line WI38 and Mouse embryonic normal cell line NIH3T3 to evaluate safety profile of synthesized compounds. The bioassay results indicates that compound Cpd-J2 to be most potent among all the synthesized compounds towards ovary cancer cell lines (OVCAR-3) with promising activity value (EC50: 6.3 μM) relative to standard doxorubicin (EC50: 0.2 μM).http://www.sciencedirect.com/science/article/pii/S221171562200426XPyridoPyrimido PiperazineAzepineAnticancer |
| spellingShingle | Jignesh B. Timaniya Paranjay H. Parikh Mrugesh J. Patel Gayatri Dave Kaushal P. Patel Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell lines Results in Chemistry Pyrido Pyrimido Piperazine Azepine Anticancer |
| title | Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell lines |
| title_full | Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell lines |
| title_fullStr | Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell lines |
| title_full_unstemmed | Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell lines |
| title_short | Design, synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives: In vitro cytotoxicity study over various cancer cell lines |
| title_sort | design synthesis and evaluation of novel substituted fused pyrido diazepine and pyrimido piperazine derivatives in vitro cytotoxicity study over various cancer cell lines |
| topic | Pyrido Pyrimido Piperazine Azepine Anticancer |
| url | http://www.sciencedirect.com/science/article/pii/S221171562200426X |
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