Synthesis and anticancer activity of some pyrido[2,3- d ]pyrimidine derivatives as apoptosis inducers and cyclin-dependent kinase inhibitors
Due to emergence of resistance to available anticancer agents, there is a need to search for new cytotoxic agents. Pyrido[2,3- ]pyrimidines ( - ) and their tricyclic derivatives ( ) were prepared and screened for their cytotoxicity against breast MCF-7, prostate PC-3 and lung A-549 cancer cell lines...
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| Published in: | Future medicinal chemistry Vol. 11; no. 18; pp. 2395 - 2414 |
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| Main Authors: | , , , , |
| Format: | Journal Article |
| Language: | English |
| Published: |
England
01-09-2019
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| Subjects: | |
| Online Access: | Get full text |
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| Summary: | Due to emergence of resistance to available anticancer agents, there is a need to search for new cytotoxic agents.
Pyrido[2,3-
]pyrimidines (
-
) and their tricyclic derivatives (
) were prepared and screened for their cytotoxicity against breast MCF-7, prostate PC-3 and lung A-549 cancer cell lines as well as normal fibroblasts WI-38.
The most active compounds were
and
compared with doxorubicin. Moreover, compounds
and
induced apoptosis in PC-3 and MCF-7, respectively via activation of CASP3 (in PC-3 only), Bax, p53 and down regulation of Bcl2 in addition to CDK4/6 inhibition.
Pyrido[2,3-
]pyrimidine represents an important core for discovery of new potent cytotoxic agents acting on the cell cycle via apoptosis induction through either intrinsic or extrinsic pathways. |
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| Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
| ISSN: | 1756-8919 1756-8927 |
| DOI: | 10.4155/fmc-2019-0050 |