Abstract
Background: A new series of quinazoline linked chalcone conjugates were synthesized and evaluated for their in vitro cytotoxicity.
Methods: The quinazoline-chalcone derivatives (13a-r) have been prepared by the Claisen-Schmidt condensation of various substituted benzaldehydes (12a-r) with substituted l-(4-(3,4- dihydroquinazolin-4-ylamino)phenyl)ethanone (11a-b) in the presence of aqueous NaOH. Three potential compounds 13f, 13g and 13h exhibited cytotoxicity against leukemia (GI50 value of 1.07, 0.26 and 0.24 µM), Non-small lung (GI50 values of 2.05,1.32 and 0.23 µM), colon (GI50 values of 0.54, 0.34 and 0.34 µM) and breast (GI50 values of 2.17, 1.84 and 0.22 µM) cell line, respectively.
Results and Conclusion: Based on these biological results, it is evident that compound 13h has the potential to be considered for further detailed studies either alone or in combination with existing therapies as potential anticancer agents.
Keywords: In vitro, cytotoxic studies, hybrid molecules, quinazolines, chalcone derivatives, potential anticancer agents.
Letters in Drug Design & Discovery
Title:Novel Hybrid Molecules of Quinazoline Chalcone Derivatives: Synthesis and Study of in vitro Cytotoxic Activities
Volume: 15 Issue: 7
Author(s): Arunkumar Thiriveedhi*, Ratnakaram Venkata Nadh, Navuluri Srinivasu and Kishore Kaushal
Affiliation:
- Division of Chemistry, Department of Science and Humanities, Vignan`s Foundation for Science Technology and Research University, Guntur-522213,India
Keywords: In vitro, cytotoxic studies, hybrid molecules, quinazolines, chalcone derivatives, potential anticancer agents.
Abstract: Background: A new series of quinazoline linked chalcone conjugates were synthesized and evaluated for their in vitro cytotoxicity.
Methods: The quinazoline-chalcone derivatives (13a-r) have been prepared by the Claisen-Schmidt condensation of various substituted benzaldehydes (12a-r) with substituted l-(4-(3,4- dihydroquinazolin-4-ylamino)phenyl)ethanone (11a-b) in the presence of aqueous NaOH. Three potential compounds 13f, 13g and 13h exhibited cytotoxicity against leukemia (GI50 value of 1.07, 0.26 and 0.24 µM), Non-small lung (GI50 values of 2.05,1.32 and 0.23 µM), colon (GI50 values of 0.54, 0.34 and 0.34 µM) and breast (GI50 values of 2.17, 1.84 and 0.22 µM) cell line, respectively.
Results and Conclusion: Based on these biological results, it is evident that compound 13h has the potential to be considered for further detailed studies either alone or in combination with existing therapies as potential anticancer agents.
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Cite this article as:
Thiriveedhi Arunkumar *, Nadh Venkata Ratnakaram , Srinivasu Navuluri and Kaushal Kishore , Novel Hybrid Molecules of Quinazoline Chalcone Derivatives: Synthesis and Study of in vitro Cytotoxic Activities, Letters in Drug Design & Discovery 2018; 15 (7) . https://dx.doi.org/10.2174/1570180814666171013162148
DOI https://dx.doi.org/10.2174/1570180814666171013162148 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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