Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones

Vankadari Srinivasarao; Chaturvedula Radha Krishna; Macha Ramesh; Tigulla Parthasarathy

doi:doi:10.11648/j.mc.20130101.11

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Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones

Vankadari Srinivasarao, Chaturvedula Radha Krishna, Macha Ramesh, Tigulla Parthasarathy

Published in Modern Chemistry (Volume 1, Issue 1)

Received: 26 November 2012 Accepted: Published: 20 February 2013

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Abstract

In a wide search program toward new anticancer agents, a series of Aromatic chalcones have been synthesized by condensing benzaldehyde derivatives with arylmethylcetone in potassium hydroxide ethanol according to the Claisen-Schmidth condensation at room temperature. The synthetic chalcones have been determined by IR spectroscopy and 1H-NMR spectroscopy. The anticancer activitiesof the compounds were evaluated against in vitro using human tumour cell lines of Jurkat and HL-60 cell lines and MTT assay. From the series, two compounds(4,15) exhibited potent growth inhibi-tory effects against the proliferation of human T-lymphocyte leukemia compared to the parent unsubstitutedchalcone. The result shows that the electron donating groups moiety may increase anticancer activity. Aromatic chalcones with hydroxyl group,methoxy group on A ring at positions 2 or 3 are considered as lead compounds for generation of new potential anticancer drugs in future.Similarly,the compounds(7,12) exhibited potent growth inhibitory effects against HL-60 cells. The results are very encouraging. Future studies include testing the compounds in vivo with and without radiation. Docking studies with 1NKP have shown that the compound 17 has highest IC50 against human leukemia cells (HL-60).

Published in	Modern Chemistry (Volume 1, Issue 1)
DOI	10.11648/j.mc.20130101.11
Page(s)	1-7
Creative Commons	This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.
Copyright	Copyright © The Author(s), 2024. Published by Science Publishing Group

Keywords

Aromatic Chalcones Synthesis, Anticancer Activity, Docking Studies, Mtt Assay

References

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Vankadari Srinivasarao, Chaturvedula Radha Krishna, Macha Ramesh, Tigulla Parthasarathy. (2013). Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones. Modern Chemistry, 1(1), 1-7. https://doi.org/10.11648/j.mc.20130101.11

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ACS Style

Vankadari Srinivasarao; Chaturvedula Radha Krishna; Macha Ramesh; Tigulla Parthasarathy. Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones. Mod. Chem. 2013, 1(1), 1-7. doi: 10.11648/j.mc.20130101.11

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AMA Style

Vankadari Srinivasarao, Chaturvedula Radha Krishna, Macha Ramesh, Tigulla Parthasarathy. Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones. Mod Chem. 2013;1(1):1-7. doi: 10.11648/j.mc.20130101.11

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@article{10.11648/j.mc.20130101.11,
  author = {Vankadari Srinivasarao and Chaturvedula Radha Krishna and Macha Ramesh and Tigulla Parthasarathy},
  title = {Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones},
  journal = {Modern Chemistry},
  volume = {1},
  number = {1},
  pages = {1-7},
  doi = {10.11648/j.mc.20130101.11},
  url = {https://doi.org/10.11648/j.mc.20130101.11},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.mc.20130101.11},
  abstract = {In a wide search program toward new anticancer agents, a series of Aromatic chalcones have been synthesized by condensing benzaldehyde derivatives with arylmethylcetone in potassium hydroxide ethanol according to the Claisen-Schmidth condensation at room temperature. The synthetic chalcones have been determined by IR spectroscopy and 1H-NMR spectroscopy. The anticancer activitiesof the compounds were evaluated against in vitro using human tumour cell lines of Jurkat and HL-60 cell lines and MTT assay. From the series, two compounds(4,15) exhibited potent growth inhibi-tory effects against the proliferation of human T-lymphocyte leukemia compared to the parent unsubstitutedchalcone. The result shows that the electron donating groups moiety may increase anticancer activity. Aromatic chalcones with hydroxyl group,methoxy group on A ring at positions 2 or 3 are considered as lead compounds for generation of new potential anticancer drugs in future.Similarly,the compounds(7,12) exhibited potent growth inhibitory effects against HL-60 cells. The results are very encouraging. Future studies include testing the compounds in vivo with and without radiation. Docking studies with 1NKP have shown that the compound 17 has highest IC50 against human leukemia cells (HL-60).},
 year = {2013}
}

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TY  - JOUR
T1  - Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones
AU  - Vankadari Srinivasarao
AU  - Chaturvedula Radha Krishna
AU  - Macha Ramesh
AU  - Tigulla Parthasarathy
Y1  - 2013/02/20
PY  - 2013
N1  - https://doi.org/10.11648/j.mc.20130101.11
DO  - 10.11648/j.mc.20130101.11
T2  - Modern Chemistry
JF  - Modern Chemistry
JO  - Modern Chemistry
SP  - 1
EP  - 7
PB  - Science Publishing Group
SN  - 2329-180X
UR  - https://doi.org/10.11648/j.mc.20130101.11
AB  - In a wide search program toward new anticancer agents, a series of Aromatic chalcones have been synthesized by condensing benzaldehyde derivatives with arylmethylcetone in potassium hydroxide ethanol according to the Claisen-Schmidth condensation at room temperature. The synthetic chalcones have been determined by IR spectroscopy and 1H-NMR spectroscopy. The anticancer activitiesof the compounds were evaluated against in vitro using human tumour cell lines of Jurkat and HL-60 cell lines and MTT assay. From the series, two compounds(4,15) exhibited potent growth inhibi-tory effects against the proliferation of human T-lymphocyte leukemia compared to the parent unsubstitutedchalcone. The result shows that the electron donating groups moiety may increase anticancer activity. Aromatic chalcones with hydroxyl group,methoxy group on A ring at positions 2 or 3 are considered as lead compounds for generation of new potential anticancer drugs in future.Similarly,the compounds(7,12) exhibited potent growth inhibitory effects against HL-60 cells. The results are very encouraging. Future studies include testing the compounds in vivo with and without radiation. Docking studies with 1NKP have shown that the compound 17 has highest IC50 against human leukemia cells (HL-60).
VL  - 1
IS  - 1
ER  -

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Author Information

Vankadari Srinivasarao

Department of chemistry, University College of Science, Osmania University, Saifabad, Hyderabad, India
Chaturvedula Radha Krishna

Department of chemistry, University College of Science, Osmania University, Saifabad, Hyderabad, India
Macha Ramesh

Department of chemistry, University College of Science, Osmania University, Saifabad, Hyderabad, India
Tigulla Parthasarathy

Department of chemistry, University College of Science, Osmania University, Saifabad, Hyderabad, India

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APA Style

Vankadari Srinivasarao, Chaturvedula Radha Krishna, Macha Ramesh, Tigulla Parthasarathy. (2013). Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones. Modern Chemistry, 1(1), 1-7. https://doi.org/10.11648/j.mc.20130101.11

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ACS Style

Vankadari Srinivasarao; Chaturvedula Radha Krishna; Macha Ramesh; Tigulla Parthasarathy. Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones. Mod. Chem. 2013, 1(1), 1-7. doi: 10.11648/j.mc.20130101.11

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AMA Style

Vankadari Srinivasarao, Chaturvedula Radha Krishna, Macha Ramesh, Tigulla Parthasarathy. Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones. Mod Chem. 2013;1(1):1-7. doi: 10.11648/j.mc.20130101.11

Copy | Download

@article{10.11648/j.mc.20130101.11,
  author = {Vankadari Srinivasarao and Chaturvedula Radha Krishna and Macha Ramesh and Tigulla Parthasarathy},
  title = {Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones},
  journal = {Modern Chemistry},
  volume = {1},
  number = {1},
  pages = {1-7},
  doi = {10.11648/j.mc.20130101.11},
  url = {https://doi.org/10.11648/j.mc.20130101.11},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.mc.20130101.11},
  abstract = {In a wide search program toward new anticancer agents, a series of Aromatic chalcones have been synthesized by condensing benzaldehyde derivatives with arylmethylcetone in potassium hydroxide ethanol according to the Claisen-Schmidth condensation at room temperature. The synthetic chalcones have been determined by IR spectroscopy and 1H-NMR spectroscopy. The anticancer activitiesof the compounds were evaluated against in vitro using human tumour cell lines of Jurkat and HL-60 cell lines and MTT assay. From the series, two compounds(4,15) exhibited potent growth inhibi-tory effects against the proliferation of human T-lymphocyte leukemia compared to the parent unsubstitutedchalcone. The result shows that the electron donating groups moiety may increase anticancer activity. Aromatic chalcones with hydroxyl group,methoxy group on A ring at positions 2 or 3 are considered as lead compounds for generation of new potential anticancer drugs in future.Similarly,the compounds(7,12) exhibited potent growth inhibitory effects against HL-60 cells. The results are very encouraging. Future studies include testing the compounds in vivo with and without radiation. Docking studies with 1NKP have shown that the compound 17 has highest IC50 against human leukemia cells (HL-60).},
 year = {2013}
}

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TY  - JOUR
T1  - Synthesis, in vitro Anticancer Activity Evaluation and Docking Investigations of Novel Aromatic Chalcones
AU  - Vankadari Srinivasarao
AU  - Chaturvedula Radha Krishna
AU  - Macha Ramesh
AU  - Tigulla Parthasarathy
Y1  - 2013/02/20
PY  - 2013
N1  - https://doi.org/10.11648/j.mc.20130101.11
DO  - 10.11648/j.mc.20130101.11
T2  - Modern Chemistry
JF  - Modern Chemistry
JO  - Modern Chemistry
SP  - 1
EP  - 7
PB  - Science Publishing Group
SN  - 2329-180X
UR  - https://doi.org/10.11648/j.mc.20130101.11
AB  - In a wide search program toward new anticancer agents, a series of Aromatic chalcones have been synthesized by condensing benzaldehyde derivatives with arylmethylcetone in potassium hydroxide ethanol according to the Claisen-Schmidth condensation at room temperature. The synthetic chalcones have been determined by IR spectroscopy and 1H-NMR spectroscopy. The anticancer activitiesof the compounds were evaluated against in vitro using human tumour cell lines of Jurkat and HL-60 cell lines and MTT assay. From the series, two compounds(4,15) exhibited potent growth inhibi-tory effects against the proliferation of human T-lymphocyte leukemia compared to the parent unsubstitutedchalcone. The result shows that the electron donating groups moiety may increase anticancer activity. Aromatic chalcones with hydroxyl group,methoxy group on A ring at positions 2 or 3 are considered as lead compounds for generation of new potential anticancer drugs in future.Similarly,the compounds(7,12) exhibited potent growth inhibitory effects against HL-60 cells. The results are very encouraging. Future studies include testing the compounds in vivo with and without radiation. Docking studies with 1NKP have shown that the compound 17 has highest IC50 against human leukemia cells (HL-60).
VL  - 1
IS  - 1
ER  -

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