Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells
Swayamsiddha Kar
1
,
Gayathri Ramamoorthy
2
,
Kartik Mitra
2
,
S. Naveen
3
,
Mahesha
4
,
Sai Kiran Mavileti
1
,
N. K. Lokanath
4
,
Mukesh Doble
2
,
Nageswara Rao Golakoti
1
1
Department of Chemistry, Sri Sathya Sai Institute of Higher Learning, Prasanthi Nilayam, Andhra Pradesh 515134, India.
|
Publication type: Journal Article
Publication date: 2020-06-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
32331934
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Spirobibenzopyrans are an unexplored class of therapeutics. We report the anticancer activity of novel spirobibenzopyrans, synthesized by a one-pot reaction and extensively characterized. Structure of one of the spirobibenzopyran has been determined by the single crystal XRD technique. The in vitro anticancer activity of these derivatives across the NCI 60-cell line panel was evaluated and for the first time their mechanism of action against HeLa cells was probed via cell morphology analysis and cell cycle analysis. They were determined to be apoptosis inducers with cell cycle arrest in G0/G1 and S phase suggesting CDK-4 protein inhibition and the inhibition of DNA replication. The DNA inhibition was studied and confirmed using the alkaline comet assay for the compound CHX-4MO-SAL showing S phase inhibition. Further, conformity with the in silico Lipinski's score signify the potential of spirobibenzopyrans as anticancer leads.
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Total citations:
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Citations from 2025:
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GOST
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Kar S. et al. Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells // Bioorganic and Medicinal Chemistry Letters. 2020. Vol. 30. No. 12. p. 127199.
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Kar S., Ramamoorthy G., Mitra K., Naveen S., Mahesha, Mavileti S. K., Lokanath N. K., Doble M., Golakoti N. R. Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells // Bioorganic and Medicinal Chemistry Letters. 2020. Vol. 30. No. 12. p. 127199.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.bmcl.2020.127199
UR - https://doi.org/10.1016/j.bmcl.2020.127199
TI - Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Kar, Swayamsiddha
AU - Ramamoorthy, Gayathri
AU - Mitra, Kartik
AU - Naveen, S.
AU - Mahesha
AU - Mavileti, Sai Kiran
AU - Lokanath, N. K.
AU - Doble, Mukesh
AU - Golakoti, Nageswara Rao
PY - 2020
DA - 2020/06/01
PB - Elsevier
SP - 127199
IS - 12
VL - 30
PMID - 32331934
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (up to 50 authors)
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@article{2020_Kar,
author = {Swayamsiddha Kar and Gayathri Ramamoorthy and Kartik Mitra and S. Naveen and Mahesha and Sai Kiran Mavileti and N. K. Lokanath and Mukesh Doble and Nageswara Rao Golakoti},
title = {Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2020},
volume = {30},
publisher = {Elsevier},
month = {jun},
url = {https://doi.org/10.1016/j.bmcl.2020.127199},
number = {12},
pages = {127199},
doi = {10.1016/j.bmcl.2020.127199}
}
Cite this
MLA
Copy
Kar, Swayamsiddha, et al. “Synthesis of novel spirobibenzopyrans as potent anticancer leads inducing apoptosis in HeLa cells.” Bioorganic and Medicinal Chemistry Letters, vol. 30, no. 12, Jun. 2020, p. 127199. https://doi.org/10.1016/j.bmcl.2020.127199.