9-Arylimino noscapinoids as potent tubulin binding anticancer agent: chemical synthesis and cellular evaluation against breast tumour cells
@article{Patel20219AryliminoNA,
title={9-Arylimino noscapinoids as potent tubulin binding anticancer agent: chemical synthesis and cellular evaluation against breast tumour cells},
author={Akul K. Patel and Rajesh Kumar Meher and P.K. Nagireddy and Pratyush Pragyandipta and Ravi Kumar Pedapati and Srinivas Kantevari and Pradeep Kumar Naik},
journal={SAR and QSAR in Environmental Research},
year={2021},
volume={32},
pages={269 - 291},
url={https://api.semanticscholar.org/CorpusID:232161419}
}These novel derivatives of noscapine have a great potential to be a novel therapeutic agent for breast cancers and arrest cell cycle in the G2/M-phase followed by induction of apoptosis.
5 Citations
Structure Based Design of Tubulin Binding 9-Arylimino Noscapinoids: Chemical Synthesis and Experimental Validation Against Breast Cancer Cell Lines
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It is concluded that 9-arylimino noscapinoids 4-6 have tremendous potential as chemotherapeutic agents for the treatment of breast cancer.
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A guide to the accessible tubulin-ligand structures is compiled here and different ligand and structure-based methods recently used for the successful selection and design of new Tubulin-targeting agents are reviewed.
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Chemistry, Medicine
The newly designed noscapinoid, 5e is an orally bioavailable, safe and effective anticancer agent with a potential for the treatment of cancer and might be a candidate for clinical evaluation.
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Medicine, Chemistry
The study reported here identified potent, third generation noscapinoids as new anti-cancer agents that perturbed DNA synthesis, delayed the cell cycle progression at G2/M phase, and induced apoptotic cell death in cancer cells.
In silico inspired design and synthesis of a novel tubulin-binding anti-cancer drug: folate conjugated noscapine (Targetin)
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Chemistry, Medicine
Chemical synthesis, tubulin-binding experiments, and anti-cancer activity in vitro corroborate fully well with the molecular modelling experiments.
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Chemistry, Medicine
The ‘blind docking’ approach as well as the reasonable accuracy of calculating ΔGbind using LIE–SGB model constitutes the first evidence that this class of compounds binds to tubulin at a site overlapping with colchicine-binding site or close to it.
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Medicine, Chemistry
9-nitro-nos has great potential to be a novel therapeutic agent for ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.
Rational Design of Novel Anti-microtubule Agent (9-Azido-Noscapine) from Quantitative Structure Activity Relationship (QSAR) Evaluation of Noscapinoids
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Chemistry, Medicine
To obtain systematic insight into the relationship between the structural framework of noscapine scaffold and its antitumor activity, the authors synthesized strategic derivatives (including two new ones in this article) that turned out to be very close to predicted pIC50.
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Chemistry, Medicine
Structural studies show that the cytotoxic agent 7A-O-demethoxy-amino-noscapine (7A-aminonoscapine) binds to the colchicine site of tubulin, and it is proposed that the anticancer activity of noscapine arises from a bioactive metabolite that binds toThe colchichine siteof tubulin to induce mitotic arrest through a microtubule cytoskeleton-based mechanism.
Synthesis and Antitumor Evaluation of Nitrovinyl Biphenyls: Anticancer Agents Based on Allocolchicines
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Chemistry, Medicine
A new class of nitrovinyl biphenyl compounds based on the structures of colchicines and allocolchicines were designed, synthesized, and shown to inhibit tubulin polymerization and cause mitotic…