Rational design, chemical synthesis and cellular evaluation of novel 1,3-diynyl derivatives of noscapine as potent tubulin binding anticancer agents.

@article{Patel2021RationalDC,
  title={Rational design, chemical synthesis and cellular evaluation of novel 1,3-diynyl derivatives of noscapine as potent tubulin binding anticancer agents.},
  author={Amiya Kumar Patel and Rajesh Kumar Meher and Praveen Kumar Reddy and Ravi Kumar Pedapati and Pratyush Pragyandipta and Srinivas Kantevari and Manas R. Naik and Pradeep Kumar Naik},
  journal={Journal of molecular graphics \& modelling},
  year={2021},
  volume={106},
  pages={
          107933
        }
}
3 Citations
Development of 1,3-diynyl derivatives of noscapine as potent tubulin binding anticancer agents for the management of breast cancer.
TLDR
1,3-diynyl-noscapinoids have great potential to be a novel therapeutic agent for breast cancers and cytotoxicity activity was validated based on cellular studies using human breast adenocarcinoma, a panel of primary breast tumor cells and one normal human embryonic kidney cell.
Structure Based Design of Tubulin Binding 9-Arylimino Noscapinoids: Chemical Synthesis and Experimental Validation Against Breast Cancer Cell Lines
TLDR
It is concluded that 9-arylimino noscapinoids 4-6 have tremendous potential as chemotherapeutic agents for the treatment of breast cancer.

References

SHOWING 1-10 OF 44 REFERENCES
Rational Design, Synthesis, and Biological Evaluation of Third Generation α-Noscapine Analogues as Potent Tubulin Binding Anti-Cancer Agents
TLDR
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.
Rational design, synthesis and biological evaluations of amino-noscapine: a high affinity tubulin-binding noscapinoid
TLDR
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.
Rational Design of Novel Anti-microtubule Agent (9-Azido-Noscapine) from Quantitative Structure Activity Relationship (QSAR) Evaluation of Noscapinoids
TLDR
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.
Rational design of biaryl pharmacophore inserted noscapine derivatives as potent tubulin binding anticancer agents
TLDR
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.
In silico inspired design and synthesis of a novel tubulin-binding anti-cancer drug: folate conjugated noscapine (Targetin)
TLDR
Chemical synthesis, tubulin-binding experiments, and anti-cancer activity in vitro corroborate fully well with the molecular modelling experiments.
Development of a Novel Nitro-Derivative of Noscapine for the Potential Treatment of Drug-Resistant Ovarian Cancer and T-Cell Lymphoma
TLDR
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.
Discovery of 1,3-diyne compounds as novel and potent antidepressant agents: synthesis, cell-based assay and behavioral studies
TLDR
It is shown that compound 7a is a promising lead candidate that deserves further evaluation in the design of antidepressants and was proved to be associated with the regulation of the apoptosis related proteins.
...
...