Rational design of 9-vinyl-phenyl noscapine as potent tubulin binding anticancer agent and evaluation of the effects of its combination on Docetaxel

  title={Rational design of 9-vinyl-phenyl noscapine as potent tubulin binding anticancer agent and evaluation of the effects of its combination on Docetaxel},
  author={Shruti Gamya Dash and Charu Suri and P.K. Nagireddy and Srinivas Kantevari and Pradeep Kumar Naik},
  journal={Journal of Biomolecular Structure and Dynamics},
  pages={5276 - 5289}
  • S. Dash, C. Suri, P. K. Naik
  • Published 1 July 2020
  • Chemistry, Biology
  • Journal of Biomolecular Structure and Dynamics
Abstract Docetaxel (DOX) based combination therapy is a novel therapeutic strategy that attracts great interest in breast cancer treatment but its clinical utility got limited due to side effects. In contrast, noscapine, an antitussive drug showed antitumor activity against many cancers without any side effects that targets microtubules and attenuates its dynamic instability. In the quest for an increase in the anticancer activity of noscapine, we strategically designed a novel derivative, 9… 
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Rational design of novel N‐alkyl amine analogues of noscapine, their chemical synthesis and cellular activity as potent anticancer agents
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Synergistic interaction of N‐3‐Br‐benzyl‐noscapine and docetaxel abrogates oncogenic potential of breast cancer cells
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Noscapine, an Emerging Medication for Different Diseases: A Mechanistic Review
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Rational Design, Synthesis, and Biological Evaluation of Third Generation α-Noscapine Analogues as Potent Tubulin Binding Anti-Cancer Agents
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)
Chemical synthesis, tubulin-binding experiments, and anti-cancer activity in vitro corroborate fully well with the molecular modelling experiments.
Rational design of biaryl pharmacophore inserted noscapine derivatives as potent tubulin binding anticancer agents
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.
Rational Design of Novel Anti-microtubule Agent (9-Azido-Noscapine) from Quantitative Structure Activity Relationship (QSAR) Evaluation of Noscapinoids
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, synthesis and biological evaluations of amino-noscapine: a high affinity tubulin-binding noscapinoid
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.
Enhancement of antitumor activity of docetaxel by celecoxib in lung tumors
The combination of cele Coxib with docetaxel produces a greater antitumor effect in s.c. A549 tumors as compared to celecoxib or docetAXel alone and this effect is associated with concomitant alterations in the intratumor levels of PGE2 and 15‐d PGJ2.
Synthesis and biological evaluation of novel biaryl type α-noscapine congeners.
The proteasome inhibitor bortezomib enhances the activity of docetaxel in orthotopic human pancreatic tumor zenografts
It is suggested that bortezomib enhances the antitumoral activity of taxanes by enforcing cell growth arrest and inhibiting angiogenesis.
The sesquiterpene lactone parthenolide in combination with docetaxel reduces metastasis and improves survival in a xenograft model of breast cancer
Results for the first time reveal the significant in vivo chemosensitizing properties of parthenolide in the metastatic breast cancer setting and support the contention that metastases are very reliant on activation of NF-κB.