Many nitrogen-moiety containing alkaloids derived from plant origins are bioactive and play a significant role in human health and emerging medicine. Noscapine, a phthalideisoquinoline alkaloid derived from Papaver somniferum, has been used as a cough suppressant since the mid 1950s, illustrating a good safety profile. Noscapine has since been discovered to arrest cells at mitosis, albeit with moderately weak activity. Immunofluorescence staining of microtubules after 24 h of noscapine exposure at 20 μM elucidated chromosomal abnormalities and the inability of chromosomes to complete congression to the equatorial plane for proper mitotic separation ( Proc. Natl. Acad. Sci. U. S. A. 1998 , 95 , 1601 - 1606 ). A number of noscapine analogues possessing various modifications have been described within the literature and have shown significantly improved antiprolific profiles for a large variety of cancer cell lines. Several semisynthetic antimitotic alkaloids are emerging as possible candidates as novel anticancer therapies. This perspective discusses the advancing understanding of noscapine and related analogues in the fight against malignant disease.
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http://dx.doi.org/10.1021/jm501180v | DOI Listing |
J Med Chem
January 2025
Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China.
The search for new and effective chemotherapeutic agents for the treatment of glioblastoma (GBM) represents an unmet need in drug discovery. Herein, a class of novel -trifluoromethylated noscapines has been disclosed. Among them, 9'-bromo--trifluoromethyl noscapine displayed superior anti-GBM potency.
View Article and Find Full Text PDFEur J Med Chem
January 2025
Centre of Excellence in Natural Products and Therapeutics, Department of Biotechnology and Bioinformatics, Sambalpur University, Jyoti Vihar, Burla, Sambalpur, 768019, Odisha, India. Electronic address:
A series of semisynthetic noscapine-urea congeners (7a-7h) as potential tubulin-binding agents are being developed by integrating a urea pharmacophore at the C-9 position of the noscapine scaffold. Their binding affinity to tubulin was predicted through molecular docking, molecular dynamics (MD) simulations, and the MM-PBSA approach. These molecules were subsequently chemically synthesized and assessed using breast cancer cell lines (MCF-7 and MDA-MB-231) and normal human embryonic kidney cells (HEK).
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid Beheshti University, Evin, 1983963113 Tehran, Iran. Electronic address:
Noscapine, a tetrahydroisoquinoline alkaloid, was first isolated from Papaver somniferum and identified by Rabiquet in 1817. It has been used as an anti-tussive agent since the mid-1950 s. After the discovery of its anti-mitotic potential, it was into the limelight once again.
View Article and Find Full Text PDFInt J Biol Macromol
August 2023
Department of Chemistry, University of Delhi, Delhi 110007, India; Dr. B. R. Ambedkar Center for Biomedical Research, University of Delhi, Delhi 110007, India; Institute of Nano Medical Sciences, University of Delhi, Delhi 110007, India; Maharaja Surajmal Brij University, Rajasthan - 321201, India. Electronic address:
Noscapine is a proficient anticancer drug active against wide variety of tumors including lung cancer. Over time, several noscapine analogues have been assessed to maximize the efficiency of the drug, amongst which 9-bromo noscapine remains one of the most potent analogues till date. In the present work, we have synthesized 9-bromo noscapine ionic liquid [9-Br-Nos]IBr, an active pharmaceutical ingredient based ionic liquid (API-IL) to address the existing issues of solubility and targeted drug delivery in the parent alkaloid as well as the synthesized analogues.
View Article and Find Full Text PDFFront Pharmacol
February 2023
Department of Clinical Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Alborz, Iran.
As February 2023, SARS-CoV-2 is still infecting people and children worldwide. Cough and dyspnea are annoying symptoms almost present in a large proportion of COVID-19 outpatients, and the duration of these symptoms might be long enough to affect the patients' quality of life. Studies have shown positive effects for noscapine plus licorice in the previous COVID-19 trials.
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