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Synthetic rigidin analogues as anticancer agents, salts, solvates and prodrugs thereof, and method of producing same
Patent Number: US9334280

Executive Summary:
  • Invention Type: Therapeutic
  • Patent Status: Granted
  • Patent Link: https://patents.google.com/patent/US9334280/
  • Research Institute: New Mexico Tech 
  • Disease Focus: Glioblastoma and melanoma
  • Basis of Invention: Synthetic rigid analogues (Rigidins) as anticancer agents, salts, solvates and prodrugs, and method to produce these agents
  • How it works: Cell death, cell cycle arrest in G1, targeting of actin or tubulin as well as histone deacetylase (HDAC) inhibition proposed
  • Lead Challenge Inventor: Snezna Rogelj, Liliya V Frolova
  • Inventors: Igor V. Magedov, Snezna Rogelj, Liliya V Frolova, Alexander Vladimir Kornienko
  • Development Stage: In vitro data in HeLa and MCF-7 cell line
  • Novelty:
    • The Rigidins incorporate the pyrrolo[2,3-d]pyrimidine ring system, which is considered a “privileged medicinal scaffold” (PMS). PMSs are molecular frameworks that are seemingly capable of serving as ligands for a diverse array of targets
  • Clinical Applications:
    • Treatment of Glioblastoma and melanoma
    • Treatment of cervical, brain, breast, lung, head and neck and colon cancer 

General Description:
The present invention describes novel hypoxanthine-like analogues of marine alkaloids rigidins. The rigidins incorporate the pyrrolo[2,3-d]pyrimidine ring system, which is considered a “privileged medicinal scaffold” (PMS). PMSs are molecular frameworks that are seemingly capable of serving as ligands for a diverse array of targets. The pyrrolo[2,3-d]pyrimidine ring system is analogous to the purine framework and, in addition to the rigidins, it is also a common motif in several other natural products, such as the nucleoside anticancer antibiotics tubercidin, toyocamycin, sangivamycin. Thus, the rigidins are an unexplored class of marine alkaloids that have a high potential for multiple biological activities.

Evaluation of these synthetically prepared alkaloids against several cancer cell lines revealed very weak antiproliferative activities (>100 micromolar IC50 values). The current discovery deals with the finding that an alteration of this reported synthetic methodology to a novel four-component reaction leads to the preparation of rigidin analogues possessing a previously unknown hypoxanthine-like skeleton. Further evaluation of these compounds against several cancer cell lines revealed a marked and unexpected potent antiproliferative effect at extremely low concentrations.

Scientific Progress:
The synthesized compounds of Formula I were evaluated for antiproliferative activity against a panel of cancer cell lines, including human HeLa cervical and MCF-7 breast adenocarcinomas. Many of the analogues exhibited nanomolar potency, characteristic of the clinically used anticancer agents.

Future Directions:
  • Pre-clinical studies on the potency and efficacy of cancer treatment using rigidins

Strengths:
  • Natural product derivatives which targets molecular mechanism of cell death and cell cycle

Patent Status:
  • Priority date: 2012-11-16
  • Filing date: 2015-04-23
  • Publication date: 2016-05-10
  • Grant date: 2016-05-10

Publications:
https://patents.google.com/patent/US7407967B2/
 
https://patents.google.com/patent/US6403636B1/
 
Inventor Bios: Snezna Rogelj, Liliya Frolova

http://infohost.nmt.edu/~biology/people/faculty/s_rogeljWork/research.html

http://infohost.nmt.edu/~chem/frolova.html
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