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US8609858: Spiro derivatives of parthenin as novel anticancer agents

The invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (?-methylene-?-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 µM to 93 µM. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the ?, ?-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.
Patent No:
US8609858
Application No:
12/921061
Filing Date:
29-04-2011
Issue Date:
17-12-2013
Applicant:
CSIR-Indian Institute of Integrative Medicine (CSIR-IIIM), Jammu
Inventor(s):
Halmuthur Mahabalarao Sampath Kumar; Saxena Ajit Kumar; Taneja Subhash Chandra; Singh Shashank Kumar; Sethi Vijay Kumar; Qazi Naveed Ahmed; Sawant Sanghapal Damodar; Doma Mahender Reddy; Banday Abid Hussain; Verma Monika; Qazi Ghulam Nabi
IPC Classification:
C07D 498/10, C07D 491/107
Country:
United States of America
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