Spiro Derivatives of Parthenin as Novel Anticancer Agents

The present 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 (...

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Hauptverfasser:	SAWANT SANGHAPAL DAMODHAR, QAZI NAVEED AHMED, DOMA MAHENDHAR REDDY, HALMUTHUR MAHABALARAO SAMPATH KUMAR, SINGH SHASHANK KUMAR, BANDAY ABID HUSSAIN, QAZI GHULARN NABI, SETHI VIJAY KUMAR, TANEJA SUBHASH CHANDRA, SAXENA AJIT KUMAR, VERMA MONIKA
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	The present 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 (α-methylene-γ-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 α, -unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.