4β-amino podophyllotoxin congeners as potential...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C548S117000

Reexamination Certificate

active

07960418

ABSTRACT:
The present invention provides new class of 4β-[4″-(1″,3″-benzothiazole-2″-yl)anilino]podophyllotoxin analogues having the structural formula as follows (4).Where R═H or CH3; R1═H, halogen, CH3and R2═H, halogen, OCH3.The present invention also provides a process for the preparation of new 4β-[4″-(1″, 3″-benzothiazole-2″-yl)anilino]podophyllotoxin analogues as useful anticancer agents. More particularly, it provides a process for the preparation of 4β-[4″-(1″,3″-benzothiazole-2″-yl)anilino] derivatives of podophyllotoxin. The process for the synthesis of new podophyllotoxin analogues as anticancer agents produces the novel and stereo-selective derivatives of the podophyllotoxin in good yields, where in the key step for the synthesis of these analogues is by direct nucleophilic substitution of C-4β-iodo intermediates. The 4β-iodopodophyllotoxin, which has been reacted with substituted or unsubstituted 4-(1,3-benzothiazole-2-yl)aniline in a stereo-selective manner to afford the 4β-[4″-(1″,3″-benzothiazole-2″-yl)anilino] derivatives of podophyllotoxin.

REFERENCES:
Fischer et al., Cancer Treatment Reviews 2007, 33, 391-406.
Sarconoma, http://en.wikipedia.org/wiki/HT1080, 2010.
Non-smallCell, http://dtp.nci.nih.ogv/docs/misc/common—files/cell—list.html (2010).

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