Bicycle Topoisomerase I Inhibiting Compounds, Process for Preparation and Use Thereof

1. The compounds show potent inhibitory activity on Human Topoisomerase 1 and also show cytotoxicity in Breast Cancer cells and therefore may act as novel anticancer therapeutics.
2. The compounds act as anticancer agent by inhibition Topoisomerase 1 enzyme like the camptothecin.
3. The compounds are stable drug candidates which possess the ability to increase the stability of the drug-DNA-TopI ternary complex that eventually results in cancer cell death to achieve clinical anticancer activity.
4. The compounds are non-camptothecin inhibitors will help to develop more effective chemotherapeutics for this deadliest disease.
5. Compounds or in acceptable salt can be useful to treat any of a variety of conditions where inhibition of topoisomerase I enzyme is important.
6. The plasma stability of the compounds shows that they are highly stable at pH 7.4 in plasma.
7. The aqueous solubility of the compounds shows good solubility at pH 7.4.

The invention relates to compounds in free form or in acceptable salt form as topoisomerase I inhibitors.

The invention relates to small molecules which together possess the ability to increase the stability of the drug-DNA-Topoisomerase I ternary complex that eventually results in cancer cell death to achieve clinical anticancer activity.

1. The compounds are stable drug candidates which possess the ability to increase the stability of the drug-DNA-TopI ternary complex that eventually results in cancer cell death to achieve clinical anticancer activity.