Structure-Activity Relationships of Azaindenoisoquinolines

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Topoisomerase 1 (TOP1) is an important protein found in the cell; it is used to unwind and reduce torsional stress on DNA during replication. TOP1 inhibitors are a useful chemotherapy agent because cells that are constantly dividing, such as cancer cells, are much more susceptible to attack; cell death will occur when topoisomerase 1 is inhibited. TOP1 inhibitors make up a large portion of the chemotherapy market because they can be used to target a wide variety of proliferating tumors. The characteristic of uninhibited division is a common feature in cancer that can be targeted without needing a specific marker for each cancer cell type. As more information becomes readily available, it is becoming apparent that within tumors there is a heterogeneous population of cells populating the primary tumor and the secondary tumors.

Purdue University researchers have developed a novel process for synthesizing four TOP1 inhibitors and have optimized their structures for the greatest inhibitory activity and cytoxicity towards dividing cells. The compounds consist of 7-, 8-, 9-, and 10-azaindenoisoquinoline structures.

-TOP1 is a proven target for cancer therapy
-Azaindenoisoquinolines have enhanced chemical stability and effectiveness over other TOP1 inhibitors
Mar 6, 2014
United States
May 19, 2015

Jul 13, 2012
Utility Patent
United States
Apr 1, 2014

United States
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