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.

Advantages:
-TOP1 is a proven target for cancer therapy
-Azaindenoisoquinolines have enhanced chemical stability and effectiveness over other TOP1 inhibitors
Mar 6, 2014
CIP-Patent
United States
9,034,870
May 19, 2015

Jul 13, 2012
Utility Patent
United States
8,686,146
Apr 1, 2014

(None)
Provisional-Patent
United States
(None)
(None)
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