Topoisomerase I and II inhibitors: A patent review

Arshdeep Singh, Navdeep Kaur, Gurpreet Singh, Pooja Sharma, P. M.S. Bedi, Sahil Sharma, Kunal Nepali

研究成果: 雜誌貢獻回顧型文獻同行評審

12 引文 斯高帕斯(Scopus)


Background: Topoisomerases are a set of nuclear enzymes that play a vital role in handling of topological consequences of DNA during various genetic activities necessary for vitality of cell. Inhibition of these enzymes consequently leads to the blockage of ligation step of the cell cycle which generates single and double strand breakage in DNA strand. Introduction of these breaks subsequently leads to programmed cell death (Apoptosis). Objective: In the past several years, topoisomerases have become one of the most expedient and strategic molecular targets for anticancer drugs and numerous patents have been filed and published on topoisomerase inhibitors. This review compiles the patent literature up to 2016 embracing topo I and II inhibitors as well as dual inhibitors which are structurally adjacent to camptothecin (CPT), natural products such as lamellarins and synthetic trisubstituted pyridines. The present assemblage can be extremely advantageous for the medicinal chemists who are in crave for the development of potential anticancer agents targeting topoisomerases. Conclusion: Recent patents indicated that some of the nitrogen containing heteroaromatic compounds have immense potential to inhibit topoisomerase enzyme. In particular, fused N-Heterocycles can be anticipated for their promising therapeutic potential alone or in combination with other anticancer agents. Naphthyridinone and indenoisoquinoline derivatives, described in the preceding sections of this review, are endowed with significant potency against topoisomerase I which clearly indicates the need of preclinical and clinical studies to place them in forefront as potential future drug candidates.
頁(從 - 到)401-423
期刊Recent Patents on Anti-Cancer Drug Discovery
出版狀態已發佈 - 11月 1 2016

ASJC Scopus subject areas

  • 腫瘤科
  • 藥物發現
  • 癌症研究
  • 藥學(醫學)


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