Steering the antitumor drug discovery campaign towards structurally diverse indolines

Amandeep Thakur, Arshdeep Singh, Navdeep Kaur, Ritu Ojha, Kunal Nepali

Research output: Contribution to journalReview articlepeer-review

39 Citations (Scopus)

Abstract

Indoline framework is often perpended as a privileged heterocycle present in medicinally valuable compounds of natural and synthetic origin. This review article presents the rational approaches/strategies employed for the design of anticancer indolines along with the structure activity relationship and mechanistic insights revealed in the in-vitro and in-vivo assays. The chemist has always been fascinated towards the indoline ring for the construction of antitumor scaffolds owing to its versatility as evidenced by its existence in scaffolds inducing antiproliferative effects via diverse mechanisms. To the delight of medicinal chemist, the applicability of indoline has also been expanded towards the design of dual inhibitors (multitargeting anticancer agents) as well as PROTACS. Overall, it can be concluded that indoline moiety is a magic bullet and the scaffolds containing this ring are foraying towards detailed preclinical and clinical stage investigations by leaps and bounds.

Original languageEnglish
Article number103436
JournalBioorganic Chemistry
Volume94
DOIs
Publication statusPublished - Jan 2020

Keywords

  • Alkaloids
  • Cancer
  • Cells
  • Dearomatization
  • Heterocycles
  • Indolines
  • Tumor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Drug Discovery
  • Organic Chemistry

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