Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents

Samir Mehndiratta, Yi-Fang Chiang, Mei-Jung Lai, Hsueh Yun Lee, Mei Chuan Chen, Ching-Chuan Kuo, Chi-Yen Chang, Jang-Yang Chang, Jing Ping Liou

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)


Described herein is the development of a novel series of 7-anilino-indoline-N-benzenesulfonamides, derived from ABT751 (1), as potent anticancer agents. Amongst the synthesized series, compounds 6, 12, 13, and 14 have shown comparable to better anticancer activity on comparing with compound 1. 7-(4-Cyanophenylamino)-1-(4-methoxybenzenesulfonyl)indoline (13) was found to be the most potent one with up to 6 fold better activity against KB, HT29, and MKN45 cancer cell lines with IC50 values of 49.7, 149, and 92 nM, respectively. Compound 13 was also found inhibiting multidrug resistant cancer cell lines, blocking cell cycle at G2/M phase, and inhibiting tubulin polymerization. Capillary disruption assay results revealed that compound 13 was able to disrupt formed capillaries in a concentration-dependent manner without affecting cell viability.

Original languageEnglish
Pages (from-to)4917-4923
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number17
Publication statusPublished - Sept 1 2014


  • ABT751
  • Antimitotic
  • CA-4
  • Vascular-disrupting agents

ASJC Scopus subject areas

  • Biochemistry
  • Clinical Biochemistry
  • Molecular Biology
  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Medicine(all)


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