4.3 Article

2,4-Diarylpyrano[3,2-c]chromen-5(4H)-ones as Antiproliferative Agents: Design, Synthesis and Biological Evaluation

Journal

CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 64, Issue 5, Pages 399-409

Publisher

PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c15-00958

Keywords

hybrid; cancer; pyran; apoptosis; cytotoxicity

Funding

  1. UGC, New Delhi under UPE (Focus Area-Health Care, Drug Development and Sports Medicines) Scheme [25994/Estt./A-11]
  2. UPE (University with potential for excellence)

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In the present study, a series of 2,4-diarylpyrano[3,2-c]chromen-5(4H)-ones were synthesised and evaluated as antiproliferative agents. The compounds were evaluated against a panel of human cancer cell lines. CH-1 exhibited significant cytoxicity against HCT 116 cell lines with an IC50 value of 1.4 and 4.3 mu m against MiaPaCa-2 cell lines. The compound CH-1 was found to induce apoptosis as evidenced by phase contrast microscopy, Hoechst 33258 staining and mitochondrial membrane potential (MMP) loss. The cell phase distribution studies indicated that the apoptotic population increased from 10.22% in the control sample to 57.19% in a sample treated with 20 mu m compound CH-1.

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