2. Academic Validation
  3. Synthesis of novel building blocks of benzosuberone bearing coumarin moieties and their evaluation as potential anticancer agents

Synthesis of novel building blocks of benzosuberone bearing coumarin moieties and their evaluation as potential anticancer agents

  • Eur J Med Chem. 2014 May 22:79:260-5. doi: 10.1016/j.ejmech.2014.04.015.
Bandi Yadagiri 1,  Uma Devi Holagunda 1,  Rajashaker Bantu 1,  Lingaiah Nagarapu 2,  C Ganesh Kumar 3,  Sujitha Pombala 3,  B Sridhar 4
Affiliations

Affiliations

  • 1 Organic Chemistry Division II, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 2 Organic Chemistry Division II, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India. Electronic address: lnagarapuiict@yahoo.com.
  • 3 Centre for Medicinal Chemistry & Pharmacology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
  • 4 Centre for X-ray Crystallography, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
PMID: 24742385 DOI: 10.1016/j.ejmech.2014.04.015
Abstract

A series of novel benzosuberone bearing coumarin moieties 5a-c have been synthesized and their structures were determined by analytical and spectral (FT-IR, (1)H NMR, (13)C NMR, HRMS) studies. The newly synthesized compounds were evaluated for their cytotoxicity against four human Cancer cell lines, A549 (Human alveolar adenocarcinoma cell line), HeLa (Human cervical Cancer cell line), MDA-MB-231 (Human breast adenocarcinoma cell line), MCF-7 (Human breast adenocarcinoma cell line) and normal cell line HEK293 (Human embryonic kidney cell line). Compound 5a exhibited promising cytotoxicity with IC50 values ranging from 3.35 to 16.79 μM against all the Cancer cell lines like A549, HeLa, MCF-7 and MDA-MB-231, while compound 5c showed significant cytotoxicity against HeLa and MDA-MB-231 with IC50 values of 6.72 and 4.87, respectively.

Keywords

Benzosuberone; Cell lines; Cytotoxicity; Vilsmeier Haack–Arnold reaction.

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