2. Academic Validation
  3. Synthesis and evaluation of 3-salicyloylpyridine derivatives as cytotoxic mitochondrial apoptosis inducers

Synthesis and evaluation of 3-salicyloylpyridine derivatives as cytotoxic mitochondrial apoptosis inducers

  • Bioorg Med Chem Lett. 2014 Oct 1;24(19):4724-4728. doi: 10.1016/j.bmcl.2014.08.010.
Alisha Sood 1,  Vishal Sharma 1,  Ashun Chaudhry 2,  Rakesh Kumar 2,  Saroj Arora 2,  Rajnikant 3,  Vivek Gupta 3,  Mohan Paul S Ishar 4
Affiliations

Affiliations

  • 1 Bio-Organic and Photochemistry Laboratory, Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
  • 2 Department of Botanical and Environmental Sciences, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
  • 3 Post-Graduate Department of Physics, University of Jammu, Jammu Tawi, 180 006, India.
  • 4 Bio-Organic and Photochemistry Laboratory, Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143005, Punjab, India. Electronic address: mpsishar@yahoo.com.
PMID: 25176329 DOI: 10.1016/j.bmcl.2014.08.010
Abstract

A series of novel 3-salicyloylpyridines (4a-h) were synthesized with good yield by modified Knoevenagel-Stobbel method; o-allylation with allyl bromide lead to formation of compounds (5a-h). The synthesized compounds were characterized by spectroscopic techniques and evaluated for cytotoxic activity against human Cancer cell lines. Compounds bearing hydroxyl group displayed high cytotoxicity (4a-h) as compared to o-allylated molecules (5a-h). The most active compound 4b was selected for further investigation to look for mechanism of cell death in prostate Cancer (PC-3) cells. The apoptotic bodies induced by 4b in PC-3 cells were scanned by confocal microscopy and confirmed by scanning electron microscopy (SEM). Further results obtained from spectrofluorimetric determination of mitochondrial membrane potential (ΔΨm) and intracellular Reactive Oxygen Species (ROS) in treated PC-3 cells revealed that mitochondria dependent Apoptosis was involved in the cell death.

Keywords

3-Formylchromone; 3-Salicyloylpyridines; Apoptosis; Cytotoxic activity.

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