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Stilbene−Chalcone Hybrids: Design, Synthesis, and Evaluation as a New Class of Antimalarial Scaffolds That Trigger Cell Death through Stage Specific Apoptosis

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Title Stilbene−Chalcone Hybrids: Design, Synthesis, and Evaluation as a
New Class of Antimalarial Scaffolds That Trigger Cell Death through
Stage Specific Apoptosis
 
Creator Sharma, N
Mohanakrishan, Dinesh
Shard, A
Sharma , A
---, Saima
Sinha, Arun K
Sahal, D
 
Subject Plant sciences
Natural Product Chemistry
 
Description Novel stilbene−chalcone (S-C) hybrids were
synthesized via a sequential Claisen−Schmidt−Knoevenagel−
Heck approach and evaluated for antiplasmodial activity in in
vitro red cell culture using SYBR Green I assay. The most
potent hybrid (11) showed IC50 of 2.2, 1.4, and 6.4 μM against
3D7 (chloroquine sensitive), Indo, and Dd2 (chloroquine
resistant) strains of Plasmodium falciparum, respectively.
Interestingly, the respective individual stilbene (IC50 > 100
μM), chalcone (IC50 = 11.5 μM), or an equimolar mixture of
stilbene and chalcone (IC50 = 32.5 μM) were less potent than
11. Studies done using specific stage enriched cultures and
parasite in continuous culture indicate that 11 and 18 spare the schizont but block the progression of the parasite life cycle at the
ring or the trophozoite stages. Further, 11 and 18 caused chromatin condensation, DNA fragmentation, and loss of
mitochondrial membrane potential in Plasmodium falciparum, thereby suggesting their ability to cause apoptosis in malaria
parasite.
 
Date 2012
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://ihbt.csircentral.net/1052/1/63_Stilbene-Chalcone_2012.pdf
Sharma, N and Mohanakrishan, Dinesh and Shard, A and Sharma , A and ---, Saima and Sinha, Arun K and Sahal, D (2012) Stilbene−Chalcone Hybrids: Design, Synthesis, and Evaluation as a New Class of Antimalarial Scaffolds That Trigger Cell Death through Stage Specific Apoptosis. Journal of Medicinal Chemistry, 55. pp. 297-311.
 
Relation http://ihbt.csircentral.net/1052/