1256152-90-5Relevant academic research and scientific papers
Chalcones as promising pesticidal agents against diamondback moth (Plutella xylostella): Microwave-assisted synthesis and structure-activity relationship
Kumar, Rakesh,Sharma, Prabha,Shard, Amit,Tewary, Dhananjay Kumar,Nadda, Gireesh,Sinha, Arun Kumar
, p. 922 - 931 (2012/08/14)
A series of chalcones (A-CH=CH-CO-B) were synthesized under microwave irradiation, and for the first time their pesticidal activity against diamondback moth (Plutella xylostella) was evaluated to identify the promising lead structures. The structure-activity relationship (SAR) analysis revealed that electron-withdrawing substituents on ring A of chalcone provided good pesticidal agents, whereas, ring B can bear either electron-withdrawing or electron-releasing substituents. Moreover, compound 22 having para-Cl substitution on ring A as well on ring B showed maximum activity with LC 50 value of 170.24 μg mL-1. Springer Science+Business Media, LLC 2011.
Reinvestigation of structure-activity relationship of methoxylated chalcones as antimalarials: Synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural β-asarone
Kumar, Rakesh,Mohanakrishnan, Dinesh,Sharma, Abhishek,Kaushik, Naveen Kumar,Kalia, Kalpana,Sinha, Arun Kumar,Sahal, Dinkar
experimental part, p. 5292 - 5301 (2011/02/23)
We have examined the antimalarial structure-activity relationship of a series of methoxylated chalcones (A-CHCH-CO-B) against Plasmodium falciparum (3D7 strain) using fluorescence-based SYBR Green assay. Our study has revealed that electron releasing methoxy groups on ring A and electron withdrawing groups on ring B increases antimalarial potency while the positional interchange of these groups causes a decrease. In particular, 2,4,5-trimethoxy substitution pattern at ring A provided potent analogues which were easily derived from abundantly available natural β-asarone rich Acorus calamus oil. Cytotoxic evaluation indicated that the most active compounds 27 (IC50: 1.8 μM) and 26 (IC50: 2 μM) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum.
