Synthesis and exploration of novel curcumin analogues as anti-malarial agents

Bioorganic & Medicinal Chemistry
Satyendra MishraAvadhesha Surolia

Abstract

Curcumin, a major yellow pigment and active component of turmeric, has been shown to possess anti-inflammatory and anti-cancer activities. Recent studies have indicated that curcumin inhibits chloroquine-sensitive (CQ-S) and chloroquine-resistant (CQ-R) Plasmodium falciparum growth in culture with an IC(50) of approximately 3.25 microM (MIC=13.2 microM) and IC(50) 4.21 microM (MIC=14.4 microM), respectively. In order to expand their potential as anti-malarials a series of novel curcumin derivatives were synthesized and evaluated for their ability to inhibit P. falciparum growth in culture. Several curcumin analogues examined show more effective inhibition of P. falciparum growth than curcumin. The most potent curcumin compounds 3, 6, and 11 were inhibitory for CQ-S P. falciparum at IC(50) of 0.48, 0.87, 0.92 microM and CQ-R P. falciparum at IC(50) of 0.45 microM, 0.89, 0.75 microM, respectively. Pyrazole analogue of curcumin (3) exhibited sevenfold higher anti-malarial potency against CQ-S and ninefold higher anti-malarial potency against CQ-R. Curcumin analogues described here represent a novel class of highly selective P. falciparum inhibitors and promising candidates for the design of novel anti-malarial agents.

Citations

Aug 13, 2011·Journal of Medicinal Chemistry·Soumyananda ChakrabortiBhabatarak Bhattacharyya
Aug 2, 2014·European Journal of Medicinal Chemistry·Ajay KumarDhirender Kaushik
Sep 29, 2011·Expert Opinion on Biological Therapy·Sandhya A MaratheDipshikha Chakravortty
Sep 14, 2012·Expert Opinion on Drug Delivery·Chandana MohantySanjeeb K Sahoo
Dec 5, 2009·European Journal of Pharmacology·Chau Ling ThamDaud A Israf
Dec 26, 2015·Bioorganic & Medicinal Chemistry·Diego CaprioglioAlberto Minassi
Sep 9, 2008·Biochemical Pharmacology·Preetha AnandBharat B Aggarwal
Dec 23, 2009·Medicinal Research Reviews·Dinesh Kumar Agrawal, Pushpesh Kumar Mishra
May 6, 2014·Biotechnology Advances·Sahdeo PrasadBharat B Aggarwal
Jan 22, 2014·Natural Product Research·Ranjith MuniguntiAngela I Calderón
May 19, 2016·European Journal of Medicinal Chemistry·Mohemmed Faraz KhanMohammad Shaquiquzzaman
Apr 20, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·María Concepción Lozada-GarcíaJaime Pérez-Villanueva
Jan 24, 2017·Bioorganic & Medicinal Chemistry Letters·Dnyaneshwar D SubhedarBapurao B Shingate
Feb 12, 2017·Experimental Parasitology·Chandrajit DohutiaKishore Sarma
Jul 1, 2017·Journal of Asian Natural Products Research·Srinu MeesalaMilind G Watve
Dec 31, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Dinesh ShettyJames P Snyder
Jan 13, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Khalid KarrouchiM'hammed Ansar
Nov 22, 2018·Chemistry & Biodiversity·Satyendra MishraChandni G Halpani
Apr 8, 2020·Phytotherapy Research : PTR·Ting XuYumeng Wei
Aug 23, 2008·Journal of Enzyme Inhibition and Medicinal Chemistry·Yasser BustanjiHatim S Alkhatib
Nov 12, 2015·Archiv der Pharmazie·Daisy R Sherin, Kallikat N Rajasekharan
May 26, 2016·Asian Pacific Journal of Cancer Prevention : APJCP·Mohamed Jawed Ahsan, Mohamed Jawed Ahsan
Jul 2, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Birgit ViiraElisabeth Davioud-Charvet
May 8, 2018·International Journal of Molecular Sciences·Elisabet Martí Coma-CrosXavier Fernàndez-Busquets
Jul 25, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Carolina Escobedo-MartínezRaúl G Enríquez
Feb 22, 2011·Organic & Biomolecular Chemistry·Wenjun LiJinxing Ye
Dec 17, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Pedro M O GomesVera L M Silva
Feb 16, 2021·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Fiona C RodriguesGoutam Thakur
Feb 8, 2020·Journal of Medicinal Chemistry·Lucie PeterkováSilvie Rimpelová
Sep 26, 2013·Biochemistry·Soumyananda ChakrabortiBhabatarak Bhattacharyya
Apr 16, 2011·Bioorganic & Medicinal Chemistry Letters·Rahul Balasaheb AherVirander Singh Chauhan

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antimalarial Agents (ASM)

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.

Antimalarial Agents

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.