Cited by 145Heterocyclic Compound Synthesis and BioactivityFree Radicals and AntioxidantsSynthesis of Organic Compounds

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Synthesis, antioxidant evaluation, and quantitative structure–activity relationship studies of chalcones

Sivakumar, P. M., Prabhakar, P. K., Doble, M.·2011·Medicinal Chemistry Research

DOI 10.1007/s00044-010-9342-1

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Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of Some N-Substituted-4-Phenothiazine-Chalcones
Tran, T., Le, M.-T., Nguyen, T.-C.-V., Tran, T., Tran, T., & Thai, K. (2020) · Molecules · doi:10.3390/molecules25173916 · Cited by 17
“For the last few years, chalcones, belonging to flavonoid derivatives, have attracted great interest due to their diverse bioactivities, encompassing antimalarial [13,14], antimicrobial [15–27], antioxidant [28], antitumor [29–31], anti-inflammatory [32–34], analgesic [34–36], to antiulcer [37,38].”
In silico modeling and synthesis of phenyl and thienyl analogs of chalcones for potential leads as anti-bacterial agents
Kar, S., Mishra, R. K., Pathak, A. K., Dikshit, A., & Golakoti, N. R. (2017) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2017.12.002 · Cited by 17
N‐methylpiperazinyl and piperdinylalkyl‐ O‐chalcone derivatives as potential polyfunctional agents against Alzheimer's disease: Design, synthesis and biological evaluation
Sharma, P., Singh, V., & Singh, M. (2023) · Chemical Biology & Drug Design · doi:10.1111/cbdd.14318 · Cited by 16
“…biological effects including anti-inflammatory (Batovska & Todorova, 2010; Singh, Sharma, Joshi, et al., 2020; Singh, Sharma, Singh, et al., 2020; Sivakumar et al., 2011), anticancer (Go et al., 2005; Karthikeyan et al., 2015; Lee et al., 2012; Orlikova et al., 2011; Romagnoli et al., 2008;…”
Background
A novel class of tyrosine derivatives as dual 5-LOX and COX-2/mPGES1 inhibitors with PGE 2 mediated anticancer properties
Puratchikody, A., Umamaheswari, A., Navabshan, I., Sinha, S., Manju, S. L., Ramanan, M., Ramamoorthy, G., & Doble, M. (2018) · New Journal of Chemistry · doi:10.1039/c8nj04385j · Cited by 16
Self-citation
Synthesis of diarylidenecyclohexanone derivatives as potential anti-inflammatory leads against COX-2/mPGES1 and 5-LOX
Kar, S., Ramamoorthy, G., Sinha, S., Ramanan, M., Pola, J. K., Golakoti, N. R., Nanubolu, J. B., Sahoo, S. K., Dandamudi, R. B., & Doble, M. (2019) · New Journal of Chemistry · doi:10.1039/c9nj00726a · Cited by 16
Self-citation
3′-Geranyl-mono-substituted chalcone Xanthoangelovl induces apoptosis in human leukemia K562 cells via activation of mitochondrial pathway
Teng, Y., Wang, L., Liu, H., Yuan, Y., Zhang, Q., Wu, M., Wang, L., Wang, H., Liu, Z., & Yu, P. (2016) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2016.11.025 · Cited by 15
Improved drug loading via spray drying of a chalcone implant for local treatment of cutaneous leishmaniasis
Sousa-Batista, A. J., Arruda-Costa, N., Rossi‐Bergmann, B., & Ré, M. I. (2018) · Drug Development and Industrial Pharmacy · doi:10.1080/03639045.2018.1461903 · Cited by 15
“However, no NO production was induced (Figure 6) and was also seen to be compatible with the antioxidant [41] and anti-inflammatory properties of chalcones, even with a decrease in NO production [42,43].”
Background
One-pot diastreoselective synthesis of highly functionalized cyclohexenones: 2-oxo-N,4,6-triarylcyclohex-3-enecarboxamides
Mousavi, M. R., Maghsoodlou, M. T., & Habibi‐Khorassani, S. M. (2014) · Molecular Diversity · doi:10.1007/s11030-014-9541-7 · Cited by 15
“com ing anti-bacterial [4,8,9], anticonvulsant [10], anti-cancer [11], anti-fungal [12,13], antiprotozoal [14], antimalarial [1,2,15], larvicidal [16], antifilarial [17], anti-inflammatory [18], antioxidant [19,20], and antimicrobial [21].”
Background
Single-dose treatment for cutaneous leishmaniasis with an easily synthesized chalcone entrapped in polymeric microparticles
Sousa-Batista, A. J., Arruda-Costa, N., Escrivani, D. O., Reynaud, F., Steel, P. G., & Rossi‐Bergmann, B. (2020) · Parasitology · doi:10.1017/s0031182020000712 · Cited by 14
Mechanochemical synthesis and characterizations of chalcone derivatives: (2E)-3-[4-(Benzyloxy)phenyl]-1-(thiophen-2-yl)prop ‑2-en-1-one and (2E)-3-(Anthracen-9-yl)-1- (thiophen-2-yl)prop‑2-en-1-one
Praveena, P., Sarojini, B. K., & Kumar, S. M. (2019) · Chemical Data Collections · doi:10.1016/j.cdc.2019.100298 · Cited by 13
Ferrocenyl chalcone derivative (E)-3-(2-methylpyrimidin-5-yl)-1-ferroceynlprop-2-en-1-one: Synthesis, Structural analysis, Docking study and their Antibacterial evaluation
Twinkle, A. R., Leenaraj, D. R., Ratković, Z., Arunsasi, B. S., Bright, K. C., & Reshma, R. (2020) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2020.128049 · Cited by 13
Sensitive fluorescent chemosensor for Hg(II) in aqueous solution using 4’-dimethylaminochalcone
Mellado, M., Roldán, N., Miranda, R., Aguilar, L. F., Bravo, M. A., & Waldo Quiroz, V. (2022) · Journal of Fluorescence · doi:10.1007/s10895-022-02941-2 · Cited by 12
Recent Development of Novel Aminoethyl-Substituted Chalcones as Potential Drug Candidates for the Treatment of Alzheimer’s Disease
Sharma, P., Singh, M., Singh, V., Singh, T. G., Singh, T., & Ahmad, S. F. (2023) · Molecules · doi:10.3390/molecules28186579 · Cited by 12
“The bioisosteric replacement of chalcone was performed by manual design as well as with a web server (MolOpt) to generate corresponding analogs with their pharmacokinetics and pharmacodynamics.”
Method
Synthesis and anticancer activity of chalcone analogues with sulfonyl groups
Muškinja, J., Burmudžija, A., Baskić, D., Popović, S., Todorović, D., Zarić, M., & Ratković, Z. (2019) · Medicinal Chemistry Research · doi:10.1007/s00044-018-02283-4 · Cited by 12
Characterization and biological activities of cyclic (1 → 3, 1 → 6)-β-glucans from Bradyrhizobium japonicum
Nair, A. V., Gummadi, S. N., & Doble, M. (2016) · Biotechnology Letters · doi:10.1007/s10529-016-2122-3 · Cited by 11
Self-citation
Synthesis, crystal structure, Hirshfeld surface analysis, spectroscopic characterization, reactivity study by DFT and MD approaches and molecular docking study of a novel chalcone derivative
Suhana Arshad, B., Pillai, R. R., Zainuri, D. A., Khalib, N. C., Razak, I. A., Armaković, S., Armaković, S. J., Panicker, C. Y., & Alsenoy, C. V. (2017) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2017.01.080 · Cited by 11
Insight into Antiacetylcholinesterase Potential of Modified Chalcones: Synthesis, Characterization, in Vitro, and Computational Investigation
Al‐Maqtari, H. M., Hasan, A. H., Suleiman, M., Abid, F. M. A., Bhat, A. R., Zahidi, M. A. A., Noamaan, M. A., Murugesan, S., Ahmed, S., & Jamalis, J. (2025) · ChemistrySelect · doi:10.1002/slct.202501227 · Cited by 12
Synthesis, spectroscopic characterization, electronic and optical studies of (2Z)‐5,6‐dimethyl‐2‐[(4‐nitrophenyl)methylidene]‐2,3‐dihydro‐1‐benzofuran‐3‐one
Diwaker, Kumar, C. S. C., Kumar, A., Chandraju, S., Quah, C. K., & Fun, H. (2014) · Journal of Computational Science · doi:10.1016/j.jocs.2014.11.005 · Cited by 10
Synthesis and Antimicrobial Evaluation of some Functionalized Heterocycles Derived from Novel Quinolinyl Chalcone
Hassan, M. M., & Farouk, O. (2017) · Journal of Heterocyclic Chemistry · doi:10.1002/jhet.2927 · Cited by 10
Synthesis, molecular structure, DFT studies, in silico docking and molecular dynamics simulations of 2,6 dimethoxychalcone derivatives as BRD4 inhibitors
Khamees, H. A., Mahendra, M., Ananda, S., Sangappa, Y., Al-Ostoot, F. H., & Abad, N. (2021) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2021.131032 · Cited by 9
Substituted chalcones with different positions of the isobornyl substituent: the synthesis and antioxidant activity
Popova, S. A., Pavlova, E. V., Шевченко, О. Г., Chukicheva, I. Y., & Kutchin, A. V. (2022) · Russian Chemical Bulletin · doi:10.1007/s11172-022-3666-0 · Cited by 9
Synthesis and Biological Evaluation of a Novel Series of 1,3-Dicoumarinyl-5-aryl-2-pyrazolines
Čačić, M., Molnar, M., & Strelec, I. (2011) · Heterocycles · doi:10.3987/com-11-12196 · Cited by 9
Novel Nitrogen-Based Chalcone Analogs Provoke Substantial Apoptosis in HER2-Positive Human Breast Cancer Cells via JNK and ERK1/ERK2 Signaling Pathways
Rizeq, B. R., Gupta, I., Kheraldine, H., Elkhalifa, D. H., Farsi, H. F. A., Moustafa, A. A., & Khalil, A. A. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22179621 · Cited by 9
“They also exhibit antioxidant [20], anti-depressant [21], and anti-inflammatory [22] activities, and can potentially reduce resistance to various chemotherapeutic agents [23].”
Background
Chemistry of plant extracts
Rashmi, H. B., & Negi, P. S. (2022) · Elsevier eBooks · doi:10.1016/b978-0-12-822475-5.00004-1 · Cited by 9
Synthesis and Biological Evaluation of Novel Chalcone and Pyrazoline Derivatives Bearing Substituted Vanillin Nucleus
Patel, P. A., Bhadani, V. N., Bhatt, P. V., & Purohit, D. M. (2014) · Journal of Heterocyclic Chemistry · doi:10.1002/jhet.2215 · Cited by 8
Theoretical studies on the interaction between chalcone dyes and Concanavalin A—The reactive group effects on the photophysical and biological properties of the fluorescence probe
Krawczyk, P., Czeleń, P., Szefler, B., & Cysewski, P. (2017) · Journal of Photochemistry and Photobiology A Chemistry · doi:10.1016/j.jphotochem.2017.06.024 · Cited by 8
Employment of thermal analysis applied to the oxidative stability evaluation of biodiesel using chalcone analogues
Berneira, L. M., Rockembach, C. T., da Silva, C. C., de Freitas, S. C., da Rosa, B. N., Pinto, E., dos Anjos, F. M., dos Santos, M. A. Z., & de Pereira, C. M. P. (2020) · Journal of Thermal Analysis and Calorimetry · doi:10.1007/s10973-020-10189-w · Cited by 8
“This antioxidant behavior is directly associated with the resonance present in its structure which can be possibly enhanced throughout the inclusion of hydroxyl groups in the molecule [4, 26].”
BackgroundMethodInfluential
A Comprehensive Appraisal of Chalcones and Their Heterocyclic Analogs as Antimicrobial Agents
Salotra, R., & Utreja, D. (2020) · Current Organic Chemistry · doi:10.2174/1385272824999200922090524 · Cited by 8
Chalcone-based bioactive scaffolds: Comparative antioxidant, antibacterial, and anti-Alzheimer activities supported by docking analysis
Öztürk, C., Bayrak, S., Gerni, S., Atmaca, U., Bayrak, Ç., & Kızıltaş, H. (2026) · Journal of the Indian Chemical Society · doi:10.1016/j.jics.2026.102435 · Cited by 7
A Concise Review on Synthesis, Anti-inflammatory and Antioxidant Activities of Chalcone
Singh, D., Kaundal, V., Aggarwal, N., Jindal, S., Ankalgi, A. D., & Goyal, K. (2022) · Asian Journal of Pharmaceutical Research · doi:10.52711/2231-5691.2022.00007 · Cited by 7
Synthesis of O-alkyl derivatives of dehydrozingerone analogues
Muškinja, J., Ratković, Z., Ranković, B., & Kosanić, M. (2016) · Kragujevac Journal of Science · doi:10.5937/kgjsci1638097m · Cited by 7
Synthesis, Characterization and Antiinflammatory Activity of Chalcone Derivatives Linked with Apocynin and 5-Nitrofuran Moiety
Reddy, A. L. V. K., & Kathale, N. E. (2017) · Asian Journal of Chemistry · doi:10.14233/ajchem.2018.20950 · Cited by 7
Chalcones as Scavengers of HOCl and Inhibitors of Oxidative Burst: Structure-Activity Relationship Studies
Martins, T. S., Silva, V. L. M., Silva, A. M. S., Lima, J. L. F. C., Fernandes, E. G. R., & Ribeiro, D. (2020) · Medicinal Chemistry · doi:10.2174/1573406417666201230093207 · Cited by 7
Synthesis and characterization of new 3,5-disubstituted-4,5-dihydro-1H-pyrazole and their carbothioamide derivatives
Ibrahim, M. (2015) · European Journal of Chemistry · doi:10.5155/eurjchem.6.1.78-83.1148 · Cited by 7
Computational Modeling, Synthesis, and Antioxidant Potential of Novel Phenylcarbamoylbenzoic Acid Analogs in Combating Oxidative Stress
Bayoumi, W. A., El‐Sayed, M. A. ‐., Baraka, H. N., & Abou-zeid, L. A. (2012) · Archiv der Pharmazie · doi:10.1002/ardp.201200183 · Cited by 7
Claisen–Schmidt condensation: Synthesis of (1S,6R)/(1R,6S)‐2‐oxo‐N,4,6‐triarylcyclohex‐3‐enecarboxamide derivatives with different substituents in H2O/EtOH
Mousavi, S. R. (2016) · Chirality · doi:10.1002/chir.22653 · Cited by 7
Synthesis and biological evaluation of glycosides containing triazene-chalcones
Qiang, L., Zhang, S., Liu, M., Li, J., Zhang, X., & Long, Y. (2017) · Molecular Diversity · doi:10.1007/s11030-017-9768-1 · Cited by 7
“Chalcones occur widely in various plants, and recent studies have shown that they can produce diverse pharmacological results, including antioxidant [11, 12], anti-inflammatory [13], antimalarial [14,15], antileishmanial [16], anticancer [17–19], and antimicrobial effects [20,21].”
Background
Synthesis a novel Schiff base and Chalcone derivatives compounds and using as flame retardant for unsaturated polyester and epoxy resins
Jawad, S. F., Behget, S. A., & Al-Baiati, M. N. (2019) · IOP Conference Series Materials Science and Engineering · doi:10.1088/1757-899x/571/1/012090 · Cited by 6
Investigating the Anticancer Properties of the Essential Oil and Aqueous Extract of Moringa oleifera and its Biosynthesized Metal Nanoparticles on MCF-7 and BT-549 Cell Lines
Noruzpour, M., Zakaria, R. A., Zare, N., Ebrahimi, H. A., Khankandi, H. P., & Bourang, S. (2024) · Journal of Breast Disease · doi:10.61186/ijbd.17.1.59 · Cited by 6

Authors: Sivakumar, P. M., Prabhakar, P. K., & Doble, M.
Affiliations: Indian Institute of Technology Madras (IN)
Corresponding author: Doble, M.
ORCID: Sivakumar, P. M.
Prabhakar, P. K.
Doble, M.
Venue: Medicinal Chemistry Research
Publisher: Springer Science and Business Media LLC
Published: 2010-03-23
Volume: 20
Issue: 4
Pages: 482-492
ISSN: 1054-2523 (ISSN-L)
1554-8120
DOI: 10.1007/s00044-010-9342-1
OpenAlex: W2092646120
Cited by: 144
References: 58
Citations by year: 2026: 4 · 2025: 6 · 2024: 7 · 2023: 11 · 2022: 11 · 2021: 5 · 2020: 14 · 2019: 12 · 2018: 13 · 2017: 14 · 2016: 15 · 2015: 9 · 2014: 9 · 2013: 5 · 2012: 5
FWCI: 2.22
Type: journal article
Language: en
Open access: closed
Licence: www.springer.com/tdm (tdm)
Locations: Medicinal Chemistry Research (publishedVersion)
Funders: Indian Institute of Technology Madras
Topics: Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
Physical Sciences › Chemistry › Organic Chemistry › Free Radicals and Antioxidants
Physical Sciences › Chemistry › Organic Chemistry › Synthesis of Organic Compounds
Keywords: chalcones, chalcone derivatives, antioxidant activity, QSAR, Claisen-Schmidt condensation, superoxide radical scavenging, hydrogen peroxide scavenging, DPPH radical scavenging, reducing power, substituent effects, lipophilicity, structure-activity relationship

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Synthesis, antioxidant evaluation, and quantitative structure–activity relationship studies of chalcones

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