Design and synthesis of novel 1,2,3-triazole derivatives of coronopilin as anti-cancer compounds

Khazir, Jabeena; Hyder, Irfan; Gayatri, J. Laxmi; Yandrati, Leela Prasad; Nalla, Naresh; Chasoo, Gousia; Mahajan, Ajay; Saxena, Ajit Kumar; Alam, Mohammad Mahboob; Qazi, G. N.; Kumar, Halmuthur M. Sampath

doi:10.1016/j.ejmech.2014.05.053

Cited by 36 publications

(16 citation statements)

References 17 publications

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“…21 α-Santonin derivatives have also been reported to possess anti-inflammatory activity mainly by targeting the NF-κB signalling pathway. 26 As part of our continued interest in the design and synthesis of sesquiterpene lactone based anticancer agents, 21,27 we here report the synthesis and anticancer activity of Micheal typethiol adducts of α-santonin. Michael adducts were synthesized through reaction of a series of aromatic, aliphatic, cyclic and heterocyclic thiols with the α-methylene group generated on the lactone ring of santonin.…”

Section: A C C E P T E D Accepted Manuscriptmentioning

confidence: 99%

Design, synthesis and anticancer activity of Michael-type thiol adducts of α-santonin analogue with exocyclic methylene

Khazir

Riley²,

Chashoo³

et al. 2015

European Journal of Medicinal Chemistry

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Section: A C C E P T E D Accepted Manuscriptmentioning

confidence: 99%

Design, synthesis and anticancer activity of Michael-type thiol adducts of α-santonin analogue with exocyclic methylene

Khazir

Riley²,

Chashoo³

et al. 2015

European Journal of Medicinal Chemistry

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“…Novel coronopilin derivatives were prepared by incorporating the substituted 1,2,3‐triazole moiety at the β‐position of the cyclopentenone ring in parthenin via CuAAC reaction. Among these derivatives, chlorobenzoyl‐substituted triazole 3 a exhibited anticancer activity on prostate cancer cells and significant inhibition of the NF‐κB pathway (p65) (Figure ) …”

Section: Dual Effect Of Phytochemicals On Oxidative Stress (Antioxidamentioning

confidence: 99%

What Has Come out from Phytomedicines and Herbal Edibles for the Treatment of Cancer?

Bonam

Tunki

et al. 2018

ChemMedChem

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Several modern treatment strategies have been adopted to combat cancer with the aim of minimizing toxicity. Medicinal plant-based compounds with the potential to treat cancer have been widely studied in preclinical research and have elicited many innovations in cutting-edge clinical research. In parallel, researchers have eagerly tried to decrease the toxicity of current chemotherapeutic agents either by combining them with herbals or in using herbals alone. The aim of this article is to present an update of medicinal plants and their bioactive compounds, or mere changes in the bioactive compounds, along with herbal edibles, which display efficacy against diverse cancer cells and in anticancer therapy. It describes the basic mechanism(s) of action of phytochemicals used either alone or in combination therapy with other phytochemicals or herbal edibles. This review also highlights the remarkable synergistic effects that arise between certain herbals and chemotherapeutic agents used in oncology. The anticancer phytochemicals used in clinical research are also described; furthermore, we discuss our own experience related to semisynthetic derivatives, which are developed based on phytochemicals. Overall, this compilation is intended to facilitate research and development projects on phytopharmaceuticals for successful anticancer drug discovery.

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“…Because of the wide clinical applications, interest in pyrimidine derivatives has led to the preparation and evaluation of hundreds of such type of molecules as potent anticancer agents revealing that pyrimidine is an important pharmacophore in the discovery of novel active molecules. In view of the above facts and in continuation of our previous efforts in the field of synthesis of novel anticancer therapeutics, the target in this study was to synthesize analogues having pyrimidine moiety conjugated through acetamide and hydrazinyl linkage with different aromatic/heterocyclic groups of documented cytotoxic potency against several cancer cell lines.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine

Khazir

Mir

Chashoo

et al. 2020

Journal of Heterocyclic Chem

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A library of acetamide and hydrazine analogues were generated on the pyrimidine ring through a multistep reaction starting from 5‐nitro‐pyrimidine‐4,6‐diol and pyrimidine‐4,6‐diol, respectively. The synthesized analogues were screened for in vitro cytotoxic activity against various human cancer cell lines like HCT‐1 and HT‐15 (colon), MCF‐7(breast), PC‐3 (prostrate), SF268 (CNS) using MTT method. From the bioassay results, it was observed that even though many of the synthesized derivatives exhibited a good potency against various screened cancer cell lines, compound 14a from the acetamide series was found to show potent anticancer activity on all the tested cancer cell lines with IC50 value of 0.36μM on CNS cell line and 1.6μM on HT‐21 cell line, and compound 19xxi from hydrazine series of pyrimidine showed potent activity against three tested cancer cell lines with IC50 value of 0.76μM on HT‐29 cell line, 2.6μM on HCT‐15, and 3.2μM on MCF‐7 cell line.

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Design and synthesis of novel 1,2,3-triazole derivatives of coronopilin as anti-cancer compounds

Cited by 36 publications

References 17 publications

Design, synthesis and anticancer activity of Michael-type thiol adducts of α-santonin analogue with exocyclic methylene

Design, synthesis and anticancer activity of Michael-type thiol adducts of α-santonin analogue with exocyclic methylene

What Has Come out from Phytomedicines and Herbal Edibles for the Treatment of Cancer?

Design, synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine

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