Novel 1‐Triazolylpyranopyrazoles as Highly Potent Anticancer Agents Obtained via MW‐Assisted Synthesis. Issue 4 (21st January 2021)

• Record Type: Journal Article
• Authors: Kumar, Rakesh; Yadav, Neha; Leekha, Ankita; Bawa, Rashim; Gahlyan, Parveen; Bhandari, Mamta; Arora, Ritu; Kamra Verma, Anita; Kakkar, Rita
• Is Part Of: ChemistrySelect. Volume 6:Issue 4(2021)
• Page Start: 589
• Page End: 594
• Publication Date: 2021-01-21
• Subjects: Cancer -- Molecular docking -- Heterocycles -- Topoisomerase IIa inhibitors -- Triazoles; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.202003680
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: A series of novel 1‐triazolylpyranopyrazole derivatives has been designed and synthesized using microwave irradiation, with the purpose of obtaining repositioned pharmaceutics. The newly synthesized 1‐triazolylpyranopyrazoles (7 a –7 n), along with their precursor alkyne (5), have been screened for their in‐vitro anti‐tumor activity against Hep3B and HEK cell lines. The majority of triazolylpyranopyrazoles elicited outstanding anti‐cancer activity on Hep3B cell lines even at concentrations as low as 25μg/mL. Further, molecular docking of these active compounds against Topoisomerase IIa substantiated a plausible target site for the compounds inhibiting Hep3B cells effectively. The biological assay results for the triazolylpyranopyrazole even surpassed the activity of the reference drug i . e . Doxorubicin, thereby appearing to be potent anticancer agents. Abstract : The authors have reported the synthesis of novel 1‐triazolylpyranopyrazole derivatives using microwave irradiation which have been screened for their in‐vitro anti‐tumor activity against Hep3B and HEK cell lines. The majority of these compounds have shown outstanding anti‐cancer activity on Hep3B cell lines even at concentrations as low as 25μg/mL. Further, molecular docking of the active compounds against Topoisomerase IIa substantiated a plausible target site for the compounds inhibiting Hep3B cells effectively. The biological assay results of most of these compounds even surpassed the activity of the reference drug i . e . Doxorubicin.