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Novel 1‐Triazolylpyranopyrazoles as Highly Potent Anticancer Agents Obtained via MW‐Assisted Synthesis
Author(s) -
Kumar Rakesh,
Yadav Neha,
Leekha Ankita,
Bawa Rashim,
Gahlyan Parveen,
Bhandari Mamta,
Arora Ritu,
Kamra Verma Anita,
Kakkar Rita
Publication year - 2021
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202003680
Subject(s) - topoisomerase , chemistry , in vitro , pharmaceutics , doxorubicin , combinatorial chemistry , cell culture , docking (animal) , biological activity , cancer cell lines , stereochemistry , pharmacology , cancer cell , biochemistry , cancer , biology , medicine , genetics , nursing , chemotherapy
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.