Microwave-assisted multicomponent synthesis of antiproliferative 2,4-dimethoxy-tetrahydropyrimido[4,5-]quinolin-6(7)-ones
In this study, we demonstrate a simple, highly efficient, rapid and convenient series of 2,4-dimethoxy-tetrahydropyrimido[4,5- b ]quinolin-6(7 H )-ones 4a-v . Microwave irradiation facilitates the one-pot multicomponent reaction of different aromatic aldehydes, 6-amino-2,4-dimethoxypyrimidine and di...
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Veröffentlicht in: | RSC advances 2022-10, Vol.12 (47), p.344-3415 |
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Hauptverfasser: | , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | In this study, we demonstrate a simple, highly efficient, rapid and convenient series of 2,4-dimethoxy-tetrahydropyrimido[4,5-
b
]quinolin-6(7
H
)-ones
4a-v
. Microwave irradiation facilitates the one-pot multicomponent reaction of different aromatic aldehydes, 6-amino-2,4-dimethoxypyrimidine and dimedone using glacial acetic acid. Metal-free multicomponent synthesis, shorter reaction time, higher product yield, easy product purification without column chromatography and outstanding green credential parameters are the key features of this protocol. We analysed
4a-v
against six human tumour cell lines for antiproliferative activity.
4h
,
4o
,
4q
and
4v
show good antiproliferative activity with a good
in silico
ADMET profile. Furthermore,
4h
,
4o
,
4q
and
4v
also show drug-likeness properties by obeying drug-like filters.
Herein, we demonstrate a simple, rapid and green synthesis of 2,4-dimethoxy-THPQs under microwave irradiation and their antiproliferative activity,
in silico
ADMET and drug-likeness studies were carried out. |
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ISSN: | 2046-2069 2046-2069 |
DOI: | 10.1039/d2ra04669e |