2021
DOI: 10.1016/j.matpr.2020.03.143
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Novel synthesised chrysin derivatives offer noteworthy insight into the structural scaffolds required for improved anti-proliferative activity

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“…Analogous compounds 91 (R 1 =H, CH 3 or CF 3 ) were shown to generally exhibit better antiproliferative activity than the parent esculetin against A549 non‐small cell lung carcinoma and B16 mouse melanoma cell lines [114] . Further examples of phenolic Mannich bases of heterocyclic substrates with anticancer activity include aminomethylated 4‐hydroxy‐1,8‐naphthyridines 92 (R 1 =CH 3 or C 6 H 5 ), [115] aminomethylated 5,7‐dihydroxyquinolin‐4‐ones 93 , [116] or aminomethylated 6‐hydroxyaurones 94 (compound with NR 2 =N(CH 3 )CH 2 C 6 H 5 and Ar=3,4,5‐(H 3 CO) 3 C 6 H 2 had IC 50 =3.9 μM against PC‐3 cells) [117] (Figure 11).…”
Section: Anticancer and Cytotoxic Activity Of Mannich Bases Derived F...mentioning
confidence: 99%
“…Analogous compounds 91 (R 1 =H, CH 3 or CF 3 ) were shown to generally exhibit better antiproliferative activity than the parent esculetin against A549 non‐small cell lung carcinoma and B16 mouse melanoma cell lines [114] . Further examples of phenolic Mannich bases of heterocyclic substrates with anticancer activity include aminomethylated 4‐hydroxy‐1,8‐naphthyridines 92 (R 1 =CH 3 or C 6 H 5 ), [115] aminomethylated 5,7‐dihydroxyquinolin‐4‐ones 93 , [116] or aminomethylated 6‐hydroxyaurones 94 (compound with NR 2 =N(CH 3 )CH 2 C 6 H 5 and Ar=3,4,5‐(H 3 CO) 3 C 6 H 2 had IC 50 =3.9 μM against PC‐3 cells) [117] (Figure 11).…”
Section: Anticancer and Cytotoxic Activity Of Mannich Bases Derived F...mentioning
confidence: 99%