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Synthesis and antiproliferative activity of pterostilbene and [Formula: see text]-methoxy pterostilbene Mannich base derivatives against Hela cells.

Liu C, Dong L, Wang S, Wang Q - Mol. Divers. (2015)

Bottom Line: Fourteen novel pterostilbene (1) and [Formula: see text]-methoxy pterostilbene (2) Mannich base derivatives (3-16) were synthesized via the microwave-assisted Mannich reaction of 1 or 2 with various secondary amines and formaldehyde.The regioselectivity of the reaction occurred preferentially at [Formula: see text] position of the B-ring of stilbene.Compounds 1-3, 7, 11-13, and 16 displayed higher (lower [Formula: see text] values) activity than the positive control cisplatin [Formula: see text].

View Article: PubMed Central - PubMed

Affiliation: College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China.

ABSTRACT
Fourteen novel pterostilbene (1) and [Formula: see text]-methoxy pterostilbene (2) Mannich base derivatives (3-16) were synthesized via the microwave-assisted Mannich reaction of 1 or 2 with various secondary amines and formaldehyde. The regioselectivity of the reaction occurred preferentially at [Formula: see text] position of the B-ring of stilbene. The biological testing results showed that all the target compounds exhibit antiproliferative activity against Hela cells from [Formula: see text]-[Formula: see text]. Compounds 1-3, 7, 11-13, and 16 displayed higher (lower [Formula: see text] values) activity than the positive control cisplatin [Formula: see text].

No MeSH data available.


Dose-response curve of compounds 1, 2, 3  and 7 on Hela cell proliferation assay
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Fig1: Dose-response curve of compounds 1, 2, 3 and 7 on Hela cell proliferation assay

Mentions: The antiproliferative activity of the pterostilbene (1), -methoxypterostilbene (2), and the Mannich base derivatives 3–16 was assessed using the CCK-8 [2H-tetrazolium, 5-(2,4-disulfophenyl)-3-(2-methoxy-4-nitrophenyl)-2-(4- nitrophenyl) inner salt, sodium salt (1:1)] assay using the human cervical carcinoma Hela cell line. The results are shown in Table 1. The dose-response curves for the CCK-8 assay of compounds 1, 2, 3 and 7 on Hela cells proliferation are shown in Fig. 1. Cisplatin (DDP) was used as positive control. The results show that all the test compounds exhibit moderate to potent antiproliferative activity against Hela cells.Table 1


Synthesis and antiproliferative activity of pterostilbene and [Formula: see text]-methoxy pterostilbene Mannich base derivatives against Hela cells.

Liu C, Dong L, Wang S, Wang Q - Mol. Divers. (2015)

Dose-response curve of compounds 1, 2, 3  and 7 on Hela cell proliferation assay
© Copyright Policy - OpenAccess
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4591201&req=5

Fig1: Dose-response curve of compounds 1, 2, 3 and 7 on Hela cell proliferation assay
Mentions: The antiproliferative activity of the pterostilbene (1), -methoxypterostilbene (2), and the Mannich base derivatives 3–16 was assessed using the CCK-8 [2H-tetrazolium, 5-(2,4-disulfophenyl)-3-(2-methoxy-4-nitrophenyl)-2-(4- nitrophenyl) inner salt, sodium salt (1:1)] assay using the human cervical carcinoma Hela cell line. The results are shown in Table 1. The dose-response curves for the CCK-8 assay of compounds 1, 2, 3 and 7 on Hela cells proliferation are shown in Fig. 1. Cisplatin (DDP) was used as positive control. The results show that all the test compounds exhibit moderate to potent antiproliferative activity against Hela cells.Table 1

Bottom Line: Fourteen novel pterostilbene (1) and [Formula: see text]-methoxy pterostilbene (2) Mannich base derivatives (3-16) were synthesized via the microwave-assisted Mannich reaction of 1 or 2 with various secondary amines and formaldehyde.The regioselectivity of the reaction occurred preferentially at [Formula: see text] position of the B-ring of stilbene.Compounds 1-3, 7, 11-13, and 16 displayed higher (lower [Formula: see text] values) activity than the positive control cisplatin [Formula: see text].

View Article: PubMed Central - PubMed

Affiliation: College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China.

ABSTRACT
Fourteen novel pterostilbene (1) and [Formula: see text]-methoxy pterostilbene (2) Mannich base derivatives (3-16) were synthesized via the microwave-assisted Mannich reaction of 1 or 2 with various secondary amines and formaldehyde. The regioselectivity of the reaction occurred preferentially at [Formula: see text] position of the B-ring of stilbene. The biological testing results showed that all the target compounds exhibit antiproliferative activity against Hela cells from [Formula: see text]-[Formula: see text]. Compounds 1-3, 7, 11-13, and 16 displayed higher (lower [Formula: see text] values) activity than the positive control cisplatin [Formula: see text].

No MeSH data available.