Objective:

2

To design and synthesize series of rotundic acid derivatives by introducing aromatic ester groups with rotundic acid as the parent nucleus

test their anti-tumor activity

in vitro

investigate the structure-activity relationship of rotundic acid derivatives in inhibiting tumor cell proliferation

and obtain the novel rotundic acid derivatives with high anti-tumor activity.

Method:

2

Compounds 1-8 were synthesized with rotundic acid as the initial raw material through the 28-etherification

3

β

and 23di-aromatic esterification eaction. The anti-tumor activities

in vitro

were evaluated by MTT assay against A375 (human malignant melanoma cells)

HeLa (human cervical cancer cells)

SPC-A1 (human lung adenocarcinoma cells)

and HepG2 (human liver cancer cells).

Result:

2

Compounds

2-8

were new compounds. Their structures were identified by melting point (MP)

high resolution electrospray ionization tandem mass spectrometry (HR-ESI-MS)

1

H nuclear magnetic resonance (

1

H-NMR) and

13

C nuclear magnetic resonance (

13

C-NMR). MTT results showed that compounds

3

5

and

8

exhibited significant anti-tumor activity

especially compound

5

was found to have the best inhibition activity on HeLa

A375

HepG2 and SPC-A1 with IC

50

values of (5.25±1.08)

(5.99±0.88)

(3.31±1.89)

(5.74±1.78) μmol·L

-1

1.92

3.22

3.79

3.72 times of that of rotundic acid

respectively.

Conclusion:

2

Compound

5

has significant anti-tumor activity with great significance for further research and development of new anti-tumor medicines.