α-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivatives

Figures & data

Figure 1. α-Gls inhibitors used as antidiabetic drugs.

Figure 2. Structures of cyclic urea 1–5 and carbamate 6–13 derivatives.

Table 1. IC₅₀ values of anti-α-Gls activity of the compounds 1–13.

Compound	IC50 μM*
1	104.06 ± 0.65
2	63.03 ± 2.12
3	67.59 ± 1.90
4	68.66 ± 3.02
5	67.63 ± 0.27
6	76.02 ± 5.66
7	83.46 ± 14.21
8	71.74 ± 2.90
9	77.61 ± 2.27
10	99.48 ± 0.16
11	70.41 ± 5.21
12	49.85 ± 0.10
13	75.52 ± 8.11
acarbose	121.01 ± 12.18

* Results are expressed as mean ± standard deviation.

Figure 3. Cell survival rate diagram of compounds show survival of HeLa, A549 and MDA-MB-453 cells grown for 72 h in the presence of increasing concentrations of investigated compounds.

Table 2. IC₅₀ values (μM) of tested compounds against malignant cell lines.

IC50*
compounds	HeLa	A549	MDA-MB-453
2	155.63 ± 31.75	110.69 ± 0.85	83.41 ± 1.60
8	158.29 ± 6.04	155.83 ± 0.70	112.42 ± 4.91
11	194.44 ± 1.44	200.00 ± 2.37	163.59 ± 3.93
12	138.74 ± 8.28	180.13 ± 2.57	107.63 ± 4.95

* Results are expressed as mean ± standard deviation.

^#The other tested compounds didn’t exhibit cytotoxic activity (the highest tested concentration was 200 μM).

Figure 4. Morphological changes observed on HeLa cells after 24 hours treatment with IC₅₀ and 2 × IC₅₀ concentrations of compounds dilutions. (A) Control; (B) IC₅₀, (C) 2 × IC₅₀ (supernatant) compound 2; (D) IC₅₀, (E) 2 × IC₅₀ (supernatant) compound 8; (F) IC₅₀, (G) 2 × IC₅₀ (supernatant) compound 11; (I) IC₅₀, (H) 2 × IC₅₀ (supernatant) compound 12; fluorescent microscope (PALM MicroBeamsystems, Carl Zeiss, 20×)

Table 3. Statistical performance of the final PLS model.

Statistical performance of the model				Molecular descriptors included in PLS model
R^2cal	R^2CV	RMSEC	RMSECV	CIQPlogS(+), FISA(+), Percent Human Oral Absorption(−), QPlogKp(−), QPlogPo/w(−), IP(eV)(+), QPPMDCK(−)
0.901	0.680	0.021	0.041