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Table 1 Synthesized DHPM derivatives

From: Impact of kinesin Eg5 inhibition by 3,4-dihydropyrimidin-2(1H)-one derivatives on various breast cancer cell features

Ent Reagent Prod. Yield (%)
R1 R2 R3 X
1 Ph Me Me O 4c 99
2 Ph OCH2CH3 Me S 4d 93
3 Ph Me Me S 4e 83
4 4-Cl-Ph OCH2CH3 Me O 4f 87
5 4-Cl-Ph OCH2CH3 Me S 4h 80
6 4-Cl-Ph Me Me S 4i 77
7 3-OH-Ph OCH2CH3 Me O 4j 98
8 3-OH-Ph Me Me O 4k 80
9a 3-OH-Ph OCH2CH3 Me S Mon 93
10 3-OH-Ph Me Me S 4m 88
11 2-OH-Ph OCH2CH3 Me O 4n 84
12 2-OH-Ph Me Me O 4o 80
13 2-OH-Ph OCH2CH3 Me S 4p 84
14 2-OH-Ph Me Me S 4q 90
15 3-NO2-Ph OCH2CH3 Me O 4r 96
16 3-NO2-Ph OCH2CH3 Me S 4t 86
17 3-NO2-Ph Me Me S 4u 86
18 2-NO2-Ph OCH2CH3 Me O 4v 70
19 2-NO2-Ph Me Me O 4x 60
20 2-NO2-Ph Me Me S 4z 60e
21 4-OH-3-MeO-Ph OCH2CH3 Me O 4ba 98
22 4-OH-3-MeO-Ph OCH2CH3 Me S 4bc 85
23 4-OH-3-MeO-Ph Me Me S 4bd 85
24 H OCH2CH3 Me O 4be 96
25 Me Me Me O 4bj 66
26 Me OCH2CH3 Me S 4bk 70
27 OCH2CH3 Me O 4bm 87
28 Me Me O 4bn 79
29b OCH2CH3 Me S 4bo 70
30 Me Me S 4bp 71
31 3-OH-Ph O 4bq 60
32c 3-OH-Ph S 4br 72
33 3-OH-Ph O 4bs 70
34d 3-OH-Ph S 4bt 70
35 OCH2CH3 Me O 4bu 66f
36 Me Me S 4bv 50f
37 OCH2CH3 Me S 4bx 42f
38 Me Me O 4by 83
  1. aMonastrol. bPiperastrol. cEnastron. dDimethylenastron. e12 h of reaction. fProduct formation was above 90%, but there was considerable loss during purification column chromatography.
  2. 37 DHPM derivatives and monastrol were studied in this work.