Add time:07/16/2019         Source:sciencedirect.com

Some derivatives of 3-ethyl-2-mercapto-thieno[2,3-d]pyrimidin-4(3H)-ones were synthesized using ethyl 2-aminothiophene-3-carboxylates as precursors in order to estimate their cytotoxicity, respectively proliferative activity.Thienopyrimidinones containing thiosemicarbazide as well as 1,3,4-thiadiazole moieties were evaluated for their cytotoxical effect on four cancer cell lines: HT-29, breast cancer cells MDA-MB-231, HeLa, HepG2 as well as human diploid cell line Lep-3. Compounds 5b, 6a and 6b revealed cytotoxicity to the four studied cancer cell lines. The highst cytotoxicity against MDA-MB-31 exhibited the thiosemicarbazide 5b with IC50 2.31.10−4 μM, but most active towards HT-29 cell lines was thienopyrimidine 6c with IC50 0.001 μM. Compound 6a showed the highest inhibitory activity with IC50 - 0.99 μM to human liver carcinoma HepG2 cells and low cytotoxicity towards Lep3 (IC50 = 191 μM). The thienopyrimidine derivative linked to thiadiazole 6b was toxic to the four studied cancer cell lines, especially to HeLa (IC50–0.83 μM), and besides that the compound demonstrated toxicity to Lep 3 cells at very high concentration 89 × 103 μM.The solid-state photostability of the derivatives 5a-c and 6a-c was tested by irradiation with UV light. All of the studied compounds show solid-state photostability in 240 min of irradiation.Using MOE software molecular docking of the three ligands 5b, 6b and 7 was accomplished into an internal pocket formed by the activation segment and the P-loop of V599EB-Raf. It was established that the binding of the ligands to V599EB-Raf promotes an inactive conformation of the enzyme.

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