Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity

Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity Publisher Pubmed

Mohammadian E¹ ; Oghabi Bakhshaiesh T² ; Jouyban A^{3, 4} ; Nazeri E² ; Hasanvand Z¹ ; Moghimi S⁵ ; Motahari R¹ ; Firoozpour L¹ ; Bijanzadeh H⁶ ; Alizadeh Sani M⁷ ; Hosseinzadeh E⁵ ; Esmaeili R² ; Foroumadi A^{1, 5}

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2. Genetics Department, Breast Cancer Research Center, Motamed Cancer Institute, ACECR, Tehran, Iran
3. Pharmaceutical Analysis Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
4. Faculty of Pharmacy, Near East University, North Cyprus, Nicosia, Turkey
5. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
6. Department of Environmental Sciences, Faculty of Natural Resources and Marine Sciences, Tarbiat Modares University, Tehran, Iran
7. Division of Food Safety and Hygiene, Department of Environmental Health, School of Public Health, Tehran University of Medical Sciences, Tehran, Iran

Source: Archiv der Pharmazie Published:2023

Abstract

An important role has been considered for the vascular endothelial growth factor receptor 2 (VEGFR-2) in the angiogenesis process, so that its inhibition is an important scientific way for cancer treatment. In this work, new thienopyrimidine derivatives were synthesized and evaluated. Compared with sorafenib, the majority of the target compounds had antiproliferative activity against the PC3, HepG2, MCF7, SW480, and HUVEC cell lines, especially 9h with IC50 values of 4.5–15.1 μM, confirming the noticeable cytotoxic effects on the listed cell lines (PC3, HepG2, SW480, and HUVEC). Analyses by flow cytometry on SW480 and HUVEC cells revealed that 9n, 9k, 9h, and 9q led to apoptotic cell death. The result of the chick chorioallantoic membrane assay showed that 9h effectively reduced the number of corresponding blood vessels. Finally, the inhibitory effect on VEGFR-2 phosphorylation was considered as the outcome of Western blot analysis of compound 9h. © 2022 Deutsche Pharmazeutische Gesellschaft.

Style	Citing Format
MLA	Mohammadian E, et al.. "Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity." Archiv der Pharmazie, vol. 356, no. 3, 2023, pp. -.
APA	Mohammadian E, Oghabi Bakhshaiesh T, Jouyban A, Nazeri E, Hasanvand Z, Moghimi S, Motahari R, Firoozpour L, Bijanzadeh H, Alizadeh Sani M, Hosseinzadeh E, Esmaeili R, Foroumadi A (2023). Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity. Archiv der Pharmazie, 356(3), -.
Chicago	Mohammadian E, Oghabi Bakhshaiesh T, Jouyban A, Nazeri E, Hasanvand Z, Moghimi S, Motahari R, et al.. "Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity." Archiv der Pharmazie 356, no. 3 (2023): -.
Harvard	Mohammadian E et al. (2023) 'Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity', Archiv der Pharmazie, 356(3), pp. -.
Vancouver	Mohammadian E, Oghabi Bakhshaiesh T, Jouyban A, Nazeri E, Hasanvand Z, Moghimi S, et al.. Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity. Archiv der Pharmazie. 2023;356(3):-.
BibTex	@article{ author = {Mohammadian E and Oghabi Bakhshaiesh T and Jouyban A and Nazeri E and Hasanvand Z and Moghimi S and Motahari R and Firoozpour L and Bijanzadeh H and Alizadeh Sani M and Hosseinzadeh E and Esmaeili R and Foroumadi A}, title = {Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity}, journal = {Archiv der Pharmazie}, volume = {356}, number = {3}, pages = {-}, year = {2023} }
RIS	TY - JOUR AU - Mohammadian E AU - Oghabi Bakhshaiesh T AU - Jouyban A AU - Nazeri E AU - Hasanvand Z AU - Moghimi S AU - Motahari R AU - Firoozpour L AU - Bijanzadeh H AU - Alizadeh Sani M AU - Hosseinzadeh E AU - Esmaeili R AU - Foroumadi A TI - Thienopyrimidine-Based Agents Bearing Diphenylurea: Design, Synthesis, and Evaluation of Antiproliferative and Antiangiogenic Activity JO - Archiv der Pharmazie VL - 356 IS - 3 SP - EP - PY - 2023 ER -

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