{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Elwan A"],"funding":["Princess Nourah bint Abdulrahman University Researchers","Princess Nourah bint Abdulrahman University"],"pagination":["5047"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9370530"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["27(15)"],"pubmed_abstract":["This work is one of our efforts to discover potent anticancer agents. We modified the most promising derivative of our previous work concerned with the development of VEGFR-2 inhibitor candidates. Thirteen new compounds based on benzoxazole moiety were synthesized and evaluated against three human cancer cell lines, namely, breast cancer (MCF-7), colorectal carcinoma (HCT116), and hepatocellular carcinoma (HepG2). The synthesized compounds were also evaluated against VEGFR-2 kinase activity. The biological testing fallouts showed that compound <b>8d</b> was more potent than standard sorafenib. Such compound showed IC<sub>50</sub> values of 3.43, 2.79, and 2.43 µM against the aforementioned cancer cell lines, respectively, compared to IC<sub>50</sub> values of 4.21, 5.30, and 3.40 µM reported for sorafenib. Compound <b>8d</b> also was found to exert exceptional VEGFR-2 inhibition activity with an IC<sub>50</sub> value of 0.0554 μM compared to sorafenib (0.0782 μM). In addition, compound <b>8h</b> revealed excellent cytotoxic effects with IC<sub>50</sub> values of 3.53, 2.94, and 2.76 µM against experienced cell lines, respectively. Furthermore, compounds <b>8a</b> and <b>8e</b> were found to inhibit VEGFR-2 kinase activity with IC<sub>50</sub> values of 0.0579 and 0.0741 μM, exceeding that of sorafenib. Compound <b>8d</b> showed a significant apoptotic effect and arrested the HepG2 cells at the pre-G1 phase. In addition, it exerted a significant inhibition for TNF-α (90.54%) and of IL-6 (92.19%) compared to dexamethasone (93.15%). The molecular docking studies showed that the binding pattern of the new compounds to VEGFR-2 kinase was similar to that of sorafenib."],"journal":["Molecules (Basel, Switzerland)"],"pubmed_title":["Modified Benzoxazole-Based VEGFR-2 Inhibitors and Apoptosis Inducers: Design, Synthesis, and Anti-Proliferative Evaluation."],"pmcid":["PMC9370530"],"funding_grant_id":["PNURSP2022R116"],"pubmed_authors":["Abdallah AE","Dahab MA","Mehany ABM","Elkady H","Mahdy HA","Elwan A","Alsfouk AA","Nabeeh A","Adel M","Elkaeed EB","Taghour MS","Eissa IH"],"additional_accession":[]},"is_claimable":false,"name":"Modified Benzoxazole-Based VEGFR-2 Inhibitors and Apoptosis Inducers: Design, Synthesis, and Anti-Proliferative Evaluation.","description":"This work is one of our efforts to discover potent anticancer agents. We modified the most promising derivative of our previous work concerned with the development of VEGFR-2 inhibitor candidates. Thirteen new compounds based on benzoxazole moiety were synthesized and evaluated against three human cancer cell lines, namely, breast cancer (MCF-7), colorectal carcinoma (HCT116), and hepatocellular carcinoma (HepG2). The synthesized compounds were also evaluated against VEGFR-2 kinase activity. The biological testing fallouts showed that compound <b>8d</b> was more potent than standard sorafenib. Such compound showed IC<sub>50</sub> values of 3.43, 2.79, and 2.43 µM against the aforementioned cancer cell lines, respectively, compared to IC<sub>50</sub> values of 4.21, 5.30, and 3.40 µM reported for sorafenib. Compound <b>8d</b> also was found to exert exceptional VEGFR-2 inhibition activity with an IC<sub>50</sub> value of 0.0554 μM compared to sorafenib (0.0782 μM). In addition, compound <b>8h</b> revealed excellent cytotoxic effects with IC<sub>50</sub> values of 3.53, 2.94, and 2.76 µM against experienced cell lines, respectively. Furthermore, compounds <b>8a</b> and <b>8e</b> were found to inhibit VEGFR-2 kinase activity with IC<sub>50</sub> values of 0.0579 and 0.0741 μM, exceeding that of sorafenib. Compound <b>8d</b> showed a significant apoptotic effect and arrested the HepG2 cells at the pre-G1 phase. In addition, it exerted a significant inhibition for TNF-α (90.54%) and of IL-6 (92.19%) compared to dexamethasone (93.15%). The molecular docking studies showed that the binding pattern of the new compounds to VEGFR-2 kinase was similar to that of sorafenib.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Aug","modification":"2026-04-08T09:47:06.718Z","creation":"2025-04-06T09:25:29.855Z"},"accession":"S-EPMC9370530","cross_references":{"pubmed":["35956997"],"doi":["10.3390/molecules27155047"]}}