{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Jiang B"],"funding":["National Natural Science Foundation of China","Undergraduate Student Innovation and Practice Incubation Base Project of Naval Medical University"],"pagination":["161"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC12844652"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["19(1)"],"pubmed_abstract":["<b>Background/Objectives:</b> Cancer persists as a leading concern in the current medical field, and current therapies are limited by toxicity, cost, and resistance. Targeted inhibition of tubulin polymerization is considered as a promising therapeutic strategy for cancer treatment. <b>Methods</b>: Thirty-one new tubulin polymerization inhibitors were designed via molecular hybridization techniques, and BLI technology was employed to quantitatively investigate their interactions with tubulin. Antiproliferative activities against MCF-7, MDA-MB-231, A549, and HeLa cell lines was evaluated using the CCK8 assay. Apoptosis induction and cell cycle arrest were analyzed by flow cytometry. The anti-tumor activity of compound <b>B6</b> was validated in a mouse melanoma tumor model. <b>Results</b>: Compounds exhibited varying degrees of antiproliferative activity against four tumor cell lines. Among them, compound <b>B6</b> was the most promising candidate and displayed strong broad-spectrum anticancer activity with an average IC<sub>50</sub> value of 2 μM. The mechanism studies revealed that compound <b>B6</b> inhibited tubulin polymerization in vitro, disrupted cell microtubule networks, and arrested the cell cycle at G2/M phase. Furthermore, <b>B6</b> displayed significant in vivo antitumor efficacy in a melanoma tumor model with tumor growth inhibition rates of 70.21% (50 mg/kg). <b>Conclusions</b>: This work shows that <b>B6</b> is a promising lead compound deserving further investigation as a potential anticancer agent."],"journal":["Pharmaceuticals (Basel, Switzerland)"],"pubmed_title":["Discovery of New Quinazolinone and Benzimidazole Analogs as Tubulin Polymerization Inhibitors with Potent Anticancer Activities."],"pmcid":["PMC12844652"],"funding_grant_id":["FH2024166","NO. 82204347, 82473778"],"pubmed_authors":["Zou Y","Gai C","Zhang J","Meng Q","Xu B","Zhao Q","Shao K","Jiang B","Chai X","Song Y"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of New Quinazolinone and Benzimidazole Analogs as Tubulin Polymerization Inhibitors with Potent Anticancer Activities.","description":"<b>Background/Objectives:</b> Cancer persists as a leading concern in the current medical field, and current therapies are limited by toxicity, cost, and resistance. Targeted inhibition of tubulin polymerization is considered as a promising therapeutic strategy for cancer treatment. <b>Methods</b>: Thirty-one new tubulin polymerization inhibitors were designed via molecular hybridization techniques, and BLI technology was employed to quantitatively investigate their interactions with tubulin. Antiproliferative activities against MCF-7, MDA-MB-231, A549, and HeLa cell lines was evaluated using the CCK8 assay. Apoptosis induction and cell cycle arrest were analyzed by flow cytometry. The anti-tumor activity of compound <b>B6</b> was validated in a mouse melanoma tumor model. <b>Results</b>: Compounds exhibited varying degrees of antiproliferative activity against four tumor cell lines. Among them, compound <b>B6</b> was the most promising candidate and displayed strong broad-spectrum anticancer activity with an average IC<sub>50</sub> value of 2 μM. The mechanism studies revealed that compound <b>B6</b> inhibited tubulin polymerization in vitro, disrupted cell microtubule networks, and arrested the cell cycle at G2/M phase. Furthermore, <b>B6</b> displayed significant in vivo antitumor efficacy in a melanoma tumor model with tumor growth inhibition rates of 70.21% (50 mg/kg). <b>Conclusions</b>: This work shows that <b>B6</b> is a promising lead compound deserving further investigation as a potential anticancer agent.","dates":{"release":"2026-01-01T00:00:00Z","publication":"2026 Jan","modification":"2026-06-15T03:15:14.179Z","creation":"2026-06-15T03:08:48.267Z"},"accession":"S-EPMC12844652","cross_references":{"pubmed":["41599758"],"doi":["10.3390/ph19010161"]}}