{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,2]],"date-time":"2026-05-02T04:25:04Z","timestamp":1777695904212,"version":"3.51.4"},"reference-count":28,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2022,12,21]],"date-time":"2022-12-21T00:00:00Z","timestamp":1671580800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"National Natural Science Foundation of China","award":["22067001"],"award-info":[{"award-number":["22067001"]}]},{"name":"National Natural Science Foundation of China","award":["2022B005"],"award-info":[{"award-number":["2022B005"]}]},{"name":"Inheritance and innovation team of Guangxi Traditional Chinese Medicine","award":["22067001"],"award-info":[{"award-number":["22067001"]}]},{"name":"Inheritance and innovation team of Guangxi Traditional Chinese Medicine","award":["2022B005"],"award-info":[{"award-number":["2022B005"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>We report herein the design and synthesis of a series of novel acridine-triazole and acridine-thiadiazole derivatives. The newly synthesized compounds and the key intermediates were all evaluated for their antitumor activities against human foreskin fibroblasts (HFF), human gastric cancer cells-803 (MGC-803), hepatocellular carcinoma bel-7404 (BEL-7404), large cell lung cancer cells (NCI-H460), and bladder cancer cells (T24). Most of the compounds exhibited high levels of antitumor activity against MGC-803 and T24 but low toxicity against human normal liver cells (LO2), and their effect was even better than the commercial anticancer drugs, 5-fluorouracil (5-FU) and cis-platinum. Further, pharmacological mechanisms such as topo I, cell cycle, cell apoptosis, and neovascularization were all evaluated. Only a few compounds exhibited potent topo I inhibitory activity at 100 \u03bcM. In addition, the most active compounds with an IC50 value of 5.52\u20138.93 \u03bcM were chosen, and they could induce cell apoptosis in the G2 stage of MGC-803 or mainly arrest T24 cells in the S stage. To our delight, most of the compounds exhibited lower zebrafish cytotoxicity but could strongly inhibit the formation of zebrafish sub-intestinal veins, indicating a potential for clinical application.<\/jats:p>","DOI":"10.3390\/ijms24010064","type":"journal-article","created":{"date-parts":[[2022,12,21]],"date-time":"2022-12-21T03:31:06Z","timestamp":1671593466000},"page":"64","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Design and Synthesis of Acridine-Triazole and Acridine-Thiadiazole Derivatives and Their Inhibitory Effect against Cancer Cells"],"prefix":"10.3390","volume":"24","author":[{"given":"Lini","family":"Huo","sequence":"first","affiliation":[{"name":"College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiaochen","family":"Liu","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yogini","family":"Jaiswal","sequence":"additional","affiliation":[{"name":"Center for Excellence in Post-Harvest Technologies, North Carolina Agricultural and Technical State University, The North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC 28081, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hao","family":"Xu","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rui","family":"Chen","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rumei","family":"Lu","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yaqin","family":"Nong","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0886-5204","authenticated-orcid":false,"given":"Leonard","family":"Williams","sequence":"additional","affiliation":[{"name":"Center for Excellence in Post-Harvest Technologies, North Carolina Agricultural and Technical State University, The North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC 28081, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yan","family":"Liang","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Guangxi Medical University, Nanning 530021, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zhiruo","family":"Jia","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,12,21]]},"reference":[{"key":"ref_1","first-page":"3080","article-title":"Progress in the study of the mechanism of action of anti-tumor drugs","volume":"30","author":"Cheng","year":"2009","journal-title":"Jilin Med."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"2293","DOI":"10.1016\/j.bmcl.2007.01.056","article-title":"Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents","volume":"17","author":"Martins","year":"2007","journal-title":"Bioorg. 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