{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,29]],"date-time":"2026-04-29T05:04:21Z","timestamp":1777439061177,"version":"3.51.4"},"reference-count":22,"publisher":"Wiley","issue":"11","license":[{"start":{"date-parts":[[2009,10,23]],"date-time":"2009-10-23T00:00:00Z","timestamp":1256256000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2009,11]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>A series of 2\u2010fluoro <jats:italic>N<\/jats:italic><jats:sup>10<\/jats:sup>\u2010substituted acridone derivatives with varying alkyl side chain length with propyl, butyl substitution, and a tertiary amine group at the terminal end of the alkyl side chain were synthesized and screened against cancer cell lines SW 1573, SW 1573 2R 160 (P\u2010gp substrate) which are non\u2010small lung cancer cell lines, MCF\u20107, MCF\u20107\/MR (BCRP substrate) are breast cancer cell lines, 2008 WT, 2008MRP1, 2008MRP2, 2008MRP3 are ovarian cancer cell lines, and human embryo kidney cell lines like HEK293, HEK293 MRP4, and HEK293 MRP5i. The propyl\u2010series compounds showed lipophilicity in the range of 1.93 to 4.40 and the butyl series in the range of 2.37 to 4.78. The compounds <jats:bold>4<\/jats:bold>, <jats:bold>7<\/jats:bold>, and<jats:bold> 8<\/jats:bold> showed good cytotoxicity against the 60 human cancer cell line panel of the National Cancer Institute, USA. The compounds<jats:bold> 14<\/jats:bold> and<jats:bold> 15<\/jats:bold> showed a better cytotoxicity in most of the cancer cell lines compared to other compounds tested. The DNA\u2010binding properties of the compounds were evaluated based on their affinity or intercalation with CT\u2010DNA measured with absorption titration. The compound<jats:bold> 11<\/jats:bold> bearing planar tricyclic ring linked with a butyl methylpiperazino side chain showed the highest binding affinity with a binding constant (K<jats:sub>i<\/jats:sub>) of 10.38\u00d710 M<jats:sup>\u20131<\/jats:sup>. Evaluation of the compounds in cell lines with an overexpression of various multidrug resistance\u2010related protein (MRP), P\u2010glycoprotein (P\u2010gp), or Breast Cancer Resistance Protein (BCRP) showed that all compounds are not substrates for any of these transporters.<\/jats:p>","DOI":"10.1002\/ardp.200900046","type":"journal-article","created":{"date-parts":[[2009,10,23]],"date-time":"2009-10-23T15:54:19Z","timestamp":1256313259000},"page":"640-650","source":"Crossref","is-referenced-by-count":25,"title":["Synthesis of 2\u2010Fluoro <i>N<\/i><sup>10<\/sup>\u2010Substituted Acridones and Their Cytotoxicity Studies in Sensitive and Resistant Cancer Cell Lines and Their DNA Intercalation Studies"],"prefix":"10.1002","volume":"342","author":[{"given":"Yergeri C.","family":"Mayur","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"family":"Zaheeruddin","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Godefridus J.","family":"Peters","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Clara","family":"Lemos","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ietje","family":"Kathmann","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Velivela V. 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