{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,3]],"date-time":"2025-11-03T13:44:53Z","timestamp":1762177493671,"version":"build-2065373602"},"reference-count":23,"publisher":"MDPI AG","issue":"6","license":[{"start":{"date-parts":[[2022,6,8]],"date-time":"2022-06-08T00:00:00Z","timestamp":1654646400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Maunders McNeil Foundation Inc."}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Medicines"],"abstract":"<jats:p>A series of 3,5-bis(benzylidene)-1-dichloroacetyl-4-piperidones 1a\u2013l was evaluated against Ca9-22, HSC-2, HSC-3, and HSC-4 squamous cell carcinomas. Virtually all of the compounds displayed potent cytotoxicity, with 83% of the CC50 values being submicromolar and several CC50 values being in the double digit nanomolar range. The compounds were appreciably less toxic to human HGF, HPLF, and HPC non-malignant cells, which led to some noteworthy selectivity index (SI) figures. From these studies, 1d,g,k emerged as the lead molecules in terms of their potencies and SI values. A Quantitative Structure-Activity Relationship (QSAR) study revealed that cytotoxic potencies and potency\u2013selectivity expression figures increased when the magnitude of the sigma values in the aryl rings was elevated. The modes of action of the representative cytotoxins in Ca9-22 cells were found to include G2\/M arrest and stimulation of the cells to undergo mitosis and cause poly(ADP-ribose) polymerase (PARP) and procaspase 3 cleavage.<\/jats:p>","DOI":"10.3390\/medicines9060035","type":"journal-article","created":{"date-parts":[[2022,6,12]],"date-time":"2022-06-12T22:37:20Z","timestamp":1655073440000},"page":"35","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["Dichloroacetyl Amides of 3,5-Bis(benzylidene)-4-piperidones Displaying Greater Toxicity to Neoplasms than to Non-Malignant Cells"],"prefix":"10.3390","volume":"9","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-9953-586X","authenticated-orcid":false,"given":"Mohammad","family":"Hossain","sequence":"first","affiliation":[{"name":"School of Sciences, Indiana University Kokomo, Kokomo, IN 46904, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3712-5790","authenticated-orcid":false,"given":"Praveen K.","family":"Roayapalley","sequence":"additional","affiliation":[{"name":"Drug Discovery and Development Research Cluster, University of Saskatchewan, Saskatoon, SK S7N 5E5, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8001-2121","authenticated-orcid":false,"given":"Hiroshi","family":"Sakagami","sequence":"additional","affiliation":[{"name":"Meikai University School of Dentistry, Sakado 350-0283, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Keitaro","family":"Satoh","sequence":"additional","affiliation":[{"name":"Meikai University School of Dentistry, Sakado 350-0283, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1362-3034","authenticated-orcid":false,"given":"Kenjiro","family":"Bandow","sequence":"additional","affiliation":[{"name":"Meikai University School of Dentistry, Sakado 350-0283, Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Umashankar","family":"Das","sequence":"additional","affiliation":[{"name":"Drug Discovery and Development Research Cluster, University of Saskatchewan, Saskatoon, SK S7N 5E5, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jonathan R.","family":"Dimmock","sequence":"additional","affiliation":[{"name":"Drug Discovery and Development Research Cluster, University of Saskatchewan, Saskatoon, SK S7N 5E5, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,6,8]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1694","DOI":"10.2174\/1568026619666190619115735","article-title":"Molecular hybridization as a tool for designing multitarget candidates for complex diseases","volume":"19","author":"Ivasiv","year":"2019","journal-title":"Curr. 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