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This reaction has proved to be a major driving force in many multicomponent reactions indicating the prolific utility toward the development of biologically fascinating molecules. This eminent reaction was acclimatised on different pharmacophoric aldehydes (benzimidazole, \u03b2\u2010carboline, phenanthrene, indole, imidazothiadiazole, pyrazole etc.) and active methylenes (oxindole, barbituric acid, Meldrum's acid, thiazolidinedione etc.) to generate the library of chemical compounds. Their potential was also explicit to understand the significance of functionalities involved, which thereby evoke further developments in drug discovery. Furthermore, most of these reaction products exhibited remarkable anticancer activity in nanomolar to micromolar ranges by targeting different cancer targets like DNA, microtubules, Topo\u2010I\/II, and kinases (PIM, PARP, NMP, p300\/CBP) etc. This review underscores the efficiency of the Knoevenagel condensation explored in the past six\u2010year to generate molecules of pharmacological interest, predominantly toward cancer. The present review also provides the aspects of structure\u2010activity relationships, mode of action and docking study with possible interaction with the target protein.<\/jats:p>","DOI":"10.1002\/cmdc.202100736","type":"journal-article","created":{"date-parts":[[2022,2,28]],"date-time":"2022-02-28T13:11:06Z","timestamp":1646053866000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":71,"title":["Contribution of Knoevenagel Condensation Products toward the Development of Anticancer Agents: An Updated Review"],"prefix":"10.1002","volume":"17","author":[{"given":"Ramya","family":"Tokala","sequence":"first","affiliation":[{"name":"Department of Medicinal Chemistry National Institution of Pharmaceutical Education and Research (NIPER)  Hyderabad 500037 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Darshana","family":"Bora","sequence":"additional","affiliation":[{"name":"Department of Medicinal Chemistry National Institution of Pharmaceutical Education and Research (NIPER)  Hyderabad 500037 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8733-9431","authenticated-orcid":false,"given":"Nagula","family":"Shankaraiah","sequence":"additional","affiliation":[{"name":"Department of Medicinal Chemistry National Institution of Pharmaceutical Education and Research (NIPER)  Hyderabad 500037 India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,3,15]]},"reference":[{"key":"e_1_2_6_1_1","doi-asserted-by":"publisher","DOI":"10.2174\/1389450116666150309115922"},{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00044-012-0133-8"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.2174\/156800911794328457"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1039\/C7MD00067G"},{"key":"e_1_2_6_5_1","doi-asserted-by":"publisher","DOI":"10.4155\/fmc.12.201"},{"key":"e_1_2_6_6_1","doi-asserted-by":"publisher","DOI":"10.2174\/1573412052953328"},{"key":"e_1_2_6_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.lfs.2022.120321"},{"key":"e_1_2_6_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molstruc.2021.132251"},{"key":"e_1_2_6_9_1","doi-asserted-by":"publisher","DOI":"10.1002\/med.21852"},{"key":"e_1_2_6_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.drudis.2021.05.015"},{"key":"e_1_2_6_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2021.113263"},{"key":"e_1_2_6_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2021.113334"},{"key":"e_1_2_6_13_1","doi-asserted-by":"publisher","DOI":"10.1039\/D0MD00422G"},{"key":"e_1_2_6_14_1","doi-asserted-by":"publisher","DOI":"10.13005\/ojc\/350154"},{"key":"e_1_2_6_15_1","unstructured":"https:\/\/www.organic-chemistry.org\/namedreactions\/knoevenagel-condensation.shtmaccessed on 21.\u200911.\u20092020."},{"key":"e_1_2_6_16_1","doi-asserted-by":"publisher","DOI":"10.1080\/00397911.2010.537423"},{"key":"e_1_2_6_17_1","doi-asserted-by":"publisher","DOI":"10.1246\/bcsj.61.2473"},{"key":"e_1_2_6_18_1","doi-asserted-by":"publisher","DOI":"10.3184\/030823409X12616597939085"},{"key":"e_1_2_6_19_1","doi-asserted-by":"publisher","DOI":"10.1080\/17518250903410074"},{"key":"e_1_2_6_20_1","doi-asserted-by":"publisher","DOI":"10.1080\/17518253.2020.1851398"},{"key":"e_1_2_6_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.mcat.2019.110744"},{"key":"e_1_2_6_22_1","doi-asserted-by":"publisher","DOI":"10.1021\/ed067pA304"},{"key":"e_1_2_6_23_1","first-page":"701","volume":"11","author":"Majid M. 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