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The \u03b2-carboline moiety, present in several biologically active natural products and drugs, is an important scaffold for antimalarial drug discovery. The present study explores the antimalarial activity of a \u03b2-carboline derivative (1R,3S)-methyl 1-(benzo[d][1,3]dioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate (9a) alone in vitro against Plasmodium falciparum and in vivo in combination therapy with the standard drug artesunate against Plasmodium berghei. Compound 9a inhibited both 3D7 and RKL-9 strains of P. falciparum with half-maximal inhibitory concentration (IC50) &amp;lt; 1 \u03bcg\/mL, respectively. The compound was nontoxic (50% cytotoxic concentration (CC50) &amp;gt; 640 \u03bcg\/mL) to normal dermal fibroblasts. Selectivity index was &amp;gt;10 against both the strains. The compound exhibited considerable in vivo antimalarial activity (median effective dose (ED50) = 27.74 mg\/kg) in monotherapy. The combination of 9a (100 mg\/kg) and artesunate (50 mg\/kg) resulted in 99.69% chemosuppression on day 5 along with a mean survival time of 25.8 \u00b1 4.91 days with complete parasite clearance. Biochemical studies indicated the safety of the HIT compound to hepatic and renal functions of mice. Molecular docking also highlighted the suitability of 9a as a potential antimalarial candidate.<\/jats:p>","DOI":"10.1021\/acsomega.0c01256","type":"journal-article","created":{"date-parts":[[2020,7,13]],"date-time":"2020-07-13T16:41:12Z","timestamp":1594658472000},"page":"17993-18006","source":"Crossref","is-referenced-by-count":47,"title":["\u03b2-Carboline Derivatives Tackling Malaria:\nBiological Evaluation and Docking Analysis"],"prefix":"10.1021","volume":"5","author":[{"given":"Varun","family":"Gorki","sequence":"first","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Neha Sylvia","family":"Walter","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rahul","family":"Singh","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Monika","family":"Chauhan","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Neelima","family":"Dhingra","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1241-9146","authenticated-orcid":true,"given":"Deepak B.","family":"Salunke","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9071-7950","authenticated-orcid":true,"given":"Sukhbir","family":"Kaur","sequence":"additional","affiliation":[{"name":"Panjab University , , ,","place":["Chandigarh, India, 160014"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2020,7,13]]},"reference":[{"key":"2026090203092032800_cit1","doi-asserted-by":"publisher","first-page":"1527","DOI":"10.1007\/s12098-011-0554-2","article-title":"Malaria and National\nVector Borne Disease Control Programme","volume":"78","author":"Sharma","year":"2011","journal-title":"Indian\nJ. 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