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We thank Dr. Gergo Toth for chiral HPLC separation and spectra.\nDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre street 9, Budapest, H-1092, Hungary \n Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, 29-39 Brunswick Square, London, WC1N 1AX, United Kingdom \n Department of Pharmacognosy, Semmelweis University, Üllői street 26, Budapest, H-1085, Hungary \n Vichem Chemie Ltd, Herman Ottó street 15, Budapest, H-1022, Hungary \n Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, Universiteitsweg 99, Utrecht, CG 3584, Netherlands \n Cited By :4 \n Export Date: 7 September 2021 \n CODEN: BMCLE \n Correspondence Address: Őrfi, L.; Department of Pharmaceutical Chemistry, Hőgyes Endre street 9, Hungary; email: orfi.laszlo@pharma.semmelweis-univ.hu\nDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre street 9, Budapest, H-1092, Hungary \n Department of 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Sunitinib, a multikinase inhibitor, was the first Fms-like tyrosine kinase 3 (FLT3) inhibitor clinically used against AML. Off-target effects are a major concern for multikinase inhibitors. As targeted delivery may reduce such undesired side effects, our goal was to develop novel amino acid substituted derivatives of sunitinib which are potent candidates to be used conjugated with antibodies and peptides. In the current paper we present the synthesis, physicochemical and in vitro characterization of sixty two Fms-like tyrosine kinase 3-internal tandem duplication (FLT3-ITD) mutant kinase inhibitors, bearing amino acid moieties, fit to be conjugated with peptide-based delivery systems via their carboxyl group. We determined the solubility, pKa, CHI and LogP values of the compounds along with their inhibition potential against FLT3-ITD mutant kinase and on MV4-11 cell line. 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