Some of alkyl, dialkylaminoalkyl and saccharide derivatives of 6H- indolo[2,3-b]quinoline manifest a cytotoxic activity. A wider application of these compounds is limited because of their low water solubility. Attaching aminoacids and peptides to a drug can increase its solubility, selectivity, and bioavailability. A series of novel 6H- in dolo[2,3- b]quinoline derivatives, substituted at C-2 or C-9 with an aminoacid, was designed and synthesized. These compounds were evaluated in vitro for their cytotoxic activity against KB cells (human cervix carcinoma). Gly, His, Pro, and Ser derivatives revealed cytotoxic activity.
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