Reactions of indolo[2,3- a ]furano[3,4- c ]carbazole-5,7-diones with hydrazine hydrate, hydroxylamine hydrochloride, and formyl hydrazine produced the corresponding N -6-substituted indolopyrrolocarbazole glycosides with the carbohydrate residues L-arabinose, D-galactose, D-xylose, and D-ribose. The obtained compounds were studied in vitro and in vivo and showed significant antiproliferative activity against HCT-116 cells (IC 50 = 10 –6 – 10 –7 M) and high antitumor effects on Ehrlich ascites tumor and P-388 lymphocytic leukemia models. The lifespan increase of animals in the first model ranged from 540 – 495% to 172 – 132%; in the second model, from 80 – 83% to 120 – 93%.
New somatostatin analogs containing the fragments of adamantane, coumarin, tetrahydrocarbazole, and palmitic acid of the general formula R-Phe-D-Trp-Lys(Boc)-Thr-OMe have been synthesized. The structure of the conjugates combines a peptide fragment, which has affinity for somatostatin receptors (sstr), and a nonpeptide fragment, which potentially possesses antitumor activity. Presumably, the compounds synthesized are the agonists of sstr. The amide bond between the peptide and nonpeptide fragments has been formed using the carbodiimide method and the method of activated esters. The structures of the conjugates have been confirmed by mass spectrometry (ESI + ) and 1 H NMR spectroscopy. The antitumor activity of the conjugates has been examined by the MTT test on human lung adenocarcinoma (A549), human prostate adenocarcinoma (PC3), human colon cancer (HCT-116), human breast cancer (MCF7), and acute human T‑cell leukemia (Jurkat) cell lines. Compounds selectively inhibiting the growth of A549 cells have been identified.