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Ultima descărcare din IBN: 2023-09-21 11:08 |
Căutarea după subiecte similare conform CZU |
547:577.1 (6) |
Organic chemistry (489) |
Material bases of life. Biochemistry. Molecular biology. Biophysics (670) |
SM ISO690:2012 GÎRBU, Vladilena, PRUTEANU, Elena, UNGUR, Nikon, PERSOONS, Leentje, DAELEMANS, Dirk, RENAUD, Philippe, KULCIŢKI, Veaceslav. New cytotoxic ent-kauranes with unprecedented pharmacophores. In: New frontiers in natural product chemistry.: A destiny on the altar of research. Dedicated to academician Pavel Vlad, Ed. 6, 21 mai 2021, Chișinău. Chișinău, Republica Moldova: Tipografia "Artpoligraf", 2021, Ediția 6, p. 26. ISBN 978-9975-3336-7-2. DOI: https://doi.org/10.19261/nfnpc.2021.ab19 |
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New frontiers in natural product chemistry. Ediția 6, 2021 |
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Conferința " New frontiers in natural product chemistry." 6, Chișinău, Moldova, 21 mai 2021 | |||||||
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DOI:https://doi.org/10.19261/nfnpc.2021.ab19 | |||||||
CZU: 547:577.1 | |||||||
Pag. 26-26 | |||||||
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The cytotoxicity of ent-kauranic derivatives functionalized with azide, lactam and pyrrolidine fragments has been demonstrated. The inverstigated compounds showed relevant activity against Capan-1 (pancreatic adenocarcinoma), Hap-1 (chronic myeloid leukemia), HCT-116 (colorectal carcinoma), NCI-H460 (lung carcinoma), DND-41 (acute lymphoblastic leukemia), HL-60 (acute myeloid leukemia), K-562 (chronic myeloid leukemia), and Z-138 (non-Hodgkin lymphoma) cancer cell lines. The selectivity index was demonstrated by higher IC50 values in normal retina cells (hTERT RPE-1). The ent-kauranic azides 1 and 2 have been synthesized by radical carboazidation reactions using two different methods: first with hexabutylditin as radical transfer reagent and di-tert-butyl hyponitrite (DTBHN) as radical initiator and the second with triethylborane in the presence of air [1, 2]. Compounds 1 and 2 were converted to lactams 3 and 4, the lactam 3 was reduced to pyrrolidine 5. Figure 1 Compounds 1 - 5 presented in Figure 1 are air- and moisture stable, soluble in DMSO and other organic solvents. |
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