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Design and synthesis of novel 7-[(N-substituted-thioureidopiperazinyl)-methyl]-camptothecin derivatives as potential cytotoxic agents.
- Source :
- Natural Product Research; Jul2020, Vol. 34 Issue 14, p2022-2029, 8p
- Publication Year :
- 2020
-
Abstract
- As part of continuing our research on diverse C-7 derivatives of camptothecin (CPT), 16 CPT derivatives bearing piperazinyl-thiourea chemical scaffold and different substituent groups have been designed, synthesized and evaluated in vitro for cytotoxicity against five tumor cell lines (A-549, MDA-MB-231, MCF-7, KB and KBvin). As a result, all the synthesized compounds showed promising in vitro cytotoxic activity against the five tumor cell lines tested, and were more potent than irinotecan. Importantly, compounds 13 g (IC<subscript>50</subscript> = 0.514 μM) and 13o (IC<subscript>50</subscript> = 0.275 μM) possessed similar or better antiproliferative activity against the multidrug-resistant (MDR) KBvin subline than that of topotecan (IC<subscript>50</subscript> = 0.511 μM) and merit further development as anticancer candidates for clinical trail. With these results in hand, we have a reason to conclude that incorporating piperazinyl-thiourea motifs into position-7 of camptothecin confers well cytotoxic activity against cancer cell lines, probably resulting in new anticancer drugs. [ABSTRACT FROM AUTHOR]
- Subjects :
- THIOUREA
CAMPTOTHECIN
CELL lines
ANTINEOPLASTIC agents
CANCER cells
Subjects
Details
- Language :
- English
- ISSN :
- 14786419
- Volume :
- 34
- Issue :
- 14
- Database :
- Complementary Index
- Journal :
- Natural Product Research
- Publication Type :
- Academic Journal
- Accession number :
- 144476615
- Full Text :
- https://doi.org/10.1080/14786419.2019.1573231