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 (IC50 = 0.514 μM) and 13o (IC50 = 0.275 μM) possessed similar or better antiproliferative activity against the multidrug-resistant (MDR) KBvin subline than that of topotecan (IC50 = 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.
journal_name
Nat Prod Resjournal_title
Natural product researchauthors
Song ZL,Yang GZ,Li JC,Liu YQ,Yang CJ,Goto M,Zhang ZJ,Morris-Natschke SL,Liu H,Lee KHdoi
10.1080/14786419.2019.1573231subject
Has Abstractpub_date
2020-07-01 00:00:00pages
2022-2029issue
14eissn
1478-6419issn
1478-6427journal_volume
34pub_type
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