Publication: Structural modification of the macrolide brefeldin a to analogues with enhanced cytotoxicity against KB cells
Issued Date
2021-11-01
Resource Type
ISSN
27740226
Other identifier(s)
2-s2.0-85121593308
Rights
Mahidol University
Rights Holder(s)
SCOPUS
Bibliographic Citation
Trends in Sciences. Vol.18, No.21 (2021)
Suggested Citation
Maneekarn Namsa-Aid, Suthep Wiyakrutta, Surasak Prachya, Anucha Namsa-Aid, Apichart Suksamrarn Structural modification of the macrolide brefeldin a to analogues with enhanced cytotoxicity against KB cells. Trends in Sciences. Vol.18, No.21 (2021). doi:10.48048/tis.2021.44 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/79286
Research Projects
Organizational Units
Authors
Journal Issue
Thesis
Title
Structural modification of the macrolide brefeldin a to analogues with enhanced cytotoxicity against KB cells
Abstract
The macrolide brefeldin A (BFA, 1) exhibited high cytotoxicity against KB cells. However, it was also toxic against non-cancerous cells. In order to lower toxicity against normal cells while maintaining the cytotoxic potency to the cancer cells, structural modification of this compound was undertaken. Starting from compound 1, the analogues 2-13 were synthesized and evaluated for cytotoxicity against KB cells. The analogue 2 exhibited the most potent cytotoxicity against KB cells, with an IC50 value of 0.034 nM, 67-fold more active than its parent compound 1. It was 41764 and 8235 fold more active than the standard drugs ellipticine and doxorubicin, respectively. The higher cytotoxicity against KB cells and lower toxicity against Vero cells of analogue 2 than those of the parent compound 1 contributed to its exceptionally high selectivity index of 9117. The results suggested that this analogue might be utilized to develop a new candidate for an anticancer drug.