Publication:
Structural modification of the macrolide brefeldin a to analogues with enhanced cytotoxicity against KB cells

0
0

Issued Date

2021

Resource Type

Article

Language

eng

File Type

application/pdf

ISSN

27740226

DOI

10.48048/tis.2021.44

Other identifier(s)

2-s2.0-85121593308

Rights Holder(s)

มหาวิทยาลัยศรีนครินทรวิโรฒ

Bibliographic Citation

Trends in Sciences. Vol 18, No.21 (2021)

Suggested Citation

Namsa-Aid M., Wiyakrutta S., Prachya S., Namsa-Aid A., Suksamrarn A. 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://hdl.handle.net/20.500.14740/8133

Title

Structural modification of the macrolide brefeldin a to analogues with enhanced cytotoxicity against KB cells

Author(s)

Namsa-Aid M.
 Wiyakrutta S.
 Prachya S.
 Namsa-Aid A.
 Suksamrarn A.

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. © 2021, Walailak University. All rights reserved.

View online Resources

Research Projects

Organizational Units

Journal Issue

URI

https://hdl.handle.net/20.500.14740/8133

Collections

Scopus: Year 1983-2021

Endorsement

Review

Supplemented By

Referenced By