Design, synthesis and structure-activity relationships of mangostin analogs as cytotoxic agents.
RSC Adv
; 8(72): 41377-41388, 2018 Dec 07.
Article
in En
| MEDLINE
| ID: mdl-35559306
ABSTRACT
In order to better understand the structure-activity relationship of mangostin, a series of xanthone derivatives based on α-mangostin were designed and synthesized. All the compounds were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Most of them showed cytotoxicity and most of all, compounds 1a and 2h showed the highest cytotoxic potency by HL-60 cancer cell lines with IC50 values of 5.96 µM and 6.90 µM respectively; compound 3e showed the highest cytotoxic potency against SMMC-7221 cancer cell line with IC50 values of 3.98 µM; compounds 2e and 2m showed lower cytotoxicity but higher selectivity than α-mangostin against HL-60 and SMMC-7221 cancer cell lines respectively. Structure-activity relationship analysis indicates that the maintenance of the isopentene group at C-8 is essential for the cytotoxic activity.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Language:
En
Journal:
RSC Adv
Year:
2018
Document type:
Article