SAR study on thiolato-bridged triosmium carbonyl clusters: higher reactivity does not equal higher antiproliferative activity
A structure-activity relationship study on triosmium clusters of the general formula Os3(μ-H)(μ-SC6H4X)(CO)10 (2-X, where X = o-, m- or p-NH2; o-, m- or p- OH; p-H, -Br, -NO2, -COOH or -CH2COOH) show that their antiproliferative activity is through the cluster core, and the nature and position of th...
Saved in:
| Main Authors: | , |
|---|---|
| Other Authors: | |
| Format: | Article |
| Language: | English |
| Published: |
2025
|
| Subjects: | |
| Online Access: | https://hdl.handle.net/10356/182219 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| Institution: | Nanyang Technological University |
| Language: | English |
| Summary: | A structure-activity relationship study on triosmium clusters of the general formula Os3(μ-H)(μ-SC6H4X)(CO)10 (2-X, where X = o-, m- or p-NH2; o-, m- or p- OH; p-H, -Br, -NO2, -COOH or -CH2COOH) show that their antiproliferative activity is through the cluster core, and the nature and position of the phenyl ring substituent X shows a significant impact on the activity. Clusters with an electron-withdrawing group are more reactive but are thus quickly consumed through reaction with serum, while those with an electron-donating group persists sufficiently to enter the cells and result in higher antiproliferative activity. Interestingly, m-substituted clusters and those with lipophilicity >6.0 also exhibit higher antiproliferative activity. In contrast, o-substituted clusters capable of intramolecular hydrogen bonding have lower cytotoxicity. The cluster 2-m-OH, with higher antiproliferative activity and lower reactivity with serum, is a potential lead compound for further mode of action studies. |
|---|