| Title |
Design, synthesis, and antitumor evaluation of histone deacetylase inhibitors with L-phenylglycine scaffold
|
|---|---|
| Published in |
Drug Design, Development and Therapy, October 2015
|
| DOI | 10.2147/dddt.s94037 |
| Pubmed ID | |
| Authors |
Yingjie Zhang, Xiaoguang Li, Jinning Hou, Yongxue Huang, Wenfang Xu |
| Abstract |
In our previous research, a novel series of histone deacetylase (HDAC) inhibitors with l-phenylglycine scaffold were designed and synthesized, among which amides D3 and D7 and ureido D18 were far superior to the positive control (suberoylanilide hydroxamic acid [SAHA]) in HDAC inhibition, but were only comparable to SAHA in antiproliferation on tumor cell lines. Herein, further structural derivation of lead compounds D3, D7, and D18 was carried out to improve their cellular activities. Most of our newly synthesized compounds exhibited more potent HDAC inhibitory activities than the positive control SAHA, and several derivatives were even better than their parent compounds. However, compared with SAHA and our lead compounds, only secondary amine series compounds exhibited improved antiproliferative activities, likely due to their appropriate topological polar surface area values and cell permeabilities. In a human histiocytic lymphoma (U937) xenograft model, the most potent secondary amine 9d exhibited similar in vivo antitumor activity to that of SAHA. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| India | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Scientists | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 12 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 12 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 2 | 17% |
| Student > Doctoral Student | 1 | 8% |
| Lecturer | 1 | 8% |
| Student > Master | 1 | 8% |
| Professor > Associate Professor | 1 | 8% |
| Other | 0 | 0% |
| Unknown | 6 | 50% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 4 | 33% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 17% |
| Unknown | 6 | 50% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 10 October 2015.
All research outputs
#20,656,161
of 25,374,647 outputs
Outputs from Drug Design, Development and Therapy
#1,437
of 2,268 outputs
Outputs of similar age
#210,058
of 286,876 outputs
Outputs of similar age from Drug Design, Development and Therapy
#71
of 110 outputs
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