Synthesis, QSAR Study and Antitumor Activity of Desmosdumotin-C Analogues / 中国药学杂志
Chinese Pharmaceutical Journal
;
(24): 1387-1392, 2017.
Article
in Chinese
| WPRIM
| ID: wpr-858603
ABSTRACT
OBJECTIVE:
To further design and synthesize Desmosdumotin-C(Des-C) derivatives and investigate their antitumor activities.METHODS:
QSAR study using the CoMFA method was performed on a set of reported Des-C derivatives to facilitate the elucidation of their SAR and discovery of new potent Des-C derivatives. Flow cytometry was used to investigate antitumor activity.RESULTS:
The established model showed good predictive ability and aid in the design of potent Des-C derivatives. An efficient three-step synthetic strategy toward Des-C derivatives was developed and applied to synthesize 10 new derivatives which showed superior antitumor activities against A549 and HL60 cells in vitro.CONCLUSION:
The structural modification of Des-C would significantly increase the antitumor activity. It is preliminarily confirmed that the derivatives are potent antitumor agents with apoptosis-inducing ability, which provides the basis for the further study.
Full text:
Available
Index:
WPRIM (Western Pacific)
Type of study:
Prognostic study
Language:
Chinese
Journal:
Chinese Pharmaceutical Journal
Year:
2017
Type:
Article
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