Combined 3D-QSAR and Docking Modelling Study on Indolocarbazole Series Compounds as Tie-2 Inhibitors
2011

3D-QSAR and Docking Study of Indolocarbazole Compounds as Tie-2 Inhibitors

Sample size: 80 publication Evidence: high

Author Information

Author(s): Tian Yuanxin, Xu Jian, Zhonghuang Zhu, Zhengguang Zhang, Jiajie Wu Shuguang

Primary Institution: Southern Medical University

Hypothesis

To investigate the structure-activity correlation of indolocarbazole series compounds and modify them to improve their selectivity and activity.

Conclusion

The study successfully constructed predictive 3D-QSAR models and elucidated the binding modes of indolocarbazole compounds with Tie-2, providing insights for designing new inhibitors.

Supporting Evidence

  • The CoMFA model had a high cross-validated square correlation coefficient q2 of 0.823.
  • The CoMSIA model also showed good predictability with a q2 value of 0.804.
  • Both models provided insights into the structure-activity relationship of the compounds.

Takeaway

Scientists studied some special compounds to see how they work against cancer and found ways to make them even better.

Methodology

3D-QSAR models were built using CoMFA and CoMSIA methods, and molecular docking was performed to confirm the results.

Limitations

The study could not obtain 3D-QSAR models for some compounds that were potent against VEGFR2.

Statistical Information

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.3390/ijms12085080

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