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The basicity of aromatic amines is much weaker than that of aliphatic amines due to the involvement of the lone pair of electrons over the N atom in resonance with the aryl rings. Generally, the electron-donating ability of any substituents on the aryl ring of aromatic amines increases the basicity of the amine by increasing electron density, and hence the availability of lone pair on the nitrogen. On the other hand, electron-withdrawing functional groups on the aryl ring of amines decrease the...
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Structural Basis for BD1-Preferring 2,4-Disubstituted Pyrimidine BRDT Inhibitors.

Taimeng Liang1, Xianghong Guan2, Alice Chan3

  • 1Department of Chemistry, University of Minnesota, 207 Pleasant Street, SE, Minneapolis, Minnesota 55455-0431, United States.

Journal of Medicinal Chemistry
|April 15, 2026
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Summary
This summary is machine-generated.

Researchers developed novel BET/kinase inhibitor analogs to target BRDT-BD1 for male contraception. Compound 13 demonstrated high selectivity and metabolic stability, marking progress in developing targeted BRDT inhibitors.

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Area of Science:

  • Medicinal Chemistry
  • Structural Biology
  • Pharmacology

Background:

  • The first bromodomain of BRDT (BRDT-BD1) has a unique Arg54 residue.
  • BET/kinase inhibitors like SG3-179 are potential therapeutic agents.

Purpose of the Study:

  • To explore the structural uniqueness of BRDT-BD1.
  • To design and synthesize analogs of SG3-179 for selective BRDT inhibition.
  • To identify potential male contraceptive agents.

Main Methods:

  • Synthesis of 23 analogs of SG3-179.
  • AlphaScreen assay for selectivity profiling.
  • Co-crystallization of BRDT-BD1 with analog 14.
  • In vitro metabolic stability and cellular permeability assays.

Main Results:

  • Serine analog 13 showed 35-fold selectivity for BRDT-T over BRD4-T.
  • Co-crystal structure revealed no direct interaction of analog 14 with Arg54.
  • Compound 13 exhibited excellent in vitro metabolic stability but poor cellular permeability.
  • Compounds 13 and 14 are highly selective BRDT-BD1 inhibitors.

Conclusions:

  • Selective BRDT-BD1 inhibitors were identified.
  • The unique Arg54 residue's role in selectivity requires further investigation.
  • Compounds 13 and 14 represent significant advancements toward developing BRDT inhibitors for male contraception.