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Silicon-Containing Building Blocks for Drug Design

Silicon-containing compounds have been largely ignored in drug design until recently. Silicon can be considered a bioisostere of carbon and hence offers an innovative avenue in drug discovery. For example, C/Si exchange in drug-like scaffolds provides an exciting approach in medicinal chemistry to improve ADME/Tox profile and to enhance potency of the biologically active compounds. Herein we have designed and synthesized a library of silicon-containing building blocks for drug design.

Design

Advantages of “Silicon Switch”:

  • Larger C−Si bond length (C–C = 1.54 Å, C–Si = 1.87 Å) → changes in the interactions with specific proteins.
  • Increase in lipophilicity → improved cell penetration and selectivity.
  • Difference in bonding preferences: Si prefers higher coordination numbers → access to compounds for which corresponding carbon analogs are not available.

We offer

Over 15 unique silicon-containing building blocks on a 1-30 g scale from stock. We also have designed a library of silicon-containing building blocks for drug discovery programs. These molecules can be synthesized upon request within 4-6 weeks.

Compounds from Stock:

Feasible Compounds:

MedChem Highlights

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