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Synthesis and evaluation of novel 7H-pyrrolo-[2,3-d]pyrimidine derivatives as potential anticancer agents

Yi-Min Liu1, Chun-Han Chen2, Teng-Kuang Yeh3

  • 1TMU Biomedical Commercialization Center, Taipei Medical University,  Taipei, Taiwan.

Future Medicinal Chemistry
|February 22, 2019
PubMed

Insights

A novel compound, 13i, shows potent anticancer activity against bladder cancer by inhibiting CK1δ. This FGFR3 inhibitor derivative offers a promising new avenue for developing targeted bladder cancer therapies.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Bladder cancer is a prevalent malignancy with limited therapeutic options.
  • Previous research identified compound 11 as a FGFR3 inhibitor with anti-bladder cancer effects.

Purpose of the Study:

  • To synthesize and evaluate novel 7H-pyrrolo-[2,3-d]pyrimidine derivatives based on compound 11.
  • To identify new agents with enhanced anticancer activity against bladder cancer cells.

Main Methods:

  • Synthesis of a series of 7H-pyrrolo-[2,3-d]pyrimidine derivatives.
  • Anticancer activity evaluation against human RT-112 bladder cancer cells.
  • Inhibition assays for CK1δ and FGFR3 kinases.
  • Cell cycle analysis and apoptosis assays.

Main Results:

  • Compound 13i demonstrated the highest efficacy against RT-112 bladder cancer cells.
  • 13i selectively inhibited CK1δ kinase activity without impacting FGFR3.
  • 13i HCl formulation enhanced solubility and induced cell cycle arrest and apoptosis.
  • Significant effects were observed in CK1δ-overexpressed bladder and ovarian cancer cells.

Conclusions:

  • Compound 13i is a potent inhibitor of CK1δ with significant anticancer activity.
  • 13i represents a promising lead compound for the development of novel anticancer drugs.
  • Targeting CK1δ may offer a new strategy for treating bladder and ovarian cancers.
Keywords:
CK1δapoptosiscancer

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