Synthesis and evaluation of the diarylthiourea analogs as novel anti-cancer agents

Shengquan Liu1, Maggie C Louie2, Vanishree Rajagopalan1

  • 1College of Pharmacy, Touro University-California, Vallejo, CA 94592, USA.

Insights

Ten novel p-nitrodiarylthiourea compounds were synthesized and tested against breast and prostate cancer cells. Compound 7 demonstrated significant anticancer activity, showing potency comparable to SHetA2.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Pharmacology

Background:

  • Breast and prostate cancers represent significant global health challenges.
  • Developing novel therapeutic agents is crucial for improving patient outcomes.
  • Diarylthiourea derivatives have shown promise as anticancer agents.

Purpose of the Study:

  • To design and synthesize novel p-nitrodiarylthiourea analogs.
  • To evaluate the in vitro anticancer activities of these compounds against human breast and prostate cancer cell lines.
  • To identify lead compounds with potent cytotoxic effects.

Main Methods:

  • Synthesis of ten p-nitrodiarylthiourea analogs.
  • In vitro evaluation of anticancer activity using breast cancer cell lines (MCF-7, T-47D, MDA-MB-453) and prostate cancer cell lines (DU-145, PC-3, LNCaP).
  • Determination of GI50 values to quantify compound potency.

Main Results:

  • The majority of synthesized compounds exhibited anticancer activity at low micromolar concentrations.
  • Compound 7 emerged as the most potent analog in the series.
  • Compound 7 displayed GI50 values of 3.16μM (MCF-7), 2.53μM (T-47D), 4.77μM (MDA-MB-453), and 3.54μM (LNCaP).
  • The observed potency of Compound 7 was comparable to the parent compound, SHetA2.

Conclusions:

  • The synthesized p-nitrodiarylthiourea analogs possess significant anticancer potential.
  • Compound 7 is a promising candidate for further investigation as an anticancer therapeutic.
  • This study contributes to the development of novel anticancer agents targeting breast and prostate cancers.

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