Synthesis and anticancer activity of (E)-2-benzothiazole hydrazones

Eric B Lindgren; Monique A de Brito; Thatyana R A Vasconcelos; Manuel O de Moraes; Raquel C Montenegro; Julliane D Yoneda; Kátia Z Leal

doi:10.1016/j.ejmech.2014.08.039

Synthesis and anticancer activity of (E)-2-benzothiazole hydrazones

Eur J Med Chem. 2014 Oct 30:86:12-6. doi: 10.1016/j.ejmech.2014.08.039. Epub 2014 Aug 11.

Authors

Eric B Lindgren¹, Monique A de Brito², Thatyana R A Vasconcelos¹, Manuel O de Moraes³, Raquel C Montenegro⁴, Julliane D Yoneda⁵, Kátia Z Leal⁶

Affiliations

¹ Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal Fluminense, Outeiro de São João Batista s/n°, 24020-141 Niterói, RJ, Brazil.
² Faculdade de Farmácia, Universidade Federal Fluminense, Rua Mário Viana 523, 24241-000 Niterói, RJ, Brazil.
³ Laboratório de Oncologia Experimental, Universidade Federal do Ceará, Rua Coronel Nunes de Melo 1127, 60430-270 Fortaleza, CE, Brazil.
⁴ Laboratório de Citogenética Humana, Instituto de Ciências Biológicas, Universidade Federal do Pará, Rua Augusto Corrêa 01, 66075-110 Belém, PA, Brazil.
⁵ Departamento de Química, Instituto de Ciências Exatas, Universidade Federal Fluminense, Rua Des. Ellis Hermydio Figueira 783, 27213-415, Volta Redonda, RJ, Brazil. Electronic address: jullianeyoneda@id.uff.br.
⁶ Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal Fluminense, Outeiro de São João Batista s/n°, 24020-141 Niterói, RJ, Brazil. Electronic address: kzleal@gmail.com.

PMID: 25147145
DOI: 10.1016/j.ejmech.2014.08.039

Abstract

Benzothiazole hydrazones have been synthesized and evaluated for their in vitro antiproliferative activity against three human cancer cell lines: HL-60 (leukemia), MDAMB-435 (breast) and HCT-8 (colon). The good cytotoxicity for the three cancer cell lines and theoretical profile of compounds 3o and 3p pointed them as promising lead molecules for anticancer drug design.

Keywords: (E)-2-benzothiazoles; Anticancer; Hydrazones; Lipinski's rule of five.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Benzothiazoles / chemical synthesis
Benzothiazoles / chemistry
Benzothiazoles / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Design
Drug Screening Assays, Antitumor
HL-60 Cells
Humans
Hydrazines / chemical synthesis
Hydrazines / chemistry
Hydrazines / pharmacology*
Molecular Structure
Structure-Activity Relationship

Substances

Antineoplastic Agents
Benzothiazoles
Hydrazines