Synthesis and antiproliferative activity in vitro of novel (2-butynyl)thioquinolines

W Mól; M Matyja; B Filip; J Wietrzyk; S Boryczka

doi:10.1016/j.bmc.2008.07.047

Synthesis and antiproliferative activity in vitro of novel (2-butynyl)thioquinolines

Bioorg Med Chem. 2008 Sep 1;16(17):8136-41. doi: 10.1016/j.bmc.2008.07.047. Epub 2008 Jul 23.

Authors

W Mól¹, M Matyja, B Filip, J Wietrzyk, S Boryczka

Affiliation

¹ Department of Organic Chemistry, The Medical University of Silesia, 41-200 Sosnowiec, PL, Poland.

PMID: 18682326
DOI: 10.1016/j.bmc.2008.07.047

Abstract

The series of new acetylenic thioquinolines containing propargyl, 2-butynyl, 4-bromo-2-butynyl, and 4-hydroxy-2-butynyl groups has been prepared and tested for antiproliferative activity in vitro against human [SW707 (colorectal adenocarcinoma), CCRF/CEM (leukemia)] and murine [P388 (leukemia), B16 (melanoma)] cancer lines. All the compounds obtained exhibited antiproliferative activity. The most active compounds 7, 16, 17, and 19 have the ID(50) values ranging from 0.2 to 4.6 microg/ml comparable to that of cisplatin used as reference compounds.

Publication types

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

MeSH terms

Adenocarcinoma / drug therapy*
Animals
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Colorectal Neoplasms / drug therapy*
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Leukemia, Experimental / drug therapy*
Melanoma, Experimental / drug therapy*
Mice
Molecular Structure
Quinolines / chemical synthesis
Quinolines / chemistry
Quinolines / pharmacology*
Stereoisomerism
Structure-Activity Relationship
Sulfides / chemical synthesis
Sulfides / chemistry
Sulfides / pharmacology*

Substances

Antineoplastic Agents
Quinolines
Sulfides