Triphenylmethylamides (TPMAs): Structure-activity relationship of compounds that induce apoptosis in melanoma cells

Rahul Palchaudhuri; Paul J Hergenrother

doi:10.1016/j.bmcl.2008.07.128

Triphenylmethylamides (TPMAs): Structure-activity relationship of compounds that induce apoptosis in melanoma cells

Bioorg Med Chem Lett. 2008 Nov 15;18(22):5888-91. doi: 10.1016/j.bmcl.2008.07.128. Epub 2008 Aug 3.

Authors

Rahul Palchaudhuri¹, Paul J Hergenrother

Affiliation

¹ Department of Chemistry, Roger Adams Laboratory, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA.

PMID: 18710803
DOI: 10.1016/j.bmcl.2008.07.128

Abstract

Triphenylmethylamides (TPMAs) have been previously identified as compounds that arrest cells in the G1-phase of the cell cycle and induce apoptotic death in melanoma cell lines in culture. Here we report the synthesis of a series of TPMA derivatives, allowing the structure-activity relationship of this class of molecules to be established. Several new compounds have been identified that induce death in UACC-62 and SK-MEL-5 human melanoma cell lines, including a compound with enhanced aqueous solubility.

Publication types

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

MeSH terms

Amides / chemical synthesis*
Amides / chemistry
Amides / pharmacology*
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects
Cell Line, Tumor
Drug Screening Assays, Antitumor
G1 Phase / drug effects
Humans
Melanoma / drug therapy*
Molecular Structure
Solubility
Structure-Activity Relationship

Substances

Amides
Antineoplastic Agents