Featured Research

from universities, journals, and other organizations

Scientists identify key structural qualities that distinguish novel anticancer agent

Date:
December 31, 2013
Source:
Roswell Park Cancer Institute
Summary:
A research team has published its latest preclinical findings about the promising antitumor agent FL118, reporting new insights about the agent's chemical structure.

A team led by Fengzhi Li, PhD, of Roswell Park Cancer Institute has reported significant new findings regarding the chemical structure of the novel anticancer agent FL118. The research, which included comparative analysis of the agent and several similar compounds, confirms the broad, superior antitumor activity of FL118 and suggests promising directions for further studies.

In September 2012, Dr. Li and colleagues published their first findings identifying FL118 as a promising anticancer agent with unique mechanisms of action and favorable toxicity profiles. The small molecule is structurally similar to camptothecin, a component in the bark and stem of a tree native to China that has long been a traditional Chinese remedy for cancer. While thousands of agents based on camptothecin have been synthesized, and two of these analogs — irinotecan and topotecan — have been approved for treatment of many solid-tumor cancers, these compounds typically are highly toxic to healthy cells, and not all of them have proven effective as anticancer agents.

These latest findings, published in Molecular Pharmaceutics, a journal of the American Chemical Society, report on the structure-activity relationship (SAR) of the hydroxyl group within the agent’s lactone ring. The research team, which included scientists from the School of Medicine and Pharmacy at the Ocean University of China, assessed the relative efficacy of FL118 and seven new compounds derived from FL118 or a sister molecule, FL113. Consistently, FL118 was significantly more effective in inhibiting cancer-survival proteins, both in vitro and in vivo, than those analogs.

“We learned that the steric configuration of FL118, the way the atoms are arranged within the molecule, is critically important to its effectiveness as an anticancer agent,” said Dr. Li, an Associate Professor of Oncology in RPCI’s Department of Pharmacology and Therapeutics. “Specifically, we now know that a free hydroxyl group is a key component for any FL118 analogs we develop, and we’ll apply that finding as we move forward with subsequent studies. It appears that FL118 will be an outstanding model on which to base new analogs that will represent even more promising investigational therapies for personalized cancer treatment.”


Story Source:

The above story is based on materials provided by Roswell Park Cancer Institute. Note: Materials may be edited for content and length.


Journal Reference:

  1. Jiuyang Zhao, Xiang Ling, Shousong Cao, Xiaojun Liu, Shengbiao Wan, Tao Jiang, Fengzhi Li. Antitumor activity of FL118, a survivin, Mcl-1, XIAP, and cIAP2 selective inhibitor, is highly dependent on its primary structure and steric configuration. Molecular Pharmaceutics, 2013; 131215164118004 DOI: 10.1021/mp4004282

Cite This Page:

Roswell Park Cancer Institute. "Scientists identify key structural qualities that distinguish novel anticancer agent." ScienceDaily. ScienceDaily, 31 December 2013. <www.sciencedaily.com/releases/2013/12/131231132732.htm>.
Roswell Park Cancer Institute. (2013, December 31). Scientists identify key structural qualities that distinguish novel anticancer agent. ScienceDaily. Retrieved April 24, 2014 from www.sciencedaily.com/releases/2013/12/131231132732.htm
Roswell Park Cancer Institute. "Scientists identify key structural qualities that distinguish novel anticancer agent." ScienceDaily. www.sciencedaily.com/releases/2013/12/131231132732.htm (accessed April 24, 2014).

Share This



More Health & Medicine News

Thursday, April 24, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Big Pharma Braces for M&A Wave

Big Pharma Braces for M&A Wave

Reuters - Business Video Online (Apr. 22, 2014) Big pharma on the move as Novartis boss, Joe Jimenez, tells Reuters about plans to transform his company via an asset exchange with GSK, and Astra Zeneca shares surge on speculation that Pfizer is looking for a takeover. Joanna Partridge reports. Video provided by Reuters
Powered by NewsLook.com
Study Says Most Crime Not Linked To Mental Illness

Study Says Most Crime Not Linked To Mental Illness

Newsy (Apr. 22, 2014) A new study finds most crimes committed by people with mental illness are not caused by symptoms of their illness or disorder. Video provided by Newsy
Powered by NewsLook.com
Hagel Gets Preview of New High-Tech Projects

Hagel Gets Preview of New High-Tech Projects

AP (Apr. 22, 2014) Defense Secretary Chuck Hagel is given hands-on demonstrations Tuesday of some of the newest research from DARPA _ the military's Defense Advanced Research Projects Agency program. (April 22) Video provided by AP
Powered by NewsLook.com
How Smaller Plates And Cutlery Could Make You Feel Fuller

How Smaller Plates And Cutlery Could Make You Feel Fuller

Newsy (Apr. 22, 2014) NBC's "Today" conducted an experiment to see if changing the size of plates and utensils affects the amount individuals eat. Video provided by Newsy
Powered by NewsLook.com

Search ScienceDaily

Number of stories in archives: 140,361

Find with keyword(s):
Enter a keyword or phrase to search ScienceDaily for related topics and research stories.

Save/Print:
Share:

Breaking News:
from the past week

In Other News

... from NewsDaily.com

Science News

Health News

Environment News

Technology News



Save/Print:
Share:

Free Subscriptions


Get the latest science news with ScienceDaily's free email newsletters, updated daily and weekly. Or view hourly updated newsfeeds in your RSS reader:

Get Social & Mobile


Keep up to date with the latest news from ScienceDaily via social networks and mobile apps:

Have Feedback?


Tell us what you think of ScienceDaily -- we welcome both positive and negative comments. Have any problems using the site? Questions?
Mobile: iPhone Android Web
Follow: Facebook Twitter Google+
Subscribe: RSS Feeds Email Newsletters
Latest Headlines Health & Medicine Mind & Brain Space & Time Matter & Energy Computers & Math Plants & Animals Earth & Climate Fossils & Ruins