Discovery and SAR exploration of N-aryl-N-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer

Abstract

A new chemical series of antiproliferative compounds was identified via high-throughput screening on DU-145 human prostate carcinoma cell line (hit compound potency - 5.7 microM). Exploration of the two peripheral diversity vectors of the hit molecule in a hit-targeted library and testing of the resulting compounds led to SAR generalizations and identification of the 'best' pharmacophoric moieties. The latter were merged in a single compound that exhibited a 200-fold better potency than the original hit compound. Specific cancer cell cytotoxicity was confirmed for the most potent compounds.

Shown for reading. Its publisher allows quoting it, not republishing it.

References 8

1. 1.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.1038/sj.onc.1207726

2. 2.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.3322/ca.2007.0010

3. 3.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.1016/j.canlet.2008.02.065

4. 4.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.1097/ppo.0b013e318161d40f

5. 5.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.1002/ardp.200800201

6. 6.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.1016/j.febslet.2006.03.041

7. 7.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.1016/s1367-5931(99)80058-1

8. 8.

   This reference’s wording can’t be shown under the paper’s licence.

   Not in our library10.3987/com-08-11340

Reads

A person counts once a day per paper. We keep no cookie and no address: a reader is a hash that changes every day. Any month under five reads shows no number.