Implementation of a Small Molecule Chemical Library in the Search for Drug Candidates

Dácil Carballo33rd EORTC-PAMM Winter Meeting

Puerto de la Cruz, Tenerife25-28 January 2012

Introduction

Need for “real-time” biological evaluation of the compounds from the organic synthesis → quick and direct development of new analogues for further SAR studies

Adequate drug candidate: bioactivivity, physical-chemical properties, metabolic stability, safety, etc.

CHEMLIBRARY

Synthesized natural products

Simplified structure derivatives (target-oriented synthesis)

Low molecular weight

leaders(diversity-oriented

synthesis)

Non-commercial

available starting

materials and advanced synthetic

intermediates

A demonstration: how useful is a chemical library

https://openinnovation.lilly.com/dd/about-open-innovation/what-are-pd2-and-targetd2.html

BioLab Screening Program

http://webpages.ull.es/users/jmpadron/biolab/index.html

Summary

A compilation and classification into a database of the compounds from organic synthesis is carried out

The members of this chemical library are being submitted to biological assays for further SAR studies

Collaborations in order to increase the scope of available biological studies

… and it is still growing!!

AcknowledgementsBioactive Product SynthesisVíctor S. MartínMiguel A. RamírezJuan I. PadrónCelina GarcíaMartín PurinoJulio RodríguezSixto PérezSergio Álvarez BioLab

José M. PadrónLeticia G. LeónEduardo Pérez-RothCarla Ríos-LuciGastón Silveira