Chemically engineered extracts as an alternative source of bioactive natural product-like compounds.

@article{citeulike:1084722, abstract = {The access to libraries of molecules with interesting biomolecular properties is a limiting step in the drug discovery process. By virtue of a long molecular evolution process, natural products are recognized as biologically validated starting points in structural space for library development. We introduce here a strategy to generate natural product-like libraries. A semisynthetic mixture of compounds was produced by diversification of a natural product extract through the chemical transformation of common chemical functionalities in natural products into chemical functionalities rarely found in nature. The resulting mixture showed antifungal activity against Candida albicans, whereas the starting extract did not show such activity. Bioguided fractionation led to the isolation of a previously undescribed active semisynthetic pyrazole. The result illustrates how biological activity can be generated by designed chemical diversification of a natural product mixture, and represents the proof of principle of an alternative strategy for producing natural product-like libraries from natural products libraries.}, address = {Farmacognosia, Facultad de Ciencias Bioqu\'{i}micas y Farmac\'{e}uticas, Universidad Nacional de Rosario. Suipacha 531, S2002LRK Rosario, Argentina.}, author = {L\'{o}pez, S. N. and Ramallo, I. A. and Sierra, M. G. and Zacchino, S. A. and Furlan, R. L. }, citeulike-article-id = {1084722}, doi = {10.1073/pnas.0608438104}, issn = {0027-8424}, journal = {Proc Natl Acad Sci U S A}, keywords = {jr20070305}, month = {January}, number = {2}, pages = {441--444}, posted-at = {2007-02-20 05:28:10}, priority = {2}, title = {Chemically engineered extracts as an alternative source of bioactive natural product-like compounds.}, url = {http://dx.doi.org/10.1073/pnas.0608438104}, volume = {104}, year = {2007} }

TY - JOUR ID - citeulike:1084722 L3 - citeulike-article-id:1084722 TI - Chemically engineered extracts as an alternative source of bioactive natural product-like compounds. JF - Proc Natl Acad Sci U S A VL - 104 IS - 2 SP - 441 EP - 444 AD - Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario. Suipacha 531, S2002LRK Rosario, Argentina. SN - 0027-8424 N2 - The access to libraries of molecules with interesting biomolecular properties is a limiting step in the drug discovery process. By virtue of a long molecular evolution process, natural products are recognized as biologically validated starting points in structural space for library development. We introduce here a strategy to generate natural product-like libraries. A semisynthetic mixture of compounds was produced by diversification of a natural product extract through the chemical transformation of common chemical functionalities in natural products into chemical functionalities rarely found in nature. The resulting mixture showed antifungal activity against Candida albicans, whereas the starting extract did not show such activity. Bioguided fractionation led to the isolation of a previously undescribed active semisynthetic pyrazole. The result illustrates how biological activity can be generated by designed chemical diversification of a natural product mixture, and represents the proof of principle of an alternative strategy for producing natural product-like libraries from natural products libraries. KW - jr20070305 AU - López, SN AU - Ramallo, IA AU - Sierra, MG AU - Zacchino, SA AU - Furlan, RL PY - 2007/01/09/ UR - http://dx.doi.org/10.1073/pnas.0608438104 ER -