Abstract: Disclosed are devices and methods for preparing pre-metabolized compound libraries and for screening compound metabolites in a high throughput format. The devices and methods disclosed herein increase the chemical diversity of a chemical library prior to screening, and thereby enhance the number and value of hits identified in such chemical screening efforts.

Abstract: A fraction separated from crude crocetin by preparative HPLC, and identified using LC/MS and NMR as crocetinic acid, markedly regressed the proliferation and increased apoptosis in pancreatic cancer cells. Purified crocetinic acid showed more potency than 15 commercial or crude crocetin using proliferation and apoptosis as markers. Purified crocetinic acid also showed significant anti-tumorigenic activity against pancreatic cancer cells in a mouse model of pancreatic cancer. Given crocetinic acid's low toxicity, crocetinic acid could be used as a chemotherapeutic or chemopreventative agent for pancreatic cancer.

Abstract: An in vivo method of inhibiting tumor growth, specifically pancreatic cancer, includes administering to a subject in need thereof an effective amount of a compound, composition, and/or a pharmaceutical formulation including crocetinic acid.

Abstract: An in vivo method of inhibiting tumor growth, specifically pancreatic cancer, includes administering to a subject in need thereof an effective amount of a compound, composition, and/or a pharmaceutical formulation including crocetinic acid.

Abstract: A fraction separated from crude crocetin by preparative HPLC, and identified using LC/MS and NMR as crocetinic acid, markedly regressed the proliferation and increased apoptosis in pancreatic cancer cells. Purified crocetinic acid showed more potency than 15 commercial or crude crocetin using proliferation and apoptosis as markers. Purified crocetinic acid also showed significant anti-tumorigenic activity against pancreatic cancer cells in a mouse model of pancreatic cancer. Given crocetinic acid's low toxicity, crocetinic acid could be used as a chemotherapeutic or chemopreventative agent for pancreatic cancer.

Abstract: The present invention provides a process for preparing an immobilized peptide derivative of formula (Vb): comprising reacting a functionalized solid support comprising Sub-L wherein Sub is a solid support and L is a cleavable linker, with H—[NH—A—C(O)]—O(tBu), then reacting the immobilized product with compound of the formula RHN—A—C(O)OH, wherein the RHN—A—C(O) group is the residue of a N-protected ?-amino acid, in the presence of a coupling agent, to yield an immobilized peptide derivative of the formula (Vb).

Abstract: The present invention provides a process for preparing a peptide of formula (I): Sub-[L]-[NH-A-C(O)]n+m—OH ??(I) comprising: (a) reacting an immobilized compound of formula (II): Sub-(L)-[NH-A-C(O)]n—OH ??(II) with an amino acid ester or peptide derivative of formula (III): H—[NH-A-C(O)]m—O(tBu) ??(III) in the presence of a coupling agent to yield a peptide compound of general formula (IV): Sub-[L]-[NH-A-C(O)]n+m—O(tBu); ??(IV) (b) removing the tBu (t-butyl) group to produce a solid-support bound carboxylic acid or peptide derivative of general formula (I); wherein n is a positive integer, e.g., 1-10, preferably 1-5; m is a positive integer.

Abstract: The present invention provides a process for preparing a peptide of formula I): Sub-[L]-[N(R1)-A-C(O)]p—[NH-A-C(O)]n+m—OH??(I) comprising: (a) reacting an immobilized compound of formula (II): Sub-(L)-[N(R1)-A-C(O)]p—[NH-A-C(O)]n—OH??(II) with an amino acid ester or peptide derivative of formula (III): H—[NH-A-C(O)]m—O(tBu)??(III) in the presence of a coupling agent to yield a peptide compound of general formula (IV): Sub-[L]-[N(R1)-A-C(O)]p—[NH-A-C(O)]n+m—O(tBu);??(IV) (b) removing the tBu (t-butyl) group to produce a solid-support bound carboxylic acid or peptide derivative of general formula (I); wherein n is a positive integer, e.g., 1–10, preferably 1–5; m is a positive integer, and P is 0–1.

Abstract: The present invention provides a process for preparing a peptide of formula (I): Sub-[L]-[NH-A-C(O)]n+m—OH??(I) comprising: (a) reacting an immobilized compound of formula (II): Sub-(L)-[NH-A-C(O)]n—OH??(II) ?with an amino acid ester or peptide derivative of formula (III): H—[NH-A-C(O)]m—O(tBu)??(III) ?in the presence of a coupling agent to yield a peptide compound of general formula (IV): Sub-[L]-[NH-A-C(O)]n+m—O(tBu);??(IV) (b) removing the tBu (t-butyl) group to produce a solid-support bound carboxylic acid or peptide derivative of general formula (I); wherein n is a positive integer, e.g., 1-10, preferably 1-5; m is a positive integer.

Abstract: The present invention provides a process for preparing a peptide of formula (I):

Abstract: The present invention provides methods and pharmaceutical preparations for inhibiting the growth of bacterial microorganisms.