hti-286 and methylamine

hti-286 has been researched along with methylamine* in 1 studies

Other Studies

1 other study(ies) available for hti-286 and methylamine

Article	Year
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286). Journal of medicinal chemistry, 2004, Sep-09, Volume: 47, Issue:19 Hemiasterlin, a tripeptide isolated from marine sponges, induces microtubule depolymerization and mitotic arrest in cells. HTI-286, an analogue from an initial study of the hemiasterlins, is presently in clinical trials. In addition to its potent antitumor effects, 2 has the advantage of circumventing the P-glycoprotein-mediated resistance that hampers the efficacy of other antimicrotubule agents such as paclitaxel and vincristine in animal models. This paper describes an in-depth study of the structure--activity relationships of analogues of 2, their effects on microtubule polymerization, and their in vitro and in vivo anticancer activity. Regions of the molecule necessary for potent activity are identified. Groups tolerant of modification, leading to novel analogues, are reported. Potent analogues identified through in vivo studies in tumor xenograft models include one superior analogue, HTI-042. Topics: Amines; Animals; Cell Death; Cell Division; Cell Line; Cyclization; Esters; Humans; Inhibitory Concentration 50; Methylamines; Mice; Microtubules; Molecular Structure; Neoplasms; Oligopeptides; Oxidation-Reduction; Peptides; Pyruvic Acid; Structure-Activity Relationship; Tubulin	2004

Article

Year

Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).

Journal of medicinal chemistry, 2004, Sep-09, Volume: 47, Issue:19

Hemiasterlin, a tripeptide isolated from marine sponges, induces microtubule depolymerization and mitotic arrest in cells. HTI-286, an analogue from an initial study of the hemiasterlins, is presently in clinical trials. In addition to its potent antitumor effects, 2 has the advantage of circumventing the P-glycoprotein-mediated resistance that hampers the efficacy of other antimicrotubule agents such as paclitaxel and vincristine in animal models. This paper describes an in-depth study of the structure--activity relationships of analogues of 2, their effects on microtubule polymerization, and their in vitro and in vivo anticancer activity. Regions of the molecule necessary for potent activity are identified. Groups tolerant of modification, leading to novel analogues, are reported. Potent analogues identified through in vivo studies in tumor xenograft models include one superior analogue, HTI-042.

Topics: Amines; Animals; Cell Death; Cell Division; Cell Line; Cyclization; Esters; Humans; Inhibitory Concentration 50; Methylamines; Mice; Microtubules; Molecular Structure; Neoplasms; Oligopeptides; Oxidation-Reduction; Peptides; Pyruvic Acid; Structure-Activity Relationship; Tubulin

2004