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228266-40-8

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Absolute configurations of tubulin inhibitors taltobulin (HTI-286) and HTI-042 characterized by X-ray diffraction analysis and NMR studies
The stereochemistry of the tubulin inhibitors taltobulin HTI-286 (2) and HTI-042 (3) was determined by utilizing the DPFGSE 1D NOE experiment. Single crystal X-ray diffraction analysis further confirmed the absolute configuration of these two compounds, w
Niu, Chuansheng,Ho, Douglas M.,Zask, Arie,Ayral-Kaloustian, Semiramis
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p. 1535 - 1538
(2010/06/21)

D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors
Modifications of the D-piece carboxylic acid group of the hemiasterlin analog HTI-286 gave tubulin inhibitors which were potent cytotoxic agents in taxol resistant cell lines expressing P-glycoprotein. Amides derived from proline had potency comparable to HTI-286. Reduction of the carboxylic acid to ketones and alcohols or its conversion to acidic heterocycles also gave potent analogs. Synthetic modifications of the carboxylic acid could be carried out selectively using a wide range of synthetic reagents. Proline analog 3 was found to be effective in a human xenograft model in athymic mice.
Zask, Arie,Birnberg, Gary,Cheung, Katherine,Kaplan, Joshua,Niu, Chuan,Norton, Emily,Yamashita, Ayako,Beyer, Carl,Krishnamurthy, Girija,Greenberger, Lee M.,Loganzo, Frank,Ayral-Kaloustian, Semiramis
p. 4353 - 4358
(2007/10/03)

More Articles about upstream products of 228266-40-8

676629-67-7
N-{1-[(1-formyl-2-methyl-propyl)-methyl-carbamoyl]-2,2-dimethyl-propyl}-3-methyl-2-methylamino-3-phenyl-butyramide

Chemical Properties

Melting Point: 135-137 °C
Boiling Point: 662.4 °C at 760 mmHg
Flash Point:354.4 °C
Density: 1.063 g/cm³
Storage Temp.:Sealed in dry,Store in freezer, under -20°C
PKA: 4.68±0.19(Predicted)
PSA: 98.74000
LogP: 4.37880

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