Disodium Phosphate of Novel Pyrazole-Linked Norcantharidin Analogs:Design, Synthesis and their Anticancer Evaluation

Title: Disodium Phosphate of Novel Pyrazole-Linked Norcantharidin Analogs:Design, Synthesis and their Anticancer Evaluation

Volume: 5 Issue: 5

Author(s): Liping Deng, Bo Yang, Qiaojun He and Yongzhou Hu

Affiliation:

Keywords: Pyrazole-linked, Norcantharidin analogs, Cycloadddition, Disodium phosphate, Anticancer evaluation, Solubility

Abstract: To design and synthesize novel pyrazole-linked norcanthridin analogs and their disodium phosphates by [3+2]1, 3-dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with three hydrazines. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumor cell lines: KB, SMMC-7721, SGC7901, ECA109, HO-8910, K562, A549 and MCF-7 producing IC50 values from 0.07 μM to > 100 μM. Compound 8c showed potency for the treatment of hepatoma, with IC50 value to SMMC-7721 cell line comparable to that of norcantharidin. High potency and selectivity of compound 12 to MCF-7 cell line prove that the phosphorylation of norcantharidin analogs is an effective way to increase the activity and solubility.

Cite this article as:

Deng Liping, Yang Bo, He Qiaojun and Hu Yongzhou, Disodium Phosphate of Novel Pyrazole-Linked Norcantharidin Analogs:Design, Synthesis and their Anticancer Evaluation, Letters in Drug Design & Discovery 2008; 5 (5) . https://dx.doi.org/10.2174/157018008784912054