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Discovery of Novel Allopurinol Derivatives With Anticancer Activity and Attenuated Xanthine Oxidase Inhibition

Discovery of Novel Allopurinol Derivatives With Anticancer Activity and Attenuated Xanthine Oxidase Inhibition

Yong Li, Ting-Ting Cao, Shanchun Guo, Qiu Zhong, Cai-Hu Li, Ying Li, Lin Dong, Shilong Zheng, Guangdi Wang, Shu-Fan Yin

Molecules. 2016 Jun 20;21(6):771.

PMID: 27331805

Abstract:

A series of pyrazolo[3,4-d]pyrimidine derivatives related to allopurinol has been synthesized and evaluated for its cytotoxicity against a panel of three cancer cell lines as well as its xanthine oxidase (XOD) inhibitory activities. Among them, compound 4 showed potent cytotoxicity with IC50 values of 25.5 and 35.2 μM against human hepatoma carcinoma cell lines, BEL-7402 and SMMC-7221, respectively. The anticancer activity of 4 was comparable to that of Tanespimycin (17-N-allylamino-17-demethoxy geldanamycin, 17-AAG) that inhibited the growth of BEL-7402 and SMMC-7221 cells at IC50 values of 12.4 and 9.85 μM, respectively. However, unlike allopurinol, which is also a strong inhibitor of XOD, compound 4 is a much weaker XOD inhibitor, suggesting that the anticancer activities of the allopurinol derivatives may not be associated with XOD inhibition. Moreover, the cytotoxicity of 4 toward normal cells is significantly lower than that of 17-AAG, making 4 a promising lead compound for further optimization of structure-activity relationships that may lead to anticancer agents of clinical utility.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP27511791	Allopurinol Related Compound A		27511-79-1	Price
AP6994258	Allopurinol Related Compound D		6994-25-8	Price

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