Pharmacological evaluation of C-3 modified Betulinic acid derivatives with potent anticancer activity
Pharmacological evaluation of C-3 modified Betulinic acid derivatives with potent anticancer activity
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DOI：
10.1007/s10637-007-9081-4
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发表时间：
2008-02-01
影响因子：
3.4
通讯作者：
Burman, Anand C.
中科院分区：
文献类型：
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作者：
Rajendran, Praveen;Jaggi, Manu;Burman, Anand C.
采用ADME、动物药代动力学和肿瘤研究等方法，对桦木酸（BA）和5个C-3位修饰的二氢BA衍生物[4-硝基苄基肟（1）、2 - 4-二氟苯甲酰氧基（2）、2- 4-二氟亚苄基氨基（3）、苯甲酰亚肼基（4）和4-氟苯基亚肼基（5）]进行了体外和体内药理学筛选。我们发现BA及其衍生物的水溶性很差，
In vitro and in vivo pharmacological screening of Betulinic acid (BA) and five dihydro-BA derivatives modified at C-3 position [4-nitrobenzyl-oximino (1), 2-4-difluoro-benzoyloxy (2), 2-4-difluoro-benzylidene-amino (3), benzoyl-hydrazono (4), and 4-fluorophenyl-hydrazono (5)], having potent in vitro anti-cancer activity was carried out using ADME, animal PK and tumor studies. We found that BA and the derivatives had poor aqueous solubility (