Gallic Acid based steroidal phenstatin analogues for selective targeting of breast cancer cells through inhibiting tubulin polymerization

被引：30

作者：

Parihar, Swati ^{[1
]}

Gupta, Atul ^{[1
]}

Chaturvedi, Amit K. ^{[1
]}

Agarwal, Jyoti ^{[1
]}

Luqman, Suaib ^{[1
]}

Changkija, Bendangla ^{[2
]}

Manohar, Murli ^{[2
]}

Chanda, Debabrata ^{[1
]}

Chanotiya, C. S. ^{[1
]}

Shanker, Karuna ^{[1
]}

Dwivedi, Anila ^{[2
]}

Konwar, Rituraj ^{[2
]}

Negi, Arvind S. ^{[1
]}

机构：

[1] Cent Inst Med & Aromat Plants CSIR CIMAP, Lucknow 226015, Uttar Pradesh, India

[2] Cent Drug Res Inst CSIR CDRI, Lucknow 226001, Uttar Pradesh, India

来源：

STEROIDS | 2012年 / 77卷 / 8-9期

关键词：

Gallic acid; Phenstatin; Anticancer; Tubulin polymerization inhibition; Acute oral toxicity; ESTROGEN-RECEPTOR; ANTINEOPLASTIC AGENTS; BIOLOGICAL EVALUATION; MICROTUBULES; RESISTANCE; PHOSPHATE;

D O I：

10.1016/j.steroids.2012.03.012

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Phenstatin analogues were synthesized on steroidal framework, for selective targeting of breast cancer cells. These analogues were evaluated for anticancer efficacy against breast cancer cell lines. Analogues 12 and 19 exhibited significant anticancer activity against MCF-7, hormone dependent breast cancer cell line. While analogues 10-14 exhibited significant anticancer activity against MDA-MB-231, hormone independent breast cancer cell line. Compound 10 showed significant oestrogen antagonistic activities with low agonistic activity in in vivo rat model. These analogues also retain tubulin polymerization inhibition activity. The most active analogue 10 was found to be non-toxic in Swiss albino mice up to 300 mg/kg dose. Gallic acid based phenstatin analogues may further be optimized as selective anti-breast cancer agents. (c) 2012 Elsevier Inc. All rights reserved.

引用

页码：878 / 886

页数：9

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