Synthesis of neolignans as microtubule stabilisers
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- 作者：B. Sathish Kumar ; Aastha Singh ; Amit Kumar ; Jyotsna Singh ; Mohammad Hasanain ; Arjun Singh ; Nusrat Masood ; Dharmendra K. Yadav ; Rituraj Konwar ; Kalyan Mitra ; Jayanta Sarkar ; Suaib Luqman ; Anirban Pal ; Feroz Khan ; Debabrata Ch ; a ; Arvind S. Negi
- 关键词：Neolignans ; Lignans ; Anticancer ; Microtubules ; In silico studies ; Acute oral toxicity
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：15 February, 2014
- 年：2014
- 卷：22
- 期：4
- 页码：1342-1354
- 全文大小：2134 K
文摘
Tubulin is a well established target for anticancer drug development. Lignans and neolignans were synthesized as tubulin interacting agents. Neolignans 10 and 19 exhibited significant anticancer activity against MCF-7 and MDAMB-231 human breast cancer cell lines. Both the compounds effectively induced stabilization of microtubule at 4 and 20 渭M concentrations respectively. Neolignan 10 induced G2/M phase arrest in MCF-7 cells. Docking experiments raveled that 10 and 19 occupied the same binding pocket of paclitaxel with some difference in active site amino acids and good bioavailability of both the compounds. In in vivo acute oral toxicity 10 was well tolerated up to 300 mg/kg dose in Swiss-albino mice.