Synthesis and evaluation of anticancer activity of novel andrographolide derivatives

A series of 3,19- O -acetal derivatives of andrographolide ( 1 ) have been synthesized by protecting the hydroxyls at C-3 and C-19 through a novel route. All the derivatives were evaluated for in vitro anticancer activity. Among the synthesized derivatives, compounds 3 , 3a , 3d , 3e , 7 and 8 showe...

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Published in:MedChemComm 2015-05, Vol.6 (5), p.898-904
Main Authors: Devendar, Ponnam, Nayak, Vadithe Lakshma, Yadav, Dharmendra Kumar, Kumar, Arigari Niranjana, Kumar, Jonnala Kotesh, Satya Srinivas, KVN, Sridhar, Balasubramanian, Khan, Feroz, Sastry, Kakaraparthi Pandu, Ramakrishna, Sistla
Format: Article
Language:English
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Summary:A series of 3,19- O -acetal derivatives of andrographolide ( 1 ) have been synthesized by protecting the hydroxyls at C-3 and C-19 through a novel route. All the derivatives were evaluated for in vitro anticancer activity. Among the synthesized derivatives, compounds 3 , 3a , 3d , 3e , 7 and 8 showed potential cytotoxicity against human cancer cell lines A549 (lung), HeLa (cervical), ACHN (renal), B-16 (melanoma) and IEC-6 (small intestine). The binding mode conformation was evaluated through docking simulations, while bioavailability/drug-likeness was evaluated through predictive ADME screening studies. All the derivatives were characterized by spectroscopy and the stereochemistry of compounds 3a and 3e was also confirmed by X-ray analysis.
ISSN:2040-2503
2040-2511
DOI:10.1039/C4MD00566J