Synthesis and evaluation of anticancer activity of novel andrographolide derivatives

Autor:	Balasubramanian Sridhar, Vadithe Lakshma Nayak, Feroz Khan, Kakaraparthi Pandu Sastry, Kvn Satya Srinivas, Ponnam Devendar, Jonnala Kotesh Kumar, Sistla Ramakrishna, Dharmendra Kumar Yadav, Arigari Niranjana Kumar
Rok vydání:	2015
Předmět:	Pharmacology biology Chemistry Stereochemistry Andrographolide Organic Chemistry Pharmaceutical Science biology.organism_classification Biochemistry In vitro Bioavailability HeLa chemistry.chemical_compound Cell culture Docking (molecular) Drug Discovery Molecular Medicine Cytotoxicity ADME
Zdroj:	MedChemComm. 6:898-904
ISSN:	2040-2511 2040-2503
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::fbdd5e26cde57da8390c677e62188e10 https://doi.org/10.1039/c4md00566j Zobrazit plný text záznamu